期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 17, 期 18, 页码 5199-5203出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2007.06.084
关键词
measles virus; HTS (high-through screening) hits; Pyrazoles.
资金
- NHGRI NIH HHS [U54 HG003918, 1 U54 HG003918-02] Funding Source: Medline
- NIAID NIH HHS [R21 AI056179-01A2, AI071002, AI056179, R21 AI056179, R01 AI071002, R01 AI071002-01] Funding Source: Medline
High-throughput screening has identified l-methyl-3-(trifluoromethyl)-N-[4-(pyrrolidinylsulfonyl)phenyl]-1H-pyrazole-5-carboxamide 16677 as a novel and potent (IC50 = 35-145 nM) inhibitor against multiple primary isolates of diverse measles virus (MV) genotypes currently Circulating worldwide. The synthesis of 16677 and several analogs together with effects on MV replication is described. The most potent analog displays nanomolar inhibition against the MV and a selectivity ratio (CC50/IC50) of ca. 16,500. Published by Elsevier Ltd.
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