Antihyperglycemic Activities of Cryptolepine Analogues: An Ethnobotanical Lead Structure Isolated fromCryptolepis sanguinolenta
Journal of Medicinal Chemistry1998Vol. 41(15), pp. 2754–2764
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Donald Bierer, L. G. DUBENKO, Pingsheng Zhang, Qing Lü, Patricia Imbach, Albert W. Garofalo, Puay‐Wah Phuan, Diana M. Fort, Joane Litvak, R. Eric Gerber, Barbara Sloan, Jian Luo, Raymond Cooper, Gerald M. Reaven
Abstract
Cryptolepine (1) is a rare example of a natural product whose synthesis was reported prior to its isolation from nature. In the previous paper we reported the discovery of cryptolepine's antihyperglycemic properties. As part of a medicinal chemistry program designed to optimize natural product lead structures originating from our ethnobotanical and ethnomedical field research, a series of substituted and heterosubstituted cryptolepine analogues was synthesized. Antihyperglycemic activity was measured in vitro and in an NIDDM mouse model to generate the first structure-bioactivity study about the cryptolepine nucleus.
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