- Design, synthesis, in silico analysis with PPAR-γ receptor and study of non-covalent interactions in unsymmetrical heterocyclic/phenyl fleximer
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This work deals with the design, synthesis, in silico analysis, crystallization, and the interpretation 2-cyano-3-{4-[2-(phthalimid-nyl)-propoxy]-phenyl}-acrylic acid ethyl ester (7). Analog 7 is designed based on rosiglitazone. The quantitative analysis
- Singh, Ved Prakash,Dowarah, Jayanta,Marak, Brilliant N.,Tewari, Ashish Kumar
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Read Online
- β-Carboline-functionalized dithioacetal as Hg2+-selective fluorescence probe in water
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A novel sensing system based on the β-carboline core has been designed and synthesized for Hg2+ detection in water. We have demonstrated that a straight forward methodology can provide rapid, sensitive and selective recognition (cross-contamination experiments) for Hg2+ over a wide pH range. The vivid fluorescence change from blue to colorless can be clearly discriminated by the naked eye. Furthermore, there is a good negative correlation between the fluorescent intensity and the concentration of Hg2+ in the range 1.0 × 10-6 M-7.0 × 10-6 M. β-Carboline as a fluorophore synthesized via this route also provides a new strategy for the design of novel fluorescence probes and fluorochromes.
- Li, Na,Dai, Jiang-Kun,Du, Hong-Tao,Yuan, Mao-Sen,Zhang, Ji-Wen,Wang, Jun-Ru
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Read Online
- Bimodal detection of carbon dioxide using fluorescent molecular aggregates
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Cyano-substituted p-phenylenevinylene (R-1) aggregates exhibiting fluorescence and Raman spectroscopic responses towards CO2 are described. The aggregation-induced emission (AIE) as well as the aggregation-enhanced Raman scattering (AERS) of R-
- Mishra, Rakesh K.,Vijayakumar, Samiyappan,Mal, Arindam,Karunakaran, Varsha,Janardhanan, Jith C.,Maiti, Kaustabh Kumar,Praveen, Vakayil K.,Ajayaghosh, Ayyappanpillai
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Read Online
- Synthesis of novel dithiocarbamyl-containing organosilicon compounds
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Aldehydes-bearing dithiocarbamate moieties were generated via highly efficient and simple method based on the one-pot reaction of amines, CS2, and 4-(bromoalkoxy)benzaldehydes with the use of K2CO3 as a catalyst under solv
- Safa, Kazem D.,Tavakkoli Osgoei, Sama,Alyari, Maryam
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Read Online
- Synthesis, Characterization and Biological Evaluation of Novel Triazole Linked Chromone Biheterocycle Analogs
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The current work focused on the synthesis of novel chromone biheterocycle analogs followed by its characterization through physicochemical and spectral techniques like FTIR, mass and NMR spectroscopy. The basic triazole heterocycle and its analogs have di
- Kalyani, Gade,Reddy, D. Ravisankar,Soujanya, Jilla
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- Development of novel tetrahydroisoquinoline-hydroxamate conjugates as potent dual SERDs/HDAC inhibitors for the treatment of breast cancer
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Concomitant inhibition of estrogen receptor alpha (ERα) and histone deacetylase (HDAC) signaling has been proven effective in endocrine-resistant ER+ breast cancers. Herein, a series of tetrahydroisoquinoline (THIQ)-hydroxamate conjugates were rationally
- Luo, Guoshun,Lin, Xin,Ren, Shengnan,Wu, Shuangjie,Wang, Xin,Ma, Luyu,Xiang, Hua
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supporting information
(2021/10/04)
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- Controlled Reduction of Nitriles by Sodium Hydride and Zinc Chloride
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A new protocol for the controlled reduction of nitriles to aldehydes was developed using a combination of sodium hydride and zinc chloride. The iminyl zinc intermediates derived from aromatic nitriles could be further functionalized with allylmetal nucleophiles to afford homoallylamines. As the method allows the reduction of various aliphatic and aromatic nitriles with a concise procedure under milder reaction conditions and exhibits wide functional group compatibility, it is well suited for use in various opportunities in chemical synthesis.
