Synthesis and antimycobacterial activity of calpinactam derivatives

  • Bioorg Med Chem Lett. 2012 Dec 15;22(24):7739-41. doi: 10.1016/j.bmcl.2012.09.069.
Kenichiro Nagai  1 ,  Nobuhiro Koyama ,  Noriko Sato ,  Chisato Yanagisawa ,  Hiroshi Tomoda
Affiliations
  • 1. Graduate School of Pharmaceutical Sciences, Kitasato University, 5-9-1 Shirokane, Minato-ku, Tokyo 108-8641, Japan. [email protected]
PMID: 23116887 DOI: 10.1016/j.bmcl.2012.09.069
Abstract

Synthesis of calpinactam 1, a Fungal antimycobacterial metabolite, utilizing solid-phase peptide synthesis is described. To explore the structure-activity relationships of 1, its derivatives with different Amino acids were also synthesized on the basis of the same synthetic strategy. These derivatives were examined for antimycobacterial activity against Mycobacterium smegmatis. Among them, only peptide 6d having d-Ala in place of d-Glu showed moderate activity.

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