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Published on: September 16, 2022
Structure-activity relationship studies of tanzawaic acid A, an antifungal agent against Rhizopus oryzae
Kotaro Tanaka1, Shiho Arima1, Daiki Lee1
1Laboratory of Synthetic Natural Products Chemistry and Medicinal Research Laboratories, School of Pharmacy, Kitasato University, 5-9-1 Shirokane, Minato-ku, Tokyo 108-8641, Japan.
Abstract:
Through structure-activity relationship studies of tanzawaic acid A (TZAA), this research aims to contribute the development of potent antifungal drugs for treating mucormycosis infections. To this end, new TZAA analogs bearing chemical modifications in the side chain and/or C8-methyl group moieties were synthesized. These analogs are not accessible from natural TZAA and therefore required total synthesis. As a result, four of the newly synthesized TZAA analogs exhibited more potent and selective inhibitory activity against R. oryzae compared to TZAA.
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