Yuh-Meei Lin - Naperville IL Herbert M. Anderson - Woodridge IL Tuah R. Jenta - Chicago IL Michael J. Williams - Ottawa IL Michael T. Flavin - Darien IL Ze-Qi Xu - Naperville IL
Assignee:
Sarawak Medichem Pharmaceuticals, Inc. - Lemont IL
International Classification:
C07D31178 C07D40714
US Classification:
549277
Abstract:
An efficient and scalable method is reported for the isolation of costatolide (2), an HIV-1-specific nonnucleoside reverse transcriptase inhibitor (NNRTI), from the latex of Calophyllum plants such as C. teysmannii var. inophylloide. An overall yield of 10. 6% of costatolide, with a purity of 96%, was obtained by repetitive recrystallization of the latex from a single organic solvent after the oily material was removed by treatment with hexane. A second major component of the latex, soulattrolide (3), another HIV-1 NNRTI, was also isolated. Both compounds were characterized by spectroscopic and chromatographic analyses and their in vitro anti-HIV activities were also confirmed. The results suggest that sufficient supplies of costatolide can be obtained in a relatively low-cost manner from natural sources.
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