- Synthesis, structures, and one/two-photon excited fluorescence of two new Ca(II)-coordinated polymers with D-π-A ligand
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Two alkaline-earth metal coordination polymers, [Ca(TAPIP)2(H2O)3]·2H2O (1) and [Ca(TAPIP)2(H2O)3]·5H2O (2), have been synthesized under hydrothermal reactions with th
- Xu, Wei,Li, Lin-Shen,Zhong, Ri-Ming,Cai, Dan-Ju,Zhan, Qiu-Qiang,Lin, Wei-Quan,Zhang, Ze-Min,Wu, Jian-Zhong,Ou, Yong-Cong
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Read Online
- Attaching azoles to Hantzsch 1,4-dihydropyridines: Synthesis, theoretical investigation of nonlinear optical properties, antimicrobial evaluation and molecular docking studies
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In the present study, we designed three novel compounds via the combination of two precious nitrogen-containing scaffolds; 1,4-dihydropyridine (DHP) and azole, in the same molecule. To synthesize the title compounds, initially, azolyl benzaldehydes were o
- Dengiz, Cagatay,Gündüz, Miyase G?zde,Ko?ak Aslan, Ebru,Nikodinovic-Runic, Jasmina,Skaro Bogojevic, Sanja
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- Two novel colorimetric fluorescent probes: Hg2+ and Al3+ in the visual colorimetric recognition environment
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Two new dual channel Schiff base fluorescent probes, Tri-R6G and Tri-Flu, were synthesized, and can detect Hg2+ and Al3+, respectively. The two probes were characterized by FTIR, 1H NMR, 13C NMR and HRMS, and their optical properties were detected by UV and FL. Test results showed the probes' detection of Hg2+ and Al3+ compared to other metal ions (Ag+, Co2+, Cd2+, Mg2+, Cu2+, Ni2+, Ba2+, Pb2+, Cr3+, Al3+, Zn2+, Hg2+, K+, Ga2+ and Fe3+), respectively. Besides, the detection limits were determined to be 1.61 × 10-8 M and 1.15 × 10-8 M through the standard curve plot, respectively. The photoelectron transfer (PET) mechanism was guessed by the Job's plot and the infrared titration. Corresponding orbital electron distribution and molecular geometry configurations of the compounds were predicted by density functional theory (DFT). In addition, the prepared test paper changed from white to pink when the target ion was detected. The color changed from colorless to pink in a solution having a concentration of 10-5 M.
- Duan, Hongdong,Fang, Shimin,Qin, Dawei,Wang, Lizhen,Yang, Geng,Zhong, Wenxia,Zhou, Jianhua
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p. 3048 - 3059
(2020/02/04)
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- PYRROLIDINE GLYCOSIDASE INHIBITORS
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Compounds of formula (I) wherein A, W, R3b, Z and p have the meaning according to the claims can be employed, inter alia, for the treatment of tauopathies and Alzheimer's disease.
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Page/Page column 150
(2020/03/15)
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- A triazolyl quinoline copper complex having an AIE property and a preparing method thereof
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A triazolyl quinoline copper complex having an AIE property and a preparing method thereof are disclosed, belonging to the technical field of metal organic complexes. The triazolyl-containing 2-substituted-8-hydroxyquinoline copper complex is synthesized,
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Paragraph 0023; 0040; 0041; 0042
(2019/01/24)
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- A triazole benzaldehyde compression fluorescein in [...] and its preparation method
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This application pertains to the field of fluorescent probe, in particular relates to a triazole benzaldehyde compression fluorescein in [...] and its preparation method. The probe is "turn - on" type fluorescent probe, the probe utilizes the photo ions electron transfer mechanism in the presence of fluorescent switch is opened, to form a new compound, ultraviolet absorption occurs red shift, fluorescence generating red-shifting and significantly enhanced fluorescent probe, and the fluorescent probe has a good selectivity, anti-metal ion interference capacity is strong, fast response, has the purpose of a simple, rapid, sensitive mercury ion specific detection reagent, can be applied to the material areas or the sensor field.
