Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 17, Issue 18, Pages 5199-5203Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2007.06.084
Keywords
measles virus; HTS (high-through screening) hits; Pyrazoles.
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Funding
- 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
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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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