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Efficient and recyclable bimetallic Co–Cu catalysts for selective hydrogenation of halogenated nitroarenes
Silica supported N-doped carbon layers encapsulating Co–Cu nanoparticles (Co1Cux@CN/SiO2) were prepared by a one-step impregnation of Co(NO3)2·6H2O, Cu(NO3)2·3H2O, urea and glucose, following in situ carbothermal reduction. Effects of Cu contents on the catalytic performance of the Co1Cux@CN/SiO2 catalysts were investigated for selective hydrogenation of p-chloronitrobenzene to p-chloroaniline. The Co1Cu0.30@CN/SiO2 with Cu/Co molar ratio of 0.30:1 presented much higher activity and stability than the monometallic Co@CN/SiO2 catalyst. The addition of Cu into Co1Cux@CN/SiO2 catalysts had favorable effects on the formation of highly active Co–N sites and N-doped carbon layer. The role of the N-doped carbon layer was to protect the Co from oxidation by air, and the Co1Cu0.30@CN/SiO2 could be reused for at least 12 cycles without decrease in catalytic efficiency. Mechanistic and in situ infrared studies revealed that the interaction effect between the Co and Cu atoms made the surface of Co highly electron rich, which decreased adsorption of halogen groups and resulting in the enhanced selectivity during chemoselective hydrogenation of halogenated nitroarenes for a wide scope of substrates.
Lu, Xionggang,Ren, Jiaan,Sheng, Yao,Wang, Xueguang,Wu, Baoqin,Zou, Xiujing
(2021/12/20)

Tunable Electrosynthesis of Anthranilic Acid Derivatives via a C-C Bond Cleavage of Isatins
A facile and direct electrocatalytic C-C bond cleavage/functionalization reaction of isatins was developed. With isatins as the amino-attached C1 sources, a variety of aminobenzoates, and aminobenzamides were synthesized in moderate to good yields under mild conditions.
Qian, Peng,Liu, Jiaojiao,Zhang, Yan,Wang, Zhiyong
p. 16008 - 16015
(2021/07/31)

Synthesis and nematicidal activities of 1,2,3-benzotriazin-4-one containing 4,5-dihydrothiazole-2-thiol derivatives against Meloidogyne incognita
A series of novel 1,2,3-benzotriazin-4-one derivatives containing 4,5-dihydrothiazole-2-thiol were synthesized and characterized by 1H NMR, 13C NMR, 19F NMR and HRMS. The bioassay results showed that compounds 3-(3-((4,5-dihydrothiazol-2-yl)thio)propyl)-7-methoxybenzo[d][1–3]triazin-4(3H)-one, 3-(3-((4,5-dihydrothiazol-2-yl)thio)propyl)-6-nitrobenzo[d][1–3]triazin-4(3H)-one, 7-chloro-3-(3-((4,5-dihydrothiazol-2-yl)thio)propyl)benzo[d][1–3]triazin-4(3H)-one exhibited good control efficacy against the cucumber root-knot nematode disease caused by Meloidogyne incognita at the concentration of 10.0 mg L?1 in vivo. Compound 7-chloro-3-(3-((4,5-dihydrothiazol-2-yl)thio)propyl)benzo[d][1–3]triazin-4(3H)-one showed excellent nematicidal activity with inhibition 68.3% at a concentration of 1.0 mg L?1. It suggested that the structure of 1,2,3-benzotriazin-4-one containing 4,5-dihydro-thiazole-2-thiol could be optimized further.
Chen, Xiulei,Zhou, Zhen,Li, Zhong,Xu, Xiaoyong
p. 194 - 200
(2019/09/13)

Quinazoline derivative as well as preparation method and application thereof (by machine translation)
The invention belongs to the technical field of medicines, and relates to a quinazoline derivative and a preparation method and application. thereof, and provides a compound as shown in general formula (I) and geometric isomers or pharmaceutically acceptable salts, hydrate, solvates thereof and preparation method. thereof.R1 , R2 , R3 , R4 , R5 The compound of . which rapidly releases the prototype drug, prototype drug under the action of an in vivo hydrolase, has a protein kinase inhibitory activity, that has an inhibitory effect PAKs on each member, kinase family and can be used to prepare PAK protein kinase inhibitor. (by machine translation)
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Paragraph 0083-0085