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Paragraph 0032-0053
(2019/07/11)
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- Triazolyl benzaldehyde rhodamine hydrazine hydrate Schiff base and preparation method thereof
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The invention belongs to the field of fluorescence probes and particularly relates to triazolyl benzaldehyde rhodamine hydrazine hydrate Schiff base and a preparation method thereof. The fluorescenceprobe turns on a fluorescence switch in the absence of mercury ions by use of a light-induced electron transfer mechanism, a novel compound is formed, besides, the significantly reinforced fluorescence probe with red shift of ultraviolet absorption and fluorescence has good selectivity, high metal ion interference resistance and rapid response, is a purposeful simple, rapid and sensitive mercury ion specific detection reagent and can be applied to the material or sensor field.
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Page/Page column 5-7
(2019/06/07)
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- Design and Synthesis of 2-Substitutedphenyl Benzo[D]Thiazole Derivatives and Their β-Amyloid Aggregation and Cholinesterase Inhibitory Activities
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The occurrence of amyloid-β (Aβ) and reduced cholinergic tranmission are two major hallmarks of Alzheimer’s disease (AD). Therefore, a series of new 2-phenylbenzo[d]thiazoles substituted with azole/piperazine moieties were designed, synthesized, and evaluated as potential dual inhibitors of Aβ aggregation and cholinesterase (ChE) activities. In vitro studies showed that compound 2m containing an imidazole ring strongly inhibited Aβ1–40 (49.2%) and Aβ1-42 aggregation (60.6%). All derivatives exhibited weak inhibitory activities against both acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). Therefore, compound 2m may represent promising therapeutic option for inhibiting Aβ-mediated pathology in AD.
- Zengin, Merve,Unsal-Tan, Oya,Kü?ükk?l?n?, Tuba Tüylü,Ayazgok, Beyza,Balkan, Ayla
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p. 322 - 328
(2019/07/29)
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- Luminescent sensing of Fe3+ and K+ by three novel imidazole dicarboxylate-based MOFs
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In this paper, three luminescent metal–organic frameworks, namely: [Zn(p-IPhHIDC)]n (1), {[Cd(p-IPhIDC)(H2O)]·CH3OH}n (2) and [Zn(p-TIPhHIDC)]n (3), bearing two novel substituted imidazole dicarboxyla
- Huang, Qiuying,Wang, Jifeng,Wang, Qi,Li, Gang
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p. 193 - 204
(2017/01/10)
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- Novel 2-Arylbenzimidazole derivatives as multi-targeting agents to treat Alzheimer’s disease
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This study describes the synthesis, pharmacological evaluation, including acetylcholinesterase (AChE)/butyrylcholinesterase (BChE) inhibition, amyloid beta (Aβ) antiaggregation, and neuroprotective effects, as well as molecular modeling of novel 2-(4-subs
- Unsal-Tan, Oya,Ozadali-Sari, Keriman,Ayazgok, Beyza,Kü?ükk?l?n?, Tuba Tüylü,Balkan, Ayla
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p. 1506 - 1515
(2017/06/05)
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- Synthesis of new hydrazone derivatives for MAO enzymes inhibitory activity
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In the present work, 14 new 1-substituted-2-phenylhydrazone derivatives were synthesized to evaluate their inhibitory activity against hMAO enzymes. The structures of the newly synthesized hydrazones 2a–2n were characterized by IR,1H-NMR,1
- Can, Nafiz ?ncü,Can, Nafiz nc,Osmaniye, Derya,Levent, Serkan,Sa Sa?lik, Begüm Nurpelin,Inci, Beril,Ilgin, Sinem,?zkay, Yusuf,Kaplancikli, Zafer Asim
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- Triazolyl benzaldehyde p-phenylenediamine bis-Schiff bases and preparation method thereof
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The invention relates to triazolyl benzaldehyde p-phenylenediamine bis-Schiff bases and a preparation method thereof. The method comprises the following steps: preparing 4-(1-1,2,4-triazolyl)benzaldehydes or triazole derivative benzaldehydes from 1,2,4-tr
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Paragraph 0032; 0033
(2018/02/03)
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- A three-nitrogen zuozuo benzenethe formaldehyde shrinks phenylenediamine double-Schiff base and its preparation method
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The invention relates to a condensed triazole benzaldehyde p-phenylenediamine bis-Schiff base and a preparation method thereof. The preparation method comprises the following steps of firstly preparing 1,2,4-triazole or triazole derivatives and p-fluorobe
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Paragraph 0033
(2017/08/25)
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- Pesticidal compositions and processes related thereto
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This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.
