Original Publication Date: 13 October, 2017
Publication / Source: Future Medicinal Chemistry
Authors: Atta KFM, Ibrahim TM, Farahat OOM ET AL.
It has been estimated that there are currently approximately 15 million cases of leishmaniasis worldwide, with an additional 2 million individuals infected annually. In addition, most medications to treat this disease have seen reports of resistance or adverse side effects, presenting the need for an improved therapeutic agent.
In this article, from Future Medicinal Chemistry, the researchers look at pyrazolopyrimidines and their derivatives, synthesizing a new series of pyrazolo[1,5-c]pyrimidines via hybridization strategies and evaluating these for in vitro antileishmanial activity. some compounds were also subject to modelling experiments to rationalize binding scenarios and also assessed for toxicity in vivo.
“Lead optimization cycles for such new chemotypes would broaden the chemical space for the antileishmanial activity and enhance the chances to discover leads with improved prognosis. Subsequently, such efforts would limit the transmission and aim to eradicate the disease.”