- Chiba, Shunsuke,Ong, Derek Yiren
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p. 1369 - 1378
(2020/04/27)
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- IMIDAZO [2, 1-F] [1, 2, 4] TRIAZIN-4-AMINE DERIVATIVES AS TLR7 AGONIST
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Disclosed herein is an imidazo [2, 1-f] [1, 2, 4] triazin-4-amine derivative or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof useful as a TLR7 agonist, and a pharmaceutical composition comprising the same. Also disclosed herein is a method of treating cancer using the imidazo [2, 1-f] [1, 2, 4] triazin-4-amine derivative or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof as TLR7 agonist.
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Paragraph 0287-0288
(2020/08/22)
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- A dual-acting 5-HT6 receptor inverse agonist/MAO-B inhibitor displays glioprotective and pro-cognitive properties
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The complex etiology of Alzheimer's disease has initiated a quest for multi-target ligands to address the multifactorial causes of this neurodegenerative disorder. In this context, we designed dual-acting 5-HT6 receptor (5-HT6R) anta
- Canale, Vittorio,Grychowska, Katarzyna,Kurczab, Rafa?,Ryng, Mateusz,Keeri, Abdul Raheem,Sata?a, Grzegorz,Olejarz-Maciej, Agnieszka,Koczurkiewicz, Paulina,Drop, Marcin,Blicharz, Klaudia,Piska, Kamil,P?kala, El?bieta,Janiszewska, Paulina,Krawczyk, Martyna,Walczak, Maria,Chaumont-Dubel, Severine,Bojarski, Andrzej J.,Marin, Philippe,Popik, Piotr,Zajdel, Pawe?
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supporting information
(2020/09/21)
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- Tuning on and off chemical- And photo-activity of exfoliated MoSe2nanosheets through morphologically selective "soft" covalent functionalization with porphyrins
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The covalent functionalization of 2D transition metal dichalcogenides (TMDCs) with organic molecules exploiting the thiol conjugation approach is still a very controversial topic. We have synthesized thiolated tetraphenyl porphyrins, with and without hydr
- Agnoli, Stefano,Blanco, Matías,Bortoli, Marco,Girardi, Leonardo,Granozzi, Gaetano,Lunardon, Marco,Mosconi, Dario,Orian, Laura
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supporting information
p. 11019 - 11030
(2020/08/19)
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- Compound for treating schizophrenia and application of compound
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The invention provides an H3 receptor compound and an application thereof. In vitro experiments of the compound show that the compound has high affinity to H3, suggesting that negative symptoms and cognitive disorders can be improved. Compared with risper
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Paragraph 0082; 0083; 0084
(2019/02/03)
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- Development of chalcone-O-alkylamine derivatives as multifunctional agents against Alzheimer's disease
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A series of novel chalcone-O-alkylamine derivatives were designed, synthesized and evaluated as multifunctional anti-Alzheimer's disease agents. Based on the experimental results, compound 23c exhibited good inhibitory potency on both acetylcholinesterase
- Bai, Ping,Wang, Keren,Zhang, Pengfei,Shi, Jian,Cheng, Xinfeng,Zhang, Qi,Zheng, Cheng,Cheng, Yao,Yang, Jian,Lu, Xiaoxia,Sang, Zhipei
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- Governing the DNA-binding mode of styryl dyes by the length of their alkyl substituents-from intercalation to major groove binding
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A series of monomeric and homodimeric 4-alkoxystyryl(pyridinium) dyes was synthesized and their DNA-binding properties were investigated. We found that the length of the alkyl substituent has a crucial influence on the binding mode of the dyes, although t
- Berdnikova, Daria V.,Sosnin, Nikolai I.,Fedorova, Olga A.,Ihmels, Heiko
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p. 545 - 554
(2018/02/07)
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- Synthesis, characterization, and antimycobacterial activity of novel thymol-triazole hybrids
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Thymol is a naturally occurring phenolic compound showing various biological activities. A library of novel thymol-triazole hybrids was synthesized and evaluated for their inhibitory activity against Mycobacterium tuberculosis (M.tb), the causative agent of TB. Most of the compounds were found to be active against M.tb H37Rv at 50 μg/mL concentration. These identified compounds have promise to be further optimized into more potent inhibitors against M.tb.