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Page/Page column 132-133
(2016/01/09)
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- METHYLENE LINKED QUINOLINYL MODULATORS OF RORyt
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The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating RORγt activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.
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Paragraph 0567; 0568
(2015/04/21)
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- METHYLENE LINKED QUINOLINYL MODULATORS OF ROR-GAMMA-T
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The present invention comprises compounds of Formula (I). wherein: R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating RORγt activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.
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Page/Page column 158
(2015/05/05)
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- PESTICIDAL COMPOSITIONS AND PROCESSES RELATED THERETO
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This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.
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Page/Page column
(2014/06/25)
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- PESTICIDAL COMPOSITIONS AND PROCESSES RELATED THERETO
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This document discloses molecules having the following formula ("Formula One"): and processes associated therewith.
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Page/Page column 131
(2014/07/08)
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- PESTICIDAL COMPOSITIONS AND PROCESSES RELATED THERETO
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This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.
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Paragraph 0656-0657
(2014/06/25)
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- PESTICIDAL COMPOSITIONS AND PROCESSES RELATED THERETO
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This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.
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Paragraph 0821; 0822
(2014/06/25)
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- Synthesis and crystal structure of charge separate manganese complex
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A novel complex Mn(taba)2?4H2O [Htaba = 4-(1H-1,2,4-triazol-1-yl) benzoic acid] containing carboxylate-triazole ligands has been synthesized and characterized by elemental analyses, IR and X-ray single crystal diffraction. The crystal of the complex belon
- Gan, Xiaoping,Chu, Mingjie,Yao, Jianguo,Geng, Wenqian,Zhang, Xiuli,Tian, Yupeng,Zhou, Hongping
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p. 257 - 260
(2014/03/21)
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- METHYLENE LINKED QUINOLINYL MODULATORS OF RORyt
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The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating RORγt activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.
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Paragraph 0593; 0594
(2014/05/07)
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- Synthesis and antimycobacterial activities of some new thiazolylhydrazone derivatives
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This Letter reports the synthesis and evaluation of some thiazolylhydrazone derivatives for their in vitro antimycobacterial activities against Mycobacterium tuberculosis H37Rv. The cytotoxic activities of all compounds were also evaluated. The compounds
- Ozadali, Keriman,Unsal Tan, Oya,Yogeeswari, Perumal,Dharmarajan, Sriram,Balkan, Ayla
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p. 1695 - 1697
(2014/04/17)
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- Substituent group variations directing the molecular packing, electronic structure, and aggregation-induced emission property of isophorone derivatives
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A series of new isophorone derivatives (1-5), incorporating the heterocyclic ring or aza-crown-ether group, with large Stokes shifts (>140 nm), have been synthesized and characterized. 1-4 display aggregation-induced emission behaviors, while dye 5 is highly emissive in solution but quenched in the solid state. It was found that the tuning of emission color of the isophorone-based compounds in the solid state could be conveniently accomplished by changing the terminal substituent group. The photophysical properties in solution, aqueous suspension, and crystalline state, along with their relationships, are comparatively investigated. Crystallographic data of 1-4 indicate that the existence of multiple intermolecular hydrogen bonding interactions between the adjacent molecules restricts the intramolecular vibration and rotation and enables compounds 1-4 to emit intensely in the solid state. The size and growth processes of particles with different water fractions were studied using a scanning electron microscope, indicating that smaller globular nanoparticles in aqueous suspension are in favor of fluorescence emissions. The above results suggest that substituent groups have a great influence on their molecular packing, electronic structure, and aggregation-induced emission properties. In addition, fluorescence cell imaging experiment proved the potential application of 5.