(2020/05/14)

Synthesis and nematicidal evaluation of 1,2,3-benzotriazin-4-one derivatives containing piperazine as linker against Meloidogyne incognita
To explore new skeleton with nematicidal activity, a series of novel 1,2,3-benzotriazin-4-one derivatives containing piperazine as linker were synthesized and varied fragments were also introduced to increase structure diversity of the new skeleton. Their inhibitory activities in vivo were evaluated against Meloidogyne incognita. The newly prepared compounds A6, A8, A21, A28 and A38 exhibited more than 50% inhibition at the concentration of 20 mg/L. Especially compound A6 displayed 71.4% inhibition against Meloidogyne incognita at the concentration of 20 mg/L. The nematicidal activities varied significantly depending on the types and positions of the substituents, which provided guidance for further structure modification.
Chen, Xiulei,Jia, Haowu,Li, Zhong,Xu, Xiaoyong
supporting information
p. 1207 - 1213
(2019/03/29)

Oxidative ring-opening of isatins for the synthesis of 2-aminobenzamides and 2-aminobenzoates
An efficient and practical isatin-based oxidative domino protocol has been developed for the facile synthesis of 2-aminobenzamides and 2-aminobenzoates. The robust nature of this reaction system is reflected by accessible starting materials, room temperature and high-yield gram-scale synthesis.
Wang, Yu-Wei,Zheng, Lei,Jia, Feng-Cheng,Chen, Yun-Feng,Wu, An-Xin
p. 1497 - 1503
(2019/02/13)

Structure-Based Design of 6-Chloro-4-aminoquinazoline-2-carboxamide Derivatives as Potent and Selective p21-Activated Kinase 4 (PAK4) Inhibitors
Herein, we report the discovery and characterization of a novel class of PAK4 inhibitors with a quinazoline scaffold. Based on the shape and chemical composition of the ATP-binding pocket of PAKs, we chose a 2,4-diaminoquinazoline series of inhibitors as a starting point. Guided by X-ray crystallography and a structure-based drug design (SBDD) approach, a series of novel 4-aminoquinazoline-2-carboxamide PAK4 inhibitors were designed and synthesized. The inhibitors' selectivity, therapeutic potency, and pharmaceutical properties were optimized. One of the best compounds, 31 (CZh226), showed remarkable PAK4 selectivity (346-fold vs PAK1) and favorable kinase selectivity profile. Moreover, this compound potently inhibited the migration and invasion of A549 tumor cells by regulating the PAK4-directed downstream signaling pathways in vitro. Taken together, these data support the further development of 31 as a lead compound for PAK4-targeted anticancer drug discovery and as a valuable research probe for the further biological investigation of group II PAKs.
Hao, Chenzhou,Zhao, Fan,Song, Hongyan,Guo, Jing,Li, Xiaodong,Jiang, Xiaolin,Huan, Ran,Song, Shuai,Zhang, Qiaoling,Wang, Ruifeng,Wang, Kai,Pang, Yu,Liu, Tongchao,Lu, Tianqi,Huang, Wanxu,Wang, Jian,Lin, Bin,He, Zhonggui,Li, Haitao,Li, Feng,Zhao, Dongmei,Cheng, Maosheng
p. 265 - 285
(2018/02/10)

