Trypanoside, anti-tuberculosis, leishmanicidal, and cytotoxic activities of tetrahydrobenzothienopyrimidines

Bioorg Med Chem. 2010 Apr 15;18(8):2880-6. doi: 10.1016/j.bmc.2010.03.018.

José C Aponte ¹, Abraham J Vaisberg, Denis Castillo, German Gonzalez, Yannick Estevez, Jorge Arevalo, Miguel Quiliano, Mirko Zimic, Manuela Verástegui, Edith Málaga, Robert H Gilman, Juan M Bustamante, Rick L Tarleton, Yuehong Wang, Scott G Franzblau, Guido F Pauli, Michel Sauvain, Gerald B Hammond

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1 Department of Chemistry, University of Louisville, Louisville, KY 40292, USA.

PMID: 20356752 DOI: 10.1016/j.bmc.2010.03.018

Abstract

The synthesis of 2-(5,6,7,8-tetrahydro[1]benzothieno[2,3-d]pyrimidin-4-yl)hydrazone-derivatives (BTPs) and their in vitro evaluation against Trypanosoma cruzi trypomastigotes, Mycobacterium tuberculosis, Leishmania amazonensis axenic amastigotes, and six human Cancer cell lines is described. The in vivo activity of the most active and least toxic compounds against T. cruzi and L. amazonensis was also studied. BTPs constitute a new family of drug leads with potential activity against infectious diseases. Due to their drug-like properties, this series of compounds can potentially serve as templates for future drug-optimization and drug-development efforts for use as therapeutic agents in developing countries.

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