New carbohydrazide derivatives of 1H-pyrazolo[3,4-b]pyridine and trypanocidal activity

Autor: RAQUEL R.S. SALVADOR, MURILO L. BELLO, IGOR R.L. BARRETO, MARIA A.F. VERA, ESTELA M.F. MURI, SÉRGIO DE ALBUQUERQUE, LUIZA R.S. DIAS
Jazyk: angličtina
Předmět:
Zdroj: Anais da Academia Brasileira de Ciências, Iss 0
Druh dokumentu: article
ISSN: 1678-2690
0001-3765
DOI: 10.1590/0001-3765201620160087
Popis: ABSTRACT This paper reports the in vitro trypanocidal activity evaluation of new carbohydrazide derivatives from 3-methyl-1-phenyl-1H-pyrazolo[3,4-b]pyridine, substituted at C-6 position by phenyl, methyl or trifluoromethyl group. These compounds were evaluated in order to identify the antiparasitic profile against trypomastigote and amastigote forms of Trypanosoma cruzi. The 4-carbohydrazide derivatives presented different profiles of activity. In the investigation of the chemical structure influence in the trypanocidal activity, the results indicated there are large lipophilicity and volume differences among these derivatives. The complementarities of their stereoelectronic and physical-chemical aspects seem to be relevant for the biological activity against T. cruzi.
Databáze: Directory of Open Access Journals