Design, synthesis and biological activities of 2,3-dihydroquinazolin-4(1H)-one derivatives as TRPM2 inhibitors
Transient receptor potential melastatin 2 (TRPM2), a Ca2+-permeable cationic channel, plays critical roles in insulin release, cytokine production, body temperature regulation and cell death as a reactive oxygen species (ROS) and temperature sensor. However, few TRPM2 inhibitors have been reported, especially TRP-subtype selective inhibitors, which hampers the investigation and validation of TRPM2 as a drug target. To discover novel TRPM2 inhibitors, 3D similarity-based virtual screening method was employed, by which 2,3-dihydroquinazolin-4(1H)-one derivative H1 was identified as a TRPM2 inhibitor. A series of novel 2,3-dihydroquinazolin-4(1H)-one derivatives were subsequently synthesized and characterized. Their inhibitory activities against the TRPM2 channel were evaluated by calcium imaging and electrophysiology approaches. Some of the compounds exhibited significant inhibitory activity, especially D9 which showed an IC50 of 3.7 μM against TRPM2 and did not affect the TRPM8 channel. The summarized structure-activity relationship (SAR) provides valuable insights for further development of specific TRPM2 targeted inhibitors.
Zhang, Han,Liu, Huan,Luo, Xiao,Wang, Yuxi,Liu, Yuan,Jin, Hongwei,Liu, Zhenming,Yang, Wei,Yu, Peilin,Zhang, Liangren,Zhang, Lihe
p. 235 - 252
(2018/05/09)

On the Synthesis and Reactivity of 2,3-Dihydropyrrolo[1,2- a ]quinazolin-5(1 H)-ones
An improved, scalable synthetic route to the quinazolinone natural product 2,3-dihydropyrrolo[1,2-a]quinazolin-5(1H)-one is reported. The applicability of this method to analogue synthesis and the synthesis of related natural products is explored. Finally, reactivity of the scaffold to a variety of electrophilic reagents, generating products stereoselectively, is reported.
Sutherell, Charlotte L.,Ley, Steven V.
supporting information
p. 135 - 144
(2016/12/24)

Anthranilamide-based 2-phenylcyclopropane-1-carboxamides, 1,1'-biphenyl-4-carboxamides and 1,1'-biphenyl-2-carboxamides: Synthesis biological evaluation and mechanism of action
Several anthranilamide-based 2-phenylcyclopropane-1-carboxamides 13a-f, 1,1’-biphenyl-4-carboxamides 14a-f and 1,1’-biphenyl-2-carboxamides 17a-f were obtained by a multistep procedure starting from the (1S,2S)-2-phenylcyclopropane-1-carbonyl chloride 11, the 1,1'-biphenyl-4-carbonyl chloride 12 or the 1,1'-biphenyl-2-carbonyl chloride 16 with the appropriate anthranilamide derivative 10a-f. Derivatives 13a-f, 14a-f and 17a-f showed antiproliferative activity against human leukemia K562?cells. Among these derivatives 13b, 14b and 17b exerted a particular cytotoxic effect on tumor cells. Derivative 17b showed a better antitumoral effect on K562?cells than 13b and 14b. Analyses performed to explore 17b mode of action revealed that it induced an arrest in G2/M phase of cell cycle which was consequent to DNA lesions as demonstrated by the increase in phospho-ATM and γH2AX, two known markers of DNA repair response system. The effect of 17b was also related to ROS generation, activation of JNK and induction of caspase-3 dependent apoptosis.
Raffa, Demetrio,Plescia, Fabiana,Maggio, Benedetta,Raimondi, Maria Valeria,D'Anneo, Antonella,Lauricella, Marianna,Daidone, Giuseppe
p. 262 - 273
(2017/04/03)