- Zheng, Zheng,Yu, Zhipeng,Yang, Mingdi,Jin, Feng,Zhang, Qiong,Zhou, Hongping,Wu, Jieying,Tian, Yupeng
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p. 3222 - 3234
(2013/06/27)
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- PESTICIDAL COMPOSITIONS AND PROCESSES RELATED THERETO
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This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.
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Page/Page column 72
(2013/02/28)
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- Noncentrosymmetric organic solid and its zinc coordination polymer with diamonded network prepared from an ionothermal reaction: Syntheses, crystal structures, and second-order nonlinear optics properties
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An organic ligand 4-(1,2,4-triazol-1-yl) benzoic acid (Htzbc) with a nonlinear optical (NLO) chromophore has been synthesized. Reaction of Zn(NO 3)2 with Htzbc ligand in 1-n-butyl-3-methylimidazolium tetrafluoroborate ionic liquid af
- Wang, Yu-Ling,Fu, Jiang-Hong,Wei, Jia-Jia,Xu, Xiang,Li, Xin-Fa,Liu, Qing-Yan
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p. 4663 - 4668
(2012/11/13)
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- Novel aryloxy azolyl chalcones with potent activity against Mycobacterium tuberculosis H37Rv
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A series of twenty seven novel aryloxy azolyl chalcones were synthesized and evaluated in vitro for the growth inhibition of Mycobacterium tuberculosis H37Rv. Ten compounds from this series exhibited good activity with MIC in the range of 3.12-0.78 μg/mL
- Marrapu, Vijay K.,Chaturvedi, Vinita,Singh, Shubhra,Singh, Shyam,Sinha, Sudhir,Bhandari, Kalpana
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experimental part
p. 4302 - 4310
(2011/11/13)
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- SAR study of clubbed [1,2,4]-triazolyl with fluorobenzimidazoles as antimicrobial and antituberculosis agents
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In the present study, a series of novel 2-[4-(1H-[1,2,4]-triazol-1-yl)phenyl]-1-substituted-4,6-difluoro-1H-benz o[d]imidazole derivatives are synthesized by the alkylation of 2-[4-(1H-[1,2,4]-triazol-1-yl)phenyl]-4,6-difluoro-1H-benzo[d]imidazole with substituted alkyl and aryl halides. The compounds were evaluated for their preliminary in-vitro antibacterial activity against Pseudomonas aeruginosa, Escherichia coli, Staphylococcus aureus, and Salmonella typhosa and then were screened for their antitubercular activity against Mycobacterium tuberculosis H37Rv strain by broth microdilution assay method. The antibacterial data suggested that the analogs with electronegative substituents emerged as promising antimicrobials. It was also observed that the promising antimicrobials have proved to be better antimycobacterials. Few of selected analogs are under further evaluation for secondary antitubercular screening, as they have shown better activity compared to rifampin.
