New nitrofurans amenable by isocyanide multicomponent chemistry are active against multidrug-resistant and poly-resistant Mycobacterium tuberculosis

Krasavin Mikhail; Parchinsky Vladislav; Kantin GrigoryManicheva OlgaDogonadze MarineVinogradova TatianaKarge BiankaBroenstrup Mark

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New nitrofurans amenable by isocyanide multicomponent chemistry are active against multidrug-resistant and poly-resistant Mycobacterium tuberculosis

机译：New nitrofurans amenable by isocyanide multicomponent chemistry are active against multidrug-resistant and poly-resistant Mycobacterium tuberculosis

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A set of structurally diverse N-amino delta-lactams decorated with a 5-nitro-2-furyl moiety was synthesized using isocyanide-based multicomponent chemistry and evaluated for antibacterial activity. Three compounds displayed a selective and potent (MIC 22-33 mu M) inhibition of M. tuberculosis H(37)Rv strain growth, while other Gram-positive (MRSA and E. faecium) or Gram-negative (E. coli, P. aeruginosa, A. baumannii, K. pneumoniae) pathogens were not affected. The compounds also displayed moderate low cytotoxicity, as demonstrated in cell line viability assays. Several multidrug-and poly-resistant patient-derived M. tuberculosis strains were found to be susceptible to treatment with these compounds. The three most potent compounds share a significant structural similarity which provides a basis for further scaffold-hopping analog design. (C) 2017 Elsevier Ltd. All rights reserved.

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来源
《Bioorganic and medicinal chemistry》 |2017年第6期|1867-1874|共8页
作者
Krasavin Mikhail; Parchinsky Vladislav; Kantin GrigoryManicheva OlgaDogonadze MarineVinogradova TatianaKarge BiankaBroenstrup Mark;
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作者单位

St Petersburg Res Inst Phthisiopulmonol, 2-4 Ligovsky Prospekt, St Petersburg 191036, Russia;

Helmholtz Ctr Infect Res, Inhoffenstr 7, D-38124 Braunschweig, Germany;

St Petersburg State Univ, Inst Chem, St Petersburg 199034, RussiaChem Divers Res Inst, Chimki 141400, Moscow Region, Russia;

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正文语种英语
中图分类药学;
关键词
Nitrofurans; Antitubercular; Drug resistance; Patient-derived strains; Multicomponent chemistry; N-amino lactams;

New nitrofurans amenable by isocyanide multicomponent chemistry are active against multidrug-resistant and poly-resistant Mycobacterium tuberculosis

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