- Negi, Beena,Rawat, Diwan S
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p. 113 - 124
(2018/09/14)
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- An efficient multigram-scale synthesis of 4-(ω-chloroalkoxy)phenols
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Efficient multigram two-step syntheses of 4-(2-chloroethoxy)phenol and 4-(3-chloropropoxy)phenol in >70% yields starting from 4-hydroxybenzaldehyde and reagents with general formula Cl(CH2)nX (X = Cl, n = 2; X = OTs, n = 3) are proposed. 4-(2-Chloroethoxy)phenol can also be conveniently prepared from 4-methoxyphenol and 1,2-dichloroethane. The compounds thus obtained can be used in carbohydrate chemistry to synthesize glycosides bearing "universal" 4-(ω-chloroalkoxy)phenyl aglycons.
- Zinin,Stepanova,Jost,Kondakov,Shpirt,Chizhov,Torgov,Kononov
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p. 304 - 312
(2017/07/11)
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- Synthesis of Imidazole and Theophylline Derivatives Incorporating Pyrimidine-Fused Heterocycles Using Magnetic Nanoparticles-Supported Tungstic Acid (MNP-TA) Catalyst
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In the current study, divers pyrimidine-fused heterocycles containing an imidazole, benzimidazole, or theophylline moieties were synthesized. For the synthesis of this category of compounds, first, some new bromo-substituted aldehydes (BSAs) were synthesi
- Divar, Masoumeh,Panahi, Farhad,Shariatipour, Sayedeh Rojin,Khalafi-Nezhad, Ali
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p. 660 - 669
(2017/02/04)
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- A Strategy for Specific Fluorescence Imaging of Monoamine Oxidase A in Living Cells
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Monoamine oxidase (MAO) has two isoforms, MAO-A and MAO-B, which show different functions, and thus selective fluorescence imaging is important for biological studies. Currently, however, specific detection of MAO-A remains a great challenge. Herein, we r
- Wu, Xiaofeng,Shi, Wen,Li, Xiaohua,Ma, Huimin
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supporting information
p. 15319 - 15323
(2017/11/30)
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- Preparation method of aromatic compound containing sulfydryl, and applications of aromatic compound in preventing HIV
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The invention discloses a preparation method of an aromatic compound containing sulfydryl, and applications of the aromatic compound in preventing HIV. The aromatic compound possesses a structure represented by formula I. Host self conservative cell prote
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Paragraph 0082; 0083; 0084
(2017/04/28)
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- Magnetic Fe3O4-BF3: Highly efficient Lewis acid catalyst for the synthesis of α-aminonitriles
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Fe3O4 magnetic nanoparticle-supported BF3 was prepared as a new magnetically separable Lewis acid catalyst and successfully used for the one-pot synthesis of α-aminonitriles. A broad range of substrates including the aromatic and heteroaromatic aldehydes, cyclic ketones (cyclopentanone, cyclohexanone and cycloheptanone), aryl-alkyl ketones, diaryl ketones and tetralones, isatin derivatives and acenaphthenequinone were condensed with amines (aliphatic and aromatic) and trimethylsilyl cyanide. All reactions were completed in short times and products were obtained in good to excellent yields. The catalyst could be recycled and reused several times without any loss of efficiency. Finally, α-aminonitrile containing adenine was successfully synthesized.
- Shekouhy, Mohsen,Moaddeli, Ali,Khalafi-Nezhad, Ali
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p. 3805 - 3827
(2016/04/05)
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- A novel BODIPY -Schiff base-based colorimetric and fluorometric dosimeter for Hg2+, Fe3+ and Au3+
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A novel Schiff base-based multi-target dosimeter for Hg2+, Fe3+ and Au3+ has been designed and synthesized. Upon addition of Hg2+, Fe3+ and Au3+ to the aqueous solution of compound BODIPY-TRIA, the dosimeter gave a rapid fluorescence response and displayed an obvious fluorescence enhancement with a blue-shift. Meanwhile, a sharp color change from purple to pale yellow occurred, which was readily detected by the naked eye. The hydrolysis of the Schiff base promoted by Hg2+, Fe3+ and Au3+ has been discussed, and the possible mechanism was confirmed by 1H NMR and MS studies. The dosimeter showed high sensitivity (10 nM for Au3+), good stability, and excellent selectivity for Hg2+, Fe3+ and Au3+ with interference by other metal ions.