- Jadhav, Ganesh Rajaram,Shaikh, Mohammad Usman,Kale, Rajesh Prabhakar,Shiradkar, Mahendra Ramesh,Gill, Charansingh Harnamsingh
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experimental part
p. 2930 - 2935
(2009/10/02)
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- INSECTICIDAL ISOXAZOLINES
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Novel isoxazolines of the formula (I) wherein A represents C or N; R represents haloalkyl; X represents halogen or haloalkyl; 1 represents 0, 1 or 2; Y represents halogen, alkyl, alkoxy, haloalkyl, cyano, nitro, amino, acylamino, alkoxycarbonylamino, halo
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Page/Page column 55; 65
(2008/06/13)
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- Arylsulfonamido-substituted hydroxamic acid derivatives
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α-Amino hydroxamic acid derivative of formula (I), in which R is C2–C7-alkyl, which is mono-, di- or trisubstituted by halogen, nitro, lower acyloxy, trifluoromethoxy, cyano, C3–C5-cycloalkyl or unsubstituted or substituted C3–C4-heteroaryl comprising one or two heteroatoms selected from the group consisting of O, S and N; or C3–C7-alkenyl or C3–C7-alkynyl, which in each case is unsubstituted or mono-, di- or trisubstituted by halogen, nitro, lower acyloxy, trifluoromethoxy, cyano, C3–C5-cycloalkyl or unsubstituted or substituted C3–C6-heteroaryl comprising one or two heteroatoms selected from the group consisting of O, S and N; and the other symbols are as defined in claim 1, are described. These compounds are MMP and in particular MMP2 inhibitors and can be used for treatment of MMP dependent diseases, in particular inflammation conditions, rheumatoid arthritis, osteoarthritis, tumors (tumor growth, metastasis, progression or invasi n) and pulmonary disorders (e.g. emphysema, COPD).
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Page/Page column 44
(2008/06/13)
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- NOVEL FLORFENICOL-TYPE ANTIBIOTICS
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The present invention relates to novel florfenicol compounds having the chemical structure: wherein the compounds are useful for the treatment and/or prevention of bacterial infections in a broad range of patients such as, without limitation, birds, fish, shellfish and mammals
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- Anilinopeptide derivatives
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The invention relates to compounds of the formula I, in which R1and R2are, independently of each other, lower alkyl or lower alkoxy-lower alkyl; R3and R4are, independently of each other, sec-lower alkyl or tert-
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- Ultrasound effect on the synthesis of 4-alkyl-(aryl)aminobenzaldehydes
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The sonochemical nucleophilic aromatic substitutions on 4-fluorobenzaldehyde with different azacycloalkanes and azoles have been studied. A beneficial ultrasound effect was observed, reactions were clean and high yields of the products were isolated after 15 min sonication.
- Magdolen, Peter,Me?iarová, Mária,Toma, ?tefan
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p. 4781 - 4785
(2007/10/03)
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- N-AROYLAMINO ACID AMIDES AS ENDOTHELIN INHIBITORS
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The present invention relates to the compounds of formula (I) STR1 wherein R is carboxy, esterified carboxy, carbamoyl, N-(alkyl or aryl)-carbamoyl, cyano, 5-tetrazolyl or CONH--SO 2--R 4 ; R. sub.1 is hydrogen, lower alkyl, aryl-lower alkyl or cycloalkyl-lower alkyl; R 2 is hydrogen or lower alkyl, or R 1 and R 2 represent lower alkylene to form together with the carbon and nitrogen atoms to which they are attached an azacycloalkane ring; R 3 is heterocyclic or carbocyclic (aryl or biaryl)-lower alkyl; Y is lower alkylidenyl, 3-to 10-membered cycloalkylidenyl which may be substituted by oxo, alkylenedioxy, hydroxy, acyloxy, lower alkoxy; or Y is 5-to 10-membered cycloalkylidenyl fused to a saturated or unsaturated carbocyclic 5-or 6-membered ring; or Y is 5-to 8-membered oxacycloalkylidenyl, 5-to 8-membered (thia-, oxothia-or dioxothia-) cycloalkylidenyl, or 5-to 8-membered azacycloalkylidenyl optionally N-substituted by lower alkyl or aryl-lower alkyl; R 4 represents hydrogen, lower alkyl, carbocyclic aryl, heterocyclic aryl, cycloalkyl, (carbocyclic aryl, heterocyclic aryl, cycloalkyl, hydroxy, acyloxy, or lower alkoxy)-lower alkyl, lower alkyl substituted by carboxyl, by esterified carboxyl or by amidated carboxyl; Ar represents carbocyclic or heterocyclic aryl; and pharmaceutically acceptable salts thereof; which are useful as endothelin inhibitors in mammals.
