Synthesis, Characterization and Pharmacological Evaluation of Chalcones and Its Derivatives for Antileishmanial Activity

Abstract

Medicinal chemistry is almost always geared toward drug discovery and development. The focus on development of new synthetic drug compounds has resulted in the incorporation of many other disciplines, such as biochemistry, combinatorial chemistry, chemical biology, phytochemistry, pharmacology, enzymology, pharmacognosy, statistics, physical chemistry and molecular biology into medicinal chemistry. In this view medicinal chemists are also trying to speed up drug discovery process for finding the lead molecule [1]. The compounds with chalcone as backbone have been reported to possess varied biological and pharmacological activities, including antimicrobial, anti-inflammatory, analgesic, cytotoxic, antitumor, antimalarial, antitubercular, antiviral, anti-HIV, antiulcerative, antileishmanial activities. Leishmaniasis is a vector-borne disease caused by protozoan parasites of the genus Leishmania. It is transmitted through the bite of female phlebotomine sandflies and can range from mild self-healing cutaneous lesions to lethal visceral leishmaniasis. Lic A (1), efficiently inhibited the proliferation of Leishmania donovani and Leishmania major promastigotes and amastigotes in vitro by inhibiting fumarate reductase (Chen et al. 1993), a selective target present in the parasite mitochondria. The Lic C (113) inhibited the growth of the L. major parasite to the same extent as Lic A (1) (Nielson et al. 1995).