- Cheng, Huan-Ren,Qian, Ying
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p. 82887 - 82893
(2015/10/19)
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- A fluorescent "turn on" chemosensor based on Bodipy-anthraquinone for Al(III) ions: Synthesis and complexation/spectroscopic studies
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A novel triazole-linked Bodipy-anthraquinone compound (Bodipy-A) was easily prepared through one step click chemistry. Bodipy-A displayed a remarkable increase in fluorescence intensity in the presence of trace amounts of Al(III). These changes could be a
- Kursunlu, Ahmed Nuri
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p. 41025 - 41032
(2015/05/20)
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- Multitarget-directed resveratrol derivatives: Anti-cholinesterases, anti-β-amyloid aggregation and monoamine oxidase inhibition properties against Alzheimer's disease
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Considering the complex pathogenesis factors of Alzheimer's disease (AD), the multitarget-directed ligand strategy is expected to provide superior effects to fight AD, instead of the classic one-drug-one-target strategy. Resveratrol, exhibiting important properties against AD, was suggested to be used as a starting compound for the treatment of AD. Based on these reasons, a series of resveratrol derivatives were designed, synthesized and biologically evaluated. Among them, compound 6r, exhibiting moderate cholinesterase inhibition activity (AChE, IC50 = 6.55 μM; BuChE, IC50 = 8.04 μM; SI = 1.23), significant inhibition of Aβ42 aggregation (57.78%, at 20 μM) and acceptable inhibitory activity against monoamine oxidases (MAO-A, IC50 = 17.58 μM; MAO-B, IC50 = 12.19 μM), was a potential anti-Alzheimer agent with balanced activities. Consequently, this study provided useful information for further development of resveratrol derivatives as multitarget-directed agents for AD therapy. This journal is the Partner Organisations 2014.
- Pan, Long-Fei,Wang, Xiao-Bing,Xie, Sai-Sai,Li, Su-Yi,Kong, Ling-Yi
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supporting information
p. 609 - 616
(2014/05/06)
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- Synthesis of novel 1,2,3-triazole derivatives of isoniazid and their in vitro and in vivo antimycobacterial activity evaluation
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We report herein the synthesis and antimycobacterial activity of 1,2,3-triazole derivatives of isoniazid. Most of the compounds exhibited potent activity against Mycobacterium tuberculosis H37Rv strain with MIC99 values ranging from 0.195 to 1.
- Kumar, Deepak,Beena,Khare, Garima,Kidwai, Saqib,Tyagi, Anil K.,Singh, Ramandeep,Rawat, Diwan S.
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p. 301 - 313
(2014/06/09)
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- Synthesis and characterization of 1H-phenanthro[9,10-d]imidazole derivatives as multifunctional agents for treatment of Alzheimer's disease
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Background Alzheimer's disease (AD) is a progressive neurodegenerative brain disorder that is characterized by dementia, cognitive impairment, and memory loss. Diverse factors are related to the development of AD, such as increased level of β-amyloid (Aβ), acetylcholine, metal ion deregulation, hyperphosphorylated tau protein, and oxidative stress. Methods The following methods were used: organic syntheses of 1H-phenanthro[9,10-d] imidazole derivatives, inhibition of self-mediated and metal-induced Aβ1-42 aggregation, inhibition studies for acetylcholinesterase and butyrylcholinesterase, anti-oxidation activity studies, CD, MTT assay, transmission electron microscopy, dot plot assay, gel electrophoresis, Western blot, and molecular docking studies. Results We synthesized and characterized a new type of 1H-phenanthro[9,10-d]imidazole derivatives as multifunctional agents for AD treatment. Our results showed that most of these derivatives exhibited strong Aβ aggregation inhibitory activity. Compound 9g had 74% Aβ1-42 aggregation inhibitory effect at 10 μM concentration with its IC50 value of 6.5 μM for self-induced Aβ1-42 aggregation. This compound also showed good inhibition of metal-mediated (Cu2 + and Fe2 +) and acetylcholinesterase-induced Aβ1-42 aggregation, as indicated by using thioflavin T assay, transmission electron microscopy, gel electrophoresis, and Western blot. Besides, compound 9g exhibited cholinesterase inhibitory activity, with its IC50 values of 0.86 μM and 0.51 μM for acetylcholinesterase and butyrylcholinesterase, respectively. In addition, compound 9g showed good anti-oxidation effect with oxygen radical absorbance capacity (ORAC) value of 2.29. Conclusions Compound 9g was found to be a potent multi-target-directed agent for Alzheimer's disease. General significance Compound 9g could become a lead compound for further development as a multi-target-directed agent for AD treatment.