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- Inhibitors of acyl-coA:cholesterol O-acyltransferase. 2. Identification and structure-activity relationships of a novel series of N-alkyl-N- (heteroaryl-substituted benzyl)-N'-arylureas
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A series of N-alkyl-N-(heteroaryl-substituted benzyl)-N'-arylurea and related derivatives represented by 2 and 3 have been prepared and evaluated for their ability to inhibit acyl-CoA:cholesterol O-acyltransferase in vitro and to lower plasma cholesterol levels in cholesterol-fed rats in vivo. Among these novel compounds, the type 3 series was superior. A pyrazol-3-yl group on the N-benzyl group of this trisubstituted urea (i.e. 3, Ar1 = pyrazol-3- yl) was identified as a heteroaromatic ring providing a good profile of biological activity. As a result of optimization of the combination with the N-alkyl group (R) and N-aryl group (At3), compound 3aq (FR186054) was identified as a new, orally efficacious ACAT inhibitor, which exhibited potent in vitro ACAT inhibitory activity (rabbit intestinal microsomes IC50 = 99 nM) and excellent hypocholesterolemic effects in cholesterol-fed rats, irrespective of administration mode (ED50 = 0.046 mg/kg dosed via the diet, ED50 = 0.44 mg/kg administered by gavage in PEG400 vehicle). Moreover, a toxicological study revealed compound 3aq to be nontoxic to the adrenal glands of dogs when tested at a single dose of 10 mg/kg po.
- Tanaka, Akira,Terasawa, Takeshi,Hagihara, Hiroyuki,Sakuma, Yuri,Ishibe, Noriko,Sawada, Masae,Takasugi, Hisashi,Tanaka, Hirokazu
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p. 2390 - 2410
(2007/10/03)
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- Antagonists of endothelin receptors
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The present invention provides novel compounds having pharmacological properties represented by the general formula I STR1 processes for the manufacture, pharmaceutical compositions and the use of the compounds of formula I and salts thereof.
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- Aromatic hydrazides as specific inhibitors of bovine serum amine oxidase
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New hydrazides were synthesized in search for specific inhibitors of bovine serum amine oxidase: a series of benzoic and phenylacetic acid hydrazides containing the 1H-imidazol-1-yl or the 1H-imidazol-1-ylmethyl group as (o,m,p)-substituent in the phenyl ring; an analogous series of p-substituted phenylhydrazides with 5 or 6-membered heterocyclic ring as substituent, and a series of similar phenylpropionic hydrazides. The longer and more flexible phenylacetic hydrazides, and to a somewhat lesser extent the phenylpropionic ones, were better specific inhibitors of bovine serum amine oxidase than the benzoic hydrazides, which were also bound by the enzyme with high affinity, but at a slow rate. Derivatives with p- and m-substituents were more reactive than the o-substituted ones. The chemical nature of the substituent was less important than its position in the phenyl ring and the presence of methylene spacers. These data point to the presence of a hydrophobic site at short distance from the protein carbonyl cofactor, so that simultaneous interaction of the 2 ends of the inhibitor molecule can occur at the 2 sites. The presence of the hydrophobic site was confirmed by the capability of some molecule deprived of the hydrazidic group to act as mild inhibitors. All hydrazides were less reactive by 2-3 orders of magnitude towards pig kidney diamine oxidase and FAD-dependent monoamine oxidase from rat brain mitochondria, while the other compounds showed similar inhibition power against all proteins. The specificity for the bovine enzyme seems therefore to be related to the concerted action of the 2 moieties of the inhibitor molecule.
- Artico,Silvestri,Stefancich,Avigliano,Di Giulio,Maccarrone,Agostinelli,Mondovi,Morpurgo
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p. 219 - 228
(2007/10/02)
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