Trypanoside,anti-tuberculosis,leishmanicidal, and cytotoxic activities of tetrahydrobenzothienopyrimidines |
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| Authors: | José C. Aponte 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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| Affiliation: | 1. Department of Chemistry, University of Louisville, Louisville, KY 40292, USA;2. Departamento de Microbiología y Laboratorios de Investigación y Desarrollo, Facultad de Ciencias y Filosofía, Universidad Peruana Cayetano Heredia, Lima, Peru;3. Instituto de Medicina Tropical Alexander von Humboldt, Universidad Peruana Cayetano Heredia, Lima, Peru;4. Bioinformatics Unit—Drug Design Group, Laboratorios de Investigación y Desarrollo, Facultad de Ciencias y Filosofía, Universidad Peruana Cayetano Heredia, Lima, Peru;5. Johns Hopkins University School of Public Health, USA;6. Center for Tropical and Emerging Global Diseases, Coverdell Center for Biomedical Research, University of Georgia, Athens, GA 30602, USA;7. Institute for Tuberculosis Research, College of Pharmacy, University of Illinois at Chicago, Chicago, IL 60612, USA;8. Department of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, University of Illinois at Chicago, Chicago, IL 60612, USA;9. Université de Toulouse;UPS;UMR 152 (Laboratoire de pharmacochimie des substances naturelles et pharmacophores redox), 118, rte de Narbonne, F-31062 Toulouse cedex 9, France |
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| 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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