- Liu, Jinggong,Qiu, Jun,Wang, Mingxue,Wang, Ling,Su, Lijuan,Gao, Jinbo,Gu, Qiong,Xu, Jun,Huang, Shi-Liang,Gu, Lian-Quan,Huang, Zhi-Shu,Li, Ding
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p. 2886 - 2903
(2014/07/21)
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- Synthesis of α-aminonitriles with benzimidazolic and theophyllinic backbones using the strecker reaction
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An example of the application of the Strecker reaction in the synthesis of a new class of α-aminonitriles with benzimidazole and theophylline backbones has been developed. For the synthesis of these compounds, first 4-hydroxybenzaldehyde was reacted with
- Khalafi-Nezhad, Ali,Divar, Masoumeh,Panahi, Farhad
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p. 10902 - 10908
(2013/11/19)
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- Facile assembly of Bodipy-based metal ion sensor using click chemistry
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In this study, two novel 4,4′-difluoro-4-bora-3a,4a-diaza-s-indacenes (BODIPY)-based metal ion sensors were synthesised using click chemistry. The coordination modes and binding constants of the complexes formed with a range of metal ions were calculated.
- Kursunlu, Ahmed Nuri,Gueler, Ersin
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p. 512 - 521
(2013/09/12)
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- 99mTc-labeled dibenzylideneacetone derivatives as potential SPECT probes for in vivo imaging of β-amyloid plaque
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Four 99mTc-labeled dibenzylideneacetone derivatives and corresponding rhenium complexes were successfully synthesized and biologically evaluated as potential imaging probes for Aβ plaques using SPECT. All rhenium complexes (5a-d) showed affinit
- Yang, Yanping,Cui, Mengchao,Jin, Bing,Wang, Xuedan,Li, Zijing,Yu, Pingrong,Jia, Jianhua,Fu, Hualong,Jia, Hongmei,Liu, Boli
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- Synthesis, antimalarial activity and cytotoxic potential of new monocarbonyl analogues of curcumin
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A series of novel monocarbonyl analogues of curcumin have been designed, synthesized and tested for their activity against Molt4, HeLa, PC3, DU145 and KB cancer cell lines. Six of the analogues showed potent cytotoxicity towards these cell lines with IC50 values below 1 μM, which is better than doxorubicin, a US FDA approved drug. Several analogues were also found to be active against both CQ-resistant (W2 clone) and CQ-sensitive (D6) strains of Plasmodium falciparum in an in-vitro antimalarial screening. This level of activity warrants further investigation of the compounds for development as anticancer and antimalarial agents.
- Manohar, Sunny,Khan, Shabana I.,Kandi, Shamseer Kulangara,Raj, Kranthi,Sun, Guojing,Yang, Xiaochuan,Calderon Molina, Angie D.,Ni, Nanting,Wang, Binghe,Rawat, Diwan S.
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supporting information
p. 112 - 116
(2013/02/23)
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- Synthesis of new optically active 2-pyrrolidinones
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A new class of optically active 2-pyrrolidinones was synthesized, starting from S-pyroglutamic acid, a well known natural chiral synthon. The synthetic design followed led to the insertion of various substituents at positions 1 and 5 of the 2-pyrrolidinone ring, including the imidazole moiety. Some of them possess two or three stereogenic centers, the configuration of which was retained under the mild conditions used. The new compounds also carry an imidazole moiety, which, along with the 2-pyrrolidinone template, may prove pivotal to several biological processes.
