title: New carbohydrazide derivatives of 1H-pyrazolo[3,4-b]pyridine and trypanocidal activity.
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.
authors.affiliation: Laboratório de Química Medicinal/LQMed, Faculdade de Farmácia, Universidade Federal Fluminense/UFF, Rua Mário Viana, 523, 24241-000 Santa Rosa, Niterói, RJ, Brazil.
authors.forename: Raquel R S
authors.initials: RR
authors.lastname: Salvador
authors.affiliation: Laboratório de Modelagem Molecular & QSAR/ModMolQSAR, Faculdade de Farmácia, Universidade Federal do Rio de Janeiro/UFRJ/CCS, Av. Carlos Chagas Filho, 373, 21941-599 Rio de Janeiro, RJ, Brazil.
authors.forename: Murilo L
authors.initials: ML
authors.lastname: Bello
authors.affiliation: Laboratório de Química Medicinal/LQMed, Faculdade de Farmácia, Universidade Federal Fