Benzimidazole inhibitors of hepatitis C virus NS5B polymerase: Identification of 2-[(4-diarylmethoxy)phenyl]-benzimidazole
摘要:
A series of 1-cycloalkyl-2-phenyl-1H-benzimidazole-5-carboxylic acid derivatives was synthesized and evaluated for inhibitory activity against HCV NS5B RNA-dependent RNA polymerase (RdRp). A SAR study was performed and led to identify the 2-[(4-diarylmethoxy)phenyl]-benzimidazoles as potent inhibitors. They inhibit subgenomic HCV RNA replication in the replicon cells at low micromolar concentrations (EC50 as low as 1.1 mu M). They are selective against. DNA polymerases (IC50 > 10 mu M) and exhibit low cytotoxicity. (C) 2006 Elsevier Ltd. All rights reserved.
Benzimidazole inhibitors of hepatitis C virus NS5B polymerase: Identification of 2-[(4-diarylmethoxy)phenyl]-benzimidazole
摘要:
A series of 1-cycloalkyl-2-phenyl-1H-benzimidazole-5-carboxylic acid derivatives was synthesized and evaluated for inhibitory activity against HCV NS5B RNA-dependent RNA polymerase (RdRp). A SAR study was performed and led to identify the 2-[(4-diarylmethoxy)phenyl]-benzimidazoles as potent inhibitors. They inhibit subgenomic HCV RNA replication in the replicon cells at low micromolar concentrations (EC50 as low as 1.1 mu M). They are selective against. DNA polymerases (IC50 > 10 mu M) and exhibit low cytotoxicity. (C) 2006 Elsevier Ltd. All rights reserved.
A Novel Class of Inhibitors for Human Steroid 5.ALPHA.-Reductase. Phenoxybenzoic Acid Derivatives. I.
作者:Susumu IGARASHI、Takenori KIMURA、Ryo NAITO、Hiromu HARA、Masahiro FUJII、Hiroshi KOUTOKU、Hiroyuki ORITANI、Toshiyasu MASE
DOI:10.1248/cpb.47.1073
日期:——
In a search for novel nonsteroidal inhibitors of human prostatic 5 alpha-reductase, we found a new series of phenoxybenzoic acid derivatives to be potent human prostatic 5 alpha-reductase inhibitors. Among them, 4-(biphenyl-4-yloxy)benzoic acid derivatives (2n, YM-31758), 2o and 2s showed more potent inhibitory activities than finasteride with IC50 values of 0.87, 0.67 and 0.56 nM, respectively. The
Novel cyclic peptide derivatives based on ogipeptins A, B, C, and D were synthesized. Starting with a mixture of ogipeptins A–D, a practical four-step synthetic procedure was followed to prepare novel derivatives with various kinds of acyl side chains. Among the 45 new synthetic derivatives identified, the antibacterial activities of compounds 8-3 and 8-38 were comparable with those of ogipeptin A
High-performance polymer blends, compositions and shaped articles made therefrom
申请人:SOLVAY (Société Anonyme)
公开号:EP2067823A1
公开(公告)日:2009-06-10
Polymer blend (B) consisting of:
- at least one poly(aryletherketone) (P1), and
- at least one high glass temperature sulfone polymer (P2).
Polymer composition (C) consisting of :
- the polymer blend (B) as above described, and.
- at least one ingredient other than the poly(aryletherketone) (P1) and the high glass temperature sulfone polymer (P2),
with the proviso that the polymer composition (C) is free of fibrous carbon nanofiller (N).
Shaped article consisting of one or more parts, at least one part of the shaped article consisting of the polymer blend (B) as above described.
Shaped article consisting of one or more parts, at least one part of the shaped article consisting of the polymer composition (C) as above described.