Design, Synthesis, and Potency of Pyruvate Dehydrogenase Complex E1 Inhibitors against Cyanobacteria
Safe and effective algaecides are needed to control agriculturally and environmentally significant algal species. Four series (6, 10, 17, and 21) of 29 novel 4-aminopyrimidine derivatives were rationally designed and synthesized. A part of 10, 17, and 21 displayed potent inhibition of Escherichia coli pyruvate dehydrogenase complex E1 (E. coli PDHc-E1) (IC50 = 2.12-18.06 μM) and good inhibition of Synechocystis sp. PCC 6803 (EC50 = 0.7-7.1 μM) and Microcystis sp. FACH 905 (EC50 = 3.7-7.6 μM). The algaecidal activity of these compounds positively correlated with their inhibition of E. coli PDHc-E1. In particular, 21l and 10b exhibited potent algaecidal activity against PCC 6803 (EC50 = 0.7 and 0.8 μM, respectively), values that were 2-fold increased compared to that of copper sulfate (EC50 = 1.8 μM), and showed the best inhibition of cyanobacterium PDHc-E1 (IC50 = 5.10 and 6.06 μM, respectively). 17h and 21e, the best inhibitors of E. coli PDHc-E1, were studied by molecular docking, site-directed mutagenesis, and enzymatic assays. These results revealed that the improved inhibition of novel inhibitors compared with that of the lead compound I was due to the formation of a new hydrogen bond with Leu264 at the active site of E. coli PDHc-E1. The results proved the great potential to obtain effective algaecides via the rational design of PDHc-E1 inhibitors. [Figure Presented]
Zhou, Yuan,Feng, Jiangtao,He, Hongwu,Hou, Leifeng,Jiang, Wen,Xie, Dan,Feng, Lingling,Cai, Meng,Peng, Hao
p. 6491 - 6502
(2017/12/26)

Structure and biocatalytic scope of thermophilic flavin-dependent halogenase and flavin reductase enzymes
Flavin-dependent halogenase (Fl-Hal) enzymes have been shown to halogenate a range of synthetic as well as natural aromatic compounds. The exquisite regioselectively of Fl-Hal enzymes can provide halogenated building blocks which are inaccessible using standard halogenation chemistries. Consequently, Fl-Hal are potentially useful biocatalysts for the chemoenzymatic synthesis of pharmaceuticals and other valuable products, which are derived from haloaromatic precursors. However, the application of Fl-Hal enzymes, in vitro, has been hampered by their poor catalytic activity and lack of stability. To overcome these issues, we identified a thermophilic tryptophan halogenase (Th-Hal), which has significantly improved catalytic activity and stability, compared with other Fl-Hal characterised to date. When used in combination with a thermostable flavin reductase, Th-Hal can efficiently halogenate a number of aromatic substrates. X-ray crystal structures of Th-Hal, and the reductase partner (Th-Fre), provide insights into the factors that contribute to enzyme stability, which could guide the discovery and engineering of more robust and productive halogenase biocatalysts.
Menon, Binuraj R. K.,Latham, Jonathan,Dunstan, Mark S.,Brandenburger, Eileen,Klemstein, Ulrike,Leys, David,Karthikeyan, Chinnan,Greaney, Michael F.,Shepherd, Sarah A.,Micklefield, Jason
supporting information
p. 9354 - 9361
(2016/10/13)

A Structure-Guided Switch in the Regioselectivity of a Tryptophan Halogenase
Flavin-dependent halogenases are potentially useful biocatalysts for the regioselective halogenation of aromatic compounds. Haloaromatic compounds can be utilised in the synthesis and biosynthesis of pharmaceuticals and other valuable products. Here we report the first X-ray crystal structure of a tryptophan 6-halogenase (SttH), which enabled key residues that contribute to the regioselectivity in tryptophan halogenases to be identified. Structure-guided mutagenesis resulted in a triple mutant (L460F/P461E/P462T) that exhibited a complete switch in regioselectivity; with the substrate 3-indolepropionate 75 % 5-chlorination was observed with the mutant in comparison to 90 % 6-chlorination for the wild-type SttH. This is the first clear example of how regiocomplementary halogenases can be created from a single parent enzyme. The biocatalytic repertoire of SttH was also expanded to include a range of indolic and non-indolic substrates.
Shepherd, Sarah A.,Menon, Binuraj R. K.,Fisk, Heidi,Struck, Anna-Winona,Levy, Colin,Leys, David,Micklefield, Jason
p. 821 - 824
(2016/05/19)

Silica-sulfuric acid: Novel, simple, efficient and reusable catalyst for hydration of nitrile to amide
Silica-sulfuric acid efficiently catalyzes conversion of aliphatic, substituted aromatic and hetero aromatic nitriles to their corresponding amides in good to excellent yields under reflux condition. Products obtained were purified by column chromatography method and characterized by 1H NMR, 13C NMR and mass spectral analysis.
Chandrashekharappa, Sandeep,Venugopala, Katharigatta N.,Venugopala, Rashmi,Odhav, Bharti
p. 2177 - 2180
(2016/07/21)