- Moutevelis-Minakakis, Panagiota,Papavassilopoulou, Eleni,Mavromoustakos, Thomas
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- Synthesis and biological evaluation of nitric oxide releasing derivatives of 6-amino-3-n-butylphthalide as potential antiplatelet agents
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A series of novel nitric oxide releasing derivatives of 6-amino-3-n-butylphthalide were designed, synthesized and evaluated as potential antiplatelet agents. Compound 10b significantly inhibited the adenosine diphosphate (ADP)-induced platelet aggregation
- Wang, Xiaoli,Wang, Linna,Huang, Zhangjian,Sheng, Xiao,Li, Tingting,Ji, Hui,Xu, Jinyi,Zhang, Yihua
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p. 1985 - 1988
(2013/05/09)
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- 1,4-naphthoquinone cations as antiplasmodial agents: Hydroxy-, acyloxy-, and alkoxy-substituted analogues
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Cations of hydroxy-substituted 1,4-naphthoquinones were synthesized and evaluated as antiplasmodial agents against Plasmodium falciparum. The atovaquone analogues were found to be inactive as antagonists of parasite growth, which was attributed to ionization of the acidic hydroxyl moiety. Upon modification to an alkoxy substituent, the antiplasmodial activity was restored in the sub-100 nM range. Optimal inhibitors were found to possess IC50 values of 17.4-49.5 nM against heteroresistant P. falciparum W2.
- Lu, Xiao,Altharawi, Ali,Gut, Jiri,Rosenthal, Philip J.,Long, Timothy E.
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supporting information
p. 1029 - 1033
(2013/02/22)
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- Heterocyclyl linked anilines and benzaldehydes as precursors for biologically significant new chemical entities
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Benzylidene and benzyl thiazolidinediones, oxazolidinediones, isoxazolidinediones and their acyclic analogs like alpha alkylthio/alkoxy phenylpropanoic acids, beta-keto esters and tyrosine-based compounds possess broad therapeutic potential in general and as Peroxisome Proliferator Activated Receptors (PPARs) agonists in particular in the management of hyperglycemia and hyperlipidaemia for the treatment of Type 2 Diabetes (T2D). We have synthesised and characterized some novel and suitably substituted heterocyclyl linked benzaldehydes and anilines, which can be easily and very readily derivatized to all the above mentioned classes to generate new chemical entities of broader biological significance. Synthesis of their benzylidene thiazolidinedione and diethyl malonate and also benzyl diethyl malonate and alpha-bromoesters derivatives is reported in some of the cases in the present work. Indian Academy of Sciences.
- Verma, Raman K.,Kumar, Vijay,Ghosh, Prithwish,Wadhwa, Lalit K.
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p. 1063 - 1069
(2013/03/13)
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- Novel and highly potent histamine H3 receptor ligands. Part 1: Withdrawing of hERG activity
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Pre-clinical investigation of some aryl-piperidinyl ether histamine H3 receptor antagonists revealed a strong hERG binding. To overcome this issue, we have developed a QSAR model specially dedicated to H3 receptor ligands. This model was designed to be di
- Levoin, Nicolas,Labeeuw, Olivier,Calmels, Thierry,Poupardin-Olivier, Olivia,Berrebi-Bertrand, Isabelle,Lecomte, Jeanne-Marie,Schwartz, Jean-Charles,Capet, Marc
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scheme or table
p. 5378 - 5383
(2011/10/12)
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- NOVEL AZA-PEPTIDES CONTAINING 2,2-DISUBSTITUTED CYCLOBUTYL AND/OR SUBSTITUTED ALKOXY BENZYL DERIVATIVES AS ANTIVIRALS
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The present invention relates to novel aza-peptides containing 2,2-disubstituted 5 cyclobutyl and/or substituted alkoxy benzyl derivatives of formula (I) and compositions for inhibiting Human Immunodeficiency Virus (HIV) and process for making the compounds.
