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Bioorg Med Chem Lett. 2012 Dec 15;22(24):7739-41. doi: 10.1016/j.bmcl.2012.09.069. Epub 2012 Oct 12.

Synthesis and antimycobacterial activity of calpinactam derivatives.

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  • 1Graduate School of Pharmaceutical Sciences, Kitasato University, 5-9-1 Shirokane, Minato-ku, Tokyo 108-8641, Japan. nagaik@pharm.kitasato-u.ac.jp


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.

Copyright © 2012 Elsevier Ltd. All rights reserved.

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