Optically-Detectable Enzyme Substrates and Their Method of Use
The present invention relates to compounds that are substrates for an enzyme, and upon reaction with the enzyme provide a detectable response, such as an optically detectable response. In particular, the compounds have utility in detecting the presence of a β-lactamase in a sample. In addition to the compounds, methods are disclosed for analyzing a sample for the presence of a β-lactmase, for example, as an indicator of expression of a nucleic acid sequence including a sequence coding for a β-lactmase. Kits are disclosed that include the disclosed compounds and additional components, for example, cells, antibodies, a β-lactmase or instructions for using the components in an assay.
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Paragraph 0407-0408

(2016/06/06)

Extending the biocatalytic scope of regiocomplementary flavin-dependent halogenase enzymes
Flavin-dependent halogenases are potentially valuable biocatalysts for the regioselective halogenation of aromatic compounds. These enzymes, utilising benign inorganic halides, offer potential advantages over traditional non-enzymatic halogenation chemistry that often lacks regiocontrol and requires deleterious reagents. Here we extend the biocatalytic repertoire of the tryptophan halogenases, demonstrating how these enzymes can halogenate a range of alternative aryl substrates. Using structure guided mutagenesis we also show that it is possible to alter the regioselectivity as well as increase the activity of the halogenases with non-native substrates including anthranilic acid; an important intermediate in the synthesis and biosynthesis of pharmaceuticals and other valuable products. This journal is
Shepherd, Sarah A.,Karthikeyan, Chinnan,Latham, Jonathan,Struck, Anna-Winona,Thompson, Mark L.,Menon, Binuraj R. K.,Styles, Matthew Q.,Levy, Colin,Leys, David,Micklefield, Jason
p. 3454 - 3460
(2015/05/27)

Synthesis, antiproliferative activity and possible mechanism of action of novel 2-acetamidobenzamides bearing the 2-phenoxy functionality
Several new 2-(2-phenoxyacetamido)benzamides 17a-v, 21 and 22 were synthesized by stirring in pyridine the acid chlorides 16a-e and the appropriate5-R-4-R1-2-aminobenzamide 15a-e and initially evaluated in vitro for antiproliferative activity against the K562 (human chronic myelogenous leukemia) cell line. Some of synthesized compounds were evaluated for their in vitro antiproliferative activity against the full NCI tumor cell line panel derived from nine clinically isolated cancer types (leukemia, non-small cell lung, colon, CNS, melanoma, ovarian, renal, prostate and breast). The most active compounds caused an arrest of K562 cells in the G0-G1 phase of cell cycle and induction of apoptosis, which was mediated by caspase activation.
Raffa, Demetrio,Maggio, Benedetta,Plescia, Fabiana,Cascioferro, Stella,Raimondi, Maria Valeria,Cancemi, Gabriella,D'Anneo, Antonella,Lauricella, Marianna,Cusimano, Maria Grazia,Bai, Ruoli,Hamel, Ernest,Daidone, Giuseppe
p. 6305 - 6316
(2015/10/05)

Recyclable ionic liquid iodinating reagent for solvent free, regioselective iodination of activated aromatic and heteroaromatic amines
This article describes a simple, efficient method for iodination of activated aromatic and heteroaromatic amines using recyclable 1-butyl-3-methylpyridinium dichloroiodate (BMPDCI) as an ionic liquid iodinating reagent, in the absence of any solvent. The main advantages are a simple efficient procedure, good yields and no need for any base/toxic heavy metals, or oxidizing agents. The ionic liquid was recovered and recycled in five subsequent reactions, without much loss of activity. This method was applied for the synthesis of the antiprotozoal drug iodoquinol and the antifungal drug clioquinol.
Deshmukh, Amarsinh,Gore, Babasaheb,Thulasiram, Hirekodathakallu V.,Swamy, Vincent P.
p. 88311 - 88315
(2015/11/09)

