2. Academic Validation
  3. Non-nucleoside inhibitors of the measles virus RNA-dependent RNA polymerase complex activity: Synthesis and in vitro evaluation

Non-nucleoside inhibitors of the measles virus RNA-dependent RNA polymerase complex activity: Synthesis and in vitro evaluation

  • Bioorg Med Chem Lett. 2007 Sep 15;17(18):5199-203. doi: 10.1016/j.bmcl.2007.06.084.
Aiming Sun 1,  Nizal Chandrakumar,  Jeong-Joong Yoon,  Richard K Plemper,  James P Snyder
Affiliations

Affiliation

  • 1 Department of Chemistry, 1515 Dickey Drive, Emory University, Atlanta, GA 30322, USA. asun2@emory.edu
PMID: 17643302 DOI: 10.1016/j.bmcl.2007.06.084
Abstract

High-throughput screening has identified 1-methyl-3-(trifluoromethyl)-N-[4-(pyrrolidinylsulfonyl)phenyl]-1H-pyrazole-5-carboxamide 16677 as a novel and potent (IC(50)=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 (CC(50)/IC(50)) of CA. 16,500.

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