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Benzimidazole analogs as WTA biosynthesis inhibitors targeting methicillin resistant Staphylococcus aureus.
Yang, Shu-Wei; Pan, Jianping; Yang, Christine; Labroli, Marc; Pan, Weidong; Caldwell, John; Ha, Sookhee; Koseoglu, Sandra; Xiao, Jing C; Mayhood, Todd; Sheth, Payal R; Garlisi, Charles G; Wu, Jin; Lee, Sang Ho; Wang, Hao; Tan, Christopher M; Roemer, Terry; Su, Jing.
Afiliação
  • Yang SW; Discovery Chemistry, Merck Research Laboratory, Kenilworth, NJ 07033, United States. Electronic address: shu-wei.yang@merck.com.
  • Pan J; Discovery Chemistry, Merck Research Laboratory, Kenilworth, NJ 07033, United States.
  • Yang C; Discovery Chemistry, Merck Research Laboratory, Kenilworth, NJ 07033, United States.
  • Labroli M; Discovery Chemistry, Merck Research Laboratory, Kenilworth, NJ 07033, United States.
  • Pan W; Discovery Chemistry, Merck Research Laboratory, Kenilworth, NJ 07033, United States.
  • Caldwell J; Discovery Chemistry, Merck Research Laboratory, Kenilworth, NJ 07033, United States.
  • Ha S; Structure Chemistry, Merck Research Laboratory, Kenilworth, NJ 07033, United States.
  • Koseoglu S; In Vitro Pharmacology Group, Merck Research Laboratory, Kenilworth, NJ 07033, United States.
  • Xiao JC; In Vitro Pharmacology Group, Merck Research Laboratory, Kenilworth, NJ 07033, United States.
  • Mayhood T; In Vitro Pharmacology Group, Merck Research Laboratory, Kenilworth, NJ 07033, United States.
  • Sheth PR; In Vitro Pharmacology Group, Merck Research Laboratory, Kenilworth, NJ 07033, United States.
  • Garlisi CG; In Vitro Pharmacology Group, Merck Research Laboratory, Kenilworth, NJ 07033, United States.
  • Wu J; Pharmacokinetics PPDM, Merck Research Laboratory, Kenilworth, NJ 07033, United States.
  • Lee SH; Infectious Disease, Merck Research Laboratory, Kenilworth, NJ 07033, United States.
  • Wang H; Infectious Disease, Merck Research Laboratory, Kenilworth, NJ 07033, United States.
  • Tan CM; Infectious Disease, Merck Research Laboratory, Kenilworth, NJ 07033, United States.
  • Roemer T; Infectious Disease, Merck Research Laboratory, Kenilworth, NJ 07033, United States.
  • Su J; Discovery Chemistry, Merck Research Laboratory, Kenilworth, NJ 07033, United States.
Bioorg Med Chem Lett ; 26(19): 4743-4747, 2016 10 01.
Article em En | MEDLINE | ID: mdl-27575474
ABSTRACT
A series of benzimidazole analogs have been synthesized to improve the profile of the previous lead compounds tarocin B and 1. The syntheses, structure-activity relationships, and selected biochemical data of these analogs are described. The optimization efforts allowed the identification of 21, a fluoro-substituted benzimidazole, exhibiting potent TarO inhibitory activity and typical profile for a wall teichoic acid (WTA) biosynthesis inhibitor. Compound 21 displayed a potent synergistic and bactericidal effect in combination with imipenem against diverse methicillin-resistant Staphylococci.
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Ácidos Teicoicos / Benzimidazóis / Staphylococcus aureus Resistente à Meticilina / Antibacterianos Limite: Animals Idioma: En Ano de publicação: 2016 Tipo de documento: Article
Texto completo
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Ácidos Teicoicos / Benzimidazóis / Staphylococcus aureus Resistente à Meticilina / Antibacterianos Limite: Animals Idioma: En Ano de publicação: 2016 Tipo de documento: Article