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Potent non-nucleoside inhibitors of the measles virus RNA-dependent RNA polymerase complex.


ABSTRACT: Measles virus (MV) is one of the most infectious pathogens known. In spite of the existence of a vaccine, approximately 350000 deaths/year result from MV or associated complications. Antimeasles compounds could conceivably diminish these statistics and provide a therapy that complements vaccine treatment. We recently described a high-throughput screening hit compound 1 (16677) against MV-infected cells with the capacity to eliminate viral reproduction at 250 nM by inhibiting the action of the virus's RNA-dependent RNA polymerase complex (RdRp). The compound, 1-methyl-3-(trifluoromethyl)- N-[4-sulfonylphenyl]-1 H-pyrazole-5-carboxamide, 1 carries a critical CF 3 moiety on the 1,2-pyrazole ring. Elaborating on the preliminary structure-activity (SAR) study, the present work presents the synthesis and SAR of a much broader range of low nanomolar nonpeptidic MV inhibitors and speculates on the role of the CF 3 functionality.

SUBMITTER: Sun A 

PROVIDER: S-EPMC2587337 | biostudies-literature | 2008 Jul

REPOSITORIES: biostudies-literature

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Potent non-nucleoside inhibitors of the measles virus RNA-dependent RNA polymerase complex.

Sun Aiming A   Yoon Jeong-Joong JJ   Yin Yan Y   Prussia Andrew A   Yang Yutao Y   Min Jaeki J   Plemper Richard K RK   Snyder James P JP  

Journal of medicinal chemistry 20080605 13


Measles virus (MV) is one of the most infectious pathogens known. In spite of the existence of a vaccine, approximately 350000 deaths/year result from MV or associated complications. Antimeasles compounds could conceivably diminish these statistics and provide a therapy that complements vaccine treatment. We recently described a high-throughput screening hit compound 1 (16677) against MV-infected cells with the capacity to eliminate viral reproduction at 250 nM by inhibiting the action of the vi  ...[more]

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