88899-85-8Relevant articles and documents
Hydroxamic acids block replication of hepatitis c virus
Ai, Teng,Xu, Yanli,Qiu, Li,Geraghty, Robert J.,Chen, Liqiang
, p. 785 - 800 (2015/01/30)
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.
Syntheses, crystal structures, and antimicrobial activities of nickel(II) and cadmium(II) complexes with 4-methylsulfonyl cinnamate and diamines
Qian, Shao-Song,Chen, Yue-Hu,Long, Qi-Peng,Wang, Fang,Zhu, Hai-Liang
, p. 4419 - 4429 (2013/02/25)
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.
NEW BENZOFURAN AND BENZOTHIOPHENE DERIVATIVES AS ANTI-INFLAMMATORY AGENTS
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, (2008/06/13)
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.