Aminothiazoles: Hit to lead development to identify antileishmanial agents

by Bhuniya D, Mukkavilli R, Shivahare R, Launay D, Ravindra T, Dere, Deshpande A, Verma A, Vishwakarma P, Moger M, Pradhan A, Pati H, Gopinath VS, Suman Gupta, Puri SK, Martin D. European Journal of Medicinal Chemistry, 2015, doi:10.1016/j.ejmech.2015.08.013

Summary: As part of the DNDi lead optimization program for the development of new chemical entities to treat visceral leishmaniasis (VL), a series of aminothiazoles were synthesized and screened for in vitro efficacy, solubility and microsomal stability. Forty three analogs were synthesized of which 15 compounds showed very potent subnanomolar efficacy in in vitro systems but the liability of metabolic instability seemed to be the major challenge for this chemical class and remains to be addressed.

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