- Hydroxamic acids block replication of hepatitis c virus
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Intrigued by the role of protein acetylation in hepatitis C virus (HCV) replication, we tested known histone deacetylase (HDAC) inhibitors and a focused library of structurally simple hydroxamic acids for inhibition of a HCV subgenomic replicon. While known HDAC inhibitors with varied inhibitory profiles proved to be either relatively toxic or ineffective, structure-activity relationship (SAR) studies on cinnamic hydroxamic acid and benzo[b]thiophen-2-hydroxamic acid gave rise to compounds 22 and 53, which showed potent and selective anti-HCV activity and therefore are promising starting points for further structural optimization and mechanistic studies.
- Ai, Teng,Xu, Yanli,Qiu, Li,Geraghty, Robert J.,Chen, Liqiang
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p. 785 - 800
(2015/01/30)
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- An efficient enantioselective synthesis of florfenicol based on sharpless asymmetric dihydroxylation
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An efficient and highly enantioselective synthesis of florfenicol- via a new intermediate threo-dihydroxy ester, with a Sharpless asymmetric dihydroxylation as the key step, is reported. A ring-opening/reduction strategy avoids the formation of a chlorinated byproduct that occurs in Schumachers phenyloxazoline procedure. The overall yield of florfenicol by this new process is 23% based on 4-(methylsulfonyl)benzaldehyde. Georg Thieme Verlag Stuttgart · New York.
- Wang, Zhong-Hua,Zheng, Chen,Li, Feng,Zhao, Lei,Chen, Fen-Er,He, Qiu-Qin
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scheme or table
p. 699 - 704
(2012/04/04)
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- Syntheses, crystal structures, and antimicrobial activities of nickel(II) and cadmium(II) complexes with 4-methylsulfonyl cinnamate and diamines
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Two metal complexes, [NiII(mscinn)2(pda)2] (1) and [CdII(mscinn)2(dmeda)2·2H 2O] (2) (mscinn=4-methylsulfonyl cinnamate, pda=propane-1,3-diamine, dmeda=N′, N′-dimethylethane-1,2-diamine), were synthesized by reacting 4-methylsulfonyl cinnamate with the diamines and metal salts. Their structures were determined by single-crystal X-ray diffraction analysis. Crystal parameters of 1: C26H38N4NiO8S 2, M=657.43, monoclinic, P21/c, a=16.6123(8) A, b=8.5956(4) A, c=11.2047(5) A, β=107.423(1)°, V=1526.54(12) A3, Z=2, Dcalcd=1.430 g cm-3, F(000)=692, μ=0.825mm-1, R1=0.0257, wR 2=0.0669. Crystal data of 2: C28H42CdN 4O8S2 · 2(H2O), M=775.24, monoclinic, P21/c, a=9.8278(4) A, b=11.6611(5) A, c=15.3972(7) A, β=96.195(1)°, V=1754.26(13) A3, Z=2, Dcalcd=1.468 g cm-3, F(000)=804, μ=0.798mm -1, R1=0.0299, wR2=0.0770. Antimicrobial activities for 1 and 2 against Escherichia coli, Pseudomonas putida, Bacillus subtilis, and Bacillus cereus had better antibacterial activity than their parent carboxylic acid against Gram-positive bacteria (B. subtilis and B. cereus). The cadmium complex of the cinnamate displayed high inhibitory activity with an MIC value of 5 μgmL-1 against P. putida, while the nickel complex also exhibited good inhibitory potency with an MIC value of 5 μgmL-1 against B. subtilis.
- Qian, Shao-Song,Chen, Yue-Hu,Long, Qi-Peng,Wang, Fang,Zhu, Hai-Liang
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p. 4419 - 4429
(2013/02/25)
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- Amides of aminoalkyl-substituted azetidines, pyrrolidines, piperidines and azepanes
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Novel amides of aminoalkyl-substituted azetidines, pyrrolidines, piperidines and azepanes, use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds, and a method of treatment employing these compounds and compositions. The compounds show a high and selective binding affinity to the histamine H3 receptor indicating histamine H3 receptor antagonistic, inverse agonistic or agonistic activity. As a result, the compounds are useful for the treatment of diseases and disorders related to the histamine H3 receptor.
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- NEW BENZOFURAN AND BENZOTHIOPHENE DERIVATIVES AS ANTI-INFLAMMATORY AGENTS
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This invention relates to compounds, which are generally anti-inflammatory and analgesic compounds, and which are represented by Formula I: wherein A is a —CH2—, —C(O)—, —O—, —S—, —S(O)—, or —S(0)2— and the other substituents are as defined in the specification; or prodrugs, individual isomers, mixtures of isomers, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds and methods for their use as therapeutic agents.
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- BENZENESULFONAMIDE DERIVATIVES
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A novel benzenesulfonamide derivative represented by the formula has an inhibitory activity against phospholipase A2, so that it is effective in the treatment of diseases for which such an activity is efficacious
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- BENZENESULFONAMIDE DERIVATIVE
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A novel benzenesulfonamide derivative of formula (I) which has an action of inhibiting phospholipase A2? and therefore is effective in treating diseases for which this action is used to advantage.
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- Central cholinergic agents. II. Synthesis and acetylcholinesterase inhibitory activities of N-[ω-[N-alkyl-N-(phenylmethyl)amino]alkyl]-3-arylpropenamides
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A series of N-[ω-[N-alkyl-N-(phenylmethyl)amino]alkyl]-3-arylpropenamides was prepared and tested for its inhibitory activities on acetylcholinesterase. Some in the series were found to be potent inhibitors. The structure-activity relationships were discussed in detail.
- Ishihara,Kato,Goto
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p. 3236 - 3243
(2007/10/02)
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