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Page/Page column 49-50
(2011/07/30)
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- Porphyrins containing nitric oxide donors: Synthesis and cancer cell-oriented NO release
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Four novel porphyrins containing nitric oxide (NO) donors were synthesized, and the structures of all the products were characterized by IR, UV-vis, 1H NMR, and elementary analysis. Interestingly, these new compounds not only were able to relea
- Liu, Wukun,Liu, Chaozhou,Gong, Changjun,Lin, Weiying,Guo, Cancheng
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scheme or table
p. 1647 - 1649
(2009/11/30)
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- NEW CHEMICAL COMPOUNDS
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The present invention provides compounds of formula (I) having muscarinic M3 receptor and β-adrenergic receptor modulating activity; processes for their preparation and their use in therapy; wherein A, R1, R2, R3 and Rsup
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(2008/12/08)
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- New PPARγ ligands based on barbituric acid: Virtual screening, synthesis and receptor binding studies
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A new series of PPARγ ligands based on barbituric acid (BA) has been designed employing virtual screening and molecular docking approach. To validate the computational approach, designed molecules were synthesized and evaluated in in vitro radioligand bin
- Sundriyal, Sandeep,Viswanad, Bhoomi,Ramarao, Poduri,Chakraborti, Asit K.,Bharatam, Prasad V.
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scheme or table
p. 4959 - 4962
(2009/05/30)
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- PROCESS FOR THE PREPARATION OF PORPHYRIN DERIVATIVES AS ANTIMICROBIAL AGENTS BY PHOTODYNAMIC THERAPY (PDT)
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There is provided a process for the preparation of 5,15-bis-[4-(3- trrmethylarnmonio-propyloxy)-phenyl]-porphyrin dihalide, wherein the process comprises step (a) of providing 4-(3-bromopropyloxy)benzaldehyde, step (b) of providing dipyrrolmethane, step (c) of reacting the 4-(3-bromopropyloxy)- benzaldehyde with the dipyrrol-methane, together with trifluoro acetic acid, in the presence of an oxidation reagent to produce 5,15-bis-[4-(3-bromo- propyloxy)-phenyl] -porphyrin which is purified by Soxhlet extraction from the adsorbed state on a bed of alumina under highly controlled conditions; and step (d) of reacting the 5,15-bis-[4-(3-bromo-propyloxy)-phenyl]-porphyrin with trimethylamine in the presence of dry dimethylformamide to produce 5,15-bis- [4-(3-trrmethylarnmonio-propyl-oxy)-phenyl] -porphyrin dibromide. In a preferred embodiment, the process further comprises step (e) of passing the 5, 15-bis-[4-(3 -1rimemylammonio-propyloxy)-phenyl]-porphyrin di-bromide produced in step (d) through an anion exchanger to produce 5,15-bis-[4-(3- trimethylammonio-propyloxy)-phenyl]-porphyrin dichloride. There is provided a process for the preparation of 5,15-bis-(4-{3-[(3-dimemylamino-propyl)- dimethyl-ammonio]-propyloxy} -phenyl] -porphyrin dihalide.
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Page/Page column title page; 18-20; Sheet 1/2
(2008/06/13)
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- Design and synthesis of 6-methyl-2-oxo-1,2,3,4-tetrahydro-pyrimidine-5-carboxylic acid derivatives as PPARγ activators
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The design and synthesis of novel series of 6-methyl-2-oxo-1,2,3,4-tetrahydro-pyrimidine-5-carboxylic acid (pyrimidone) derivatives that are high affinity ligands for peroxisome proliferators activated receptor γ have been reported as a potential substitu
- Kumar, Rakesh,Mittal, Amit,Ramachandran, Uma
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p. 4613 - 4618
(2008/03/11)
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- New mustard-linked 2-aryl-bis-benzimidazoles with anti-proliferative activity
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We describe new methodology for the synthesis of symmetric bis-benzimidazoles carrying 2-aryl moieties, including 2-[4-(3′- aminopropoxy)phenyl] and 2-[4-(3′-aminopropanamido)phenyl] substituents, together with the synthesis of novel hybrid molecules comprising bis-benzimidazoles in ester and amide combination with the N-mustard chlorambucil. The in vitro activities of these compounds against five cancer cell lines are also provided. The Royal Society of Chemistry 2006.
