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Pulchrol ( 1 ) is a natural benzochromene isolated from the roots of Bourreria pulchra , shown to possess potent antiparasitic activity towards both Leishmania and Trypanozoma species. As it is not understood which molecular features of 1 are important for the antiparasitic activity, several analogues were synthesized and assayed. The ultimate goal is to understand the structure-activity relationships (SAR:s) and create a QSAR model that can be used for the development of clinically useful antiparasitic agents. In this study, we have synthesized 25 2-methoxy-6,6-dimethyl-6 H -benzo[ c ]chromen analogues of 1 and its co-metabolite pulchral ( 5a ), by semi-synthetic procedures starting from the natural product pulchrol ( 1 ) itself. All 27 compounds, including the two natural products 1 and 5a , were subsequently assayed in vitro for antiparasitic activity against Trypanozoma cruzi , Leishmania brasiliensis and Leishmania amazoniensis . In addition, the cytotoxicity in RAW cells was assayed, and a selectivity index (SI) for each compound and each parasite was calculated. Several compounds are more potent or equi-potent compared with the positive controls Benznidazole ( Trypanozoma ) and Miltefosine ( Leishmania ). The compounds with the highest potencies as well as SI-values are esters of 1 with various carboxylic acids.

SAR:s for the Antiparasitic Plant Metabolite Pulchrol. 1. The Benzyl Alcohol Functionality