2-Cinnamamido, 2-(3-phenylpropiolamido), and 2-(3-phenylpropanamido) benzamides: Synthesis, antiproliferativeactivity, and mechanism of action
Several new benzamides 4a-q were synthesized by stirring in pyridine the acid chlorides 3a-q with the appropriate anthranilamide derivatives 2a-g. Some of the synthesized compounds were evaluated for their in vitro antiproliferative activity against a panel of 5 human cell lines (K562 human chronic myelogenous leukemia cells, MCF-7 breast cancer cells, HTC-116 and HT26 colon cancer cells and NCI H460 non-small cell lung cancer cells).
Raffa, Demetrio,Maggio, Benedetta,Raimondi, Maria Valeria,Cusimano, Maria Grazia,Amico, Giandomenico,Carollo, Anna,Conaldi, Pier Giulio,Bai, Ruoli,Hamel, Ernest,Daidone, Giuseppe
p. 427 - 435
(2013/10/01)

Synthesis, antiproliferative activity, and mechanism of action of a series of 2-{[(2E)-3-phenylprop-2-enoyl]amino}benzamides
Several new 2-{[(2E)-3-phenylprop-2-enoyl]amino}benzamides 12a-s and 17t-v were synthesized by stirring in pyridine the (E)-3-(2-R1-3-R2-4-R3-phenyl) acrylic acid chlorides 11c-k and 11t-v with the appropriate anthranilamide derivatives 10a-c or the 5-iodoanthranilic acid 13. Some of the synthesized compounds were evaluated for their in vitro antiproliferative activity against the full NCI tumor cell line panel derived from nine clinically isolated cancer types (leukemia, non-small cell lung, colon, CNS, melanoma, ovarian, renal, prostate and breast). COMPARE analysis, effects on tubulin polymerization in cells and with purified tubulin, and effects on cell cycle distribution for 17t, the most active of the series, indicate that these new antiproliferative compounds act as antitubulin agents.
Raffa, Demetrio,Maggio, Benedetta,Plescia, Fabiana,Cascioferro, Stella,Plescia, Salvatore,Raimondi, Maria Valeria,Daidone, Giuseppe,Tolomeo, Manlio,Grimaudo, Stefania,Di Cristina, Antonietta,Pipitone, Rosaria Maria,Bai, Ruoli,Hamel, Ernest
supporting information; experimental part
p. 2786 - 2796
(2011/07/08)

Copper-catalyzed direct amination of ortho-functionalized haloarenes with sodium azide as the amino source
A simple copper-catalyzed direct amination of ortho-functionalized haloarenes (2-halobenzoic acid, 2-halobenzamide, and N-(2-bromophenyl)acetamide derivatives) has been developed with use of NaN3 as the amino source in ethanol, and the corresponding ortho-functionalized aromatic amines were synthesized in good to excellent yields. The protocol undergoes one-pot Ullmann-type coupling of ortho-functionalized haloarenes with NaN3 to lead to ortho-functionalized azidoarenes, followed by reduction with ethanol.
Zhao, Haibo,Fu, Hua,Qiao, Renzhong
experimental part
p. 3311 - 3316
(2010/08/05)

COMPOSITIONS AND METHODS FOR MODULATING GATED ION CHANNELS
Disclosed are quinoline and quinazoline compounds which modulate the activity of the gated ion channels. Compounds that modulate these gated ion channels are useful in the treatment of diseases and disorders related to pain, inflammation, the neurological system, the gastrointestinal system and genitourinary system. Preferred compounds include quinoline or quinazoline derivatives substituted at the 4- position via N(H), C(O) or O moieties.
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Page/Page column Sheet 10/15

(2010/11/27)

Synthesis of 2-amino-5-chlorobenzonitrile
Synthesis of 2-amino-5-chlorobenzonitrile by using cheaper and easily available raw materials is discussed.
Mahajan,Mahalakshmi
p. 1299 - 1300
(2007/10/03)