- Le Sann, Christine,Baron, Anne,Mann, John,Van Den Berg, Hendrik,Gunaratnam, Mekala,Neidle, Stephen
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p. 1305 - 1312
(2007/10/03)
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- One-dimensional energy/electron transfer through a helical channel
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We have synthesized A-D-A-type linear chain chromophores based on oligo(phenylene vinylene) as an electron donor (D) and several electron/energy acceptors (A), which are linked by an alkyl spacer with various lengths and are processed for a helical encaps
- Kim, Oh-Kil,Je, Jongtae,Melinger, Joseph S.
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p. 4532 - 4533
(2007/10/03)
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- Design, synthesis, and evaluation of 2-alkoxydihydrocinnamates as PPAR agonists
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A series of 2-alkoxydihydrocinnamates were synthesized as PPARγ and PPARα dual agonists. In vitro studies in cell model showed that these compounds were efficacious. Compound 1g was found to be a potent PPARα/γ dual agonist and will be further evaluated for the treatment of type II diabetes.
- Lu, Ying,Guo, Zongru,Guo, Yanshen,Feng, Jun,Chu, Fengming
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p. 915 - 919
(2007/10/03)
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- Synthesis and evaluation of azaindole-α-alkyloxyphenylpropionic acid analogues as PPARα/γ agonists
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A series of azaindole-α-alkyloxyphenylpropionic acid analogues was synthesized and evaluated for PPAR agonist activities. Structure-activity relationship was developed for PPARα/γ dual agonism. One of the synthesized compound 7a was identified as a potent
- Cai, Zhefeng,Feng, Jun,Guo, Yanshen,Li, Pingping,Shen, Zhufang,Chu, Fengming,Guo, Zongru
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p. 866 - 874
(2007/10/03)
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- Substituted aryloximes
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The present invention relates to substituted aryl oximes and methods of using them.
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Page/Page column 17
(2010/02/11)
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- Synthesis and photophysical properties of porphyrins containing viologen units for ultrafast molecular photonics
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Several 5,15-diarylporphyrin derivatives containing viologen units as an electron acceptor for ultrafast intramolecular electron transfer have been synthesized. The fluorescence of the porphyrin-viologen linked systems was appreciably quenched by the attached viologens. In accordance with this, the formation of a charge-separated state was observed upon excitation with a femtosecond (fs) laser at 400 nm. The rate of electron transfer and back transfer was controlled by the different length of alkyl chain spacers between porphyrin and viologen. Attempts to use these porphyrin molecules as a thin film component of ultrafast parallel data processing by guided wave mode geometry were limited by gradual deterioration upon repeated fs laser excitation.
- Laudien, Robert,Yoshida, Iori,Nagamura, Toshihiko
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p. 1772 - 1777
(2007/10/03)
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- 1,2-dithiolane derivatives
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This invention provides new thiazolindinedione derivatives and new arylacetic acid derivatives. These compounds are useful for the treatment of cardiovascular diseases, certain endocrine diseases, certain inflammatory diseases, certain neoplastic (maligna
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Page column 22
(2010/11/29)
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- Aminoisoquinolines and aminotheinopyridine derivatives and their use as anti-inflammatory agents
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PCT No. PCT/SE97/00589 Sec. 371 Date Aug. 19, 1997 Sec. 102(e) Date Aug. 19, 1997 PCT Filed Apr. 9, 1997 PCT Pub. No. WO97/38977 PCT Pub. Date Oct. 23, 1997Compounds of formula I wherein R, R1, R2, and R3 and A are as defined herein, together with pharmaceutically acceptable salts, enantiomers or tautomers are useful as pharmaceuticals, particularly in the treatment of inflammatory disease.
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- Radical isomerization via intramolecular ipso substitution of aryl ethers: Aryl translocation from oxygen to carbon
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Bromopropyl aryl ethers an converted to 3-arylpropanols under standard radical generating conditions in the presence of tributylstannane and AIBN. This rearrangement involves intramolecular ipso attack of the alkyl radicals which generates spiro cyclohexadienyl radical intermediates.
- Lee, Eun,Lee, Chulbom,Tae, Jin Sung,Whang, Ho Sung,Li, Kap Sok
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p. 2343 - 2346
(2007/10/02)
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