Discovery of quinazolines as a novel structural class of potent inhibitors of NF-κB activation
We disclose here a new structural class of low-molecular-weight inhibitors of NF-κB activation that were designed and synthesized by starting from quinazoline derivative 6a. Structure-activity relationship (SAR) studies based on 6a elucidated the structural requirements essential for the inhibitory activity toward NF-κB transcriptional activation, and led to the identification of the 6-amino-4-phenethylaminoquinazoline skeleton as the basic framework. In this series of compounds, 11q, containing the 4-phenoxyphenethyl moiety at the C(4)-position, showed strong inhibitory effects on both NF-κB transcriptional activation and TNF-α production. Furthermore, 11q exhibited an anti-inflammatory effect on carrageenin-induced paw edema in rats.
Tobe, Masanori,Isobe, Yoshiaki,Tomizawa, Hideyuki,Nagasaki, Takahiro,Takahashi, Hirotada,Fukazawa, Tominaga,Hayashi, Hideya
p. 383 - 391
(2007/10/03)

Method for inhibiting neoplastic cells and related conditions by exposure to 4-aminoquinazoline derivatives
A method for inhibiting neoplastic cells and related conditions by exposing them to 4-aminoquinazoline derivatives.
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(2008/06/13)

Reductive cyclization of nitro and azide compounds with aldehydes and ketones promoted by metallic samarium and catalytic amount of iodine
Reductive cyclization of nitro and azide compounds was discussed. The cyclization was done with aldehydes and ketones which is promoted by metallic samarium and catalytic amount of iodine. Results showed that three equivalents of samarium were required when the substrate was a nitro compound and one equivalent of samarium was needed for the azide compounds.
Su, Weike,Yang, Bibo
p. 695 - 697
(2007/10/03)

Synthesis and structure-activity relationship of diarylamide derivatives as selective inhibitors of the proliferation of human coronary artery smooth muscle cells
A series of diarylamide derivatives were synthesized and evaluated for their inhibitory activities against human coronary artery smooth muscle cells (SMCs) and human coronary artery endothelial cells (ECs). Compound 2w was superior to the lead compound, Tranilast, in terms of the potency of the activity and cell selectivity.
Gita, Haruhisa,Sobe, Yoshiaki,Akaku, Haruo,Ekine, Rena,Oto, Yuso,Isawa, Satoru,Hayashi, Hideya
p. 549 - 551
(2007/10/03)

Concerning the baker's yeast (Saccharomyces cerevisiae) mediated reduction of nitroarenes and other N-O containing functional groups
Nitro- and nitrosoarenes can be reduced using baker's yeast (Saccharomyces cerevisiae) under two distinct sets of conditions, one of which is in fact a well established non-enzymic process. In order to clarify reports in the literature a comparison of the two methods has been made.
Blackie, Josie A.,Turner, Nicholas J.,Wells, Andrew S.
p. 3043 - 3046
(2007/10/03)

Fluorescent molecular probes I. The synthesis and biological properties of an ELF β-glucuronidase substrate that yields fluorescent precipitates at the enzymatic activity sites
A novel quinazolinone-based fluorogenic β-glucuronidase substrate has been synthesized and evaluated. In this protocol, a partially protected salicyl glucuronide is oxidatively condensed with anthranilamide to afford the required quinazolinonyl glucuronic acid methyl ester that is readily deprotected to yield the desired glucuronide, known as ELF-97 glucuronide. The glucuronide is a sensitive fluorogenic β-glucuronidase substrate that yields a bright yellow-green fluorescent precipitate upon enzymatic reaction.
Diwu, Zhenjun,Lu, Yixin,Upson, Rosalyn H.,Zhou, Mingjie,Klaubert, Dieter H.,Haugland, Richard P.
p. 7159 - 7164
(2007/10/03)

4-aminoquinazoline derivatives
The compounds of the formula: STR1 wherein R1, Y, A, R4, n, Z, CyB, R3, and m are defined in the specification.
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(2008/06/13)

Substituted quinazolines as angiotensin II antagonists
There are disclosed compounds of the general formula I: STR1 wherein A is --CR7 =CR8 --; Z is --CR7 =CR8 --; X is H, NR 9 R10, OR11, CN, F, Cl, I, Br, perfluoroalkyl, alkyl,alkoxy, alkyl-OH, alkoxyalkyl, --(CH2)n CO2 R11,--(CH2)n CONR9 R10 ; Y is NR13,NR13 CR12 R14, CR12 R14 NR13 ; R1 is 5-tetrazolyl, CO2 R11,SO3 H, NHSO2 CH3, NHSO2 CF3 ; R2,R3,R4,R7 R8 is H, alkyl, alkoxy, alkoxyalkyl, alkyl-OH, perfluoroalkyl, aralkyl, CN, NO2, SO2 R13, --(CH2)n CO2 R11,--(CH2)n CONR9 R10, OR11,F,Cl,Br,I,NR9 R10 ; R5 is alkyl, alkoxy, alkoxyalkyl, alkyl-OH, perfluoroalkyl, aralkyl, H, --CN, NO2, SO2 R13,--(CH2)n CO2 R11, --(CH2)n CONR9 R10, --OH,OR11,F,Cl,Br,I,NR9 R10 ; R9,R10 is H, alkyl, alkoxyalkyl,alkyl-OH, perfluoroalkyl, aralkyl; R11 is H, alkyl, aralkyl, alkoxyalkyl; R12,R14 is H, alkyl, alkoxy, alkoxyalkyl, alkyl-OH, perfluoroalkyl, aralkyl, CN, NO2, SO2 R13, --(CH2)n CO2 R11, --(CH2)n CONR9 R10 ; R13 is H, OR11, alkyl, perfluoroalkyl, aralkyl, --(CH2)n CO2 R11,--(CH2)n CONR9 R10 ; wherein alkyl is defined as 1-8 carbons, branched or straight chain; perfluoroalkyl is defined as 1-6 carbons; aralkyl is defined as 7-12 carbons or 7-12 carbons substituted with fluorine, bromine or chlorine and the phamaceutically acceptable salts, solvates and hydrates thereof, which by virtue of their ability to antagonize angiotensin II are useful for the treatment of hypertension and congestive heart-failure. The compounds are also useful for reducing lipid levels in the blood plasma and are thus useful for treating hyperlipidemia and hypercholesterolemia. Also disclosed are processes for the production of said compounds and pharmaceutical compositions containing said compounds.
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(2008/06/13)

Intramolecular 1,3-Dipolar Cycloadditions. Part 1. A Facile Synthesis of Benzimidazo- and Quinazolinotriazolobenzodiazepines
The synthesis of hitherto unknown 9H-benzimidazotriazolobenzodiazepines (4, 11a-e and 12a-c) and 9H-quinazolinotriazolobenzodiazepin-11-ones (5 and 18a-g) is reported. 2-(2-Azidoaryl)benzimidazoles (6 and 10a-h) and 2-(2-azidoaryl)quinazolin-4(3H)-ones (7 and 17a-g) react with propargyl bromide to give non-isolable intermediates which undergo an intramolecular 1,3-dipolar cycloaddition to the title compounds.
Mohiuddin, Ghulam,Reddy, Padala Satyanarayana,Ahmed, Khalil,Ratnam, Chengalvala Venkata
p. 1839 - 1868
(2007/10/02)

1,2,3-Benzotriazin-4-ones and related systems. Part II. Thermolytic decomposition of substituted 1,2,3-benzotriazin-4-ones and isatoic anhydrides
Several nuclear-substituted 1,2,3-benzotriazin-4-ones have been thermolysed in an inert solvent. In each case the major identifiable product proved to be a 2-(o-aminophenyl)-3,1-benzoxazin-4-one. Nuclear-substituted isatoic anhydrides on thermolysis behaved similarly.
Archer, John G.,Barker, Alan J.,Smalley, Robert K.
p. 1169 - 1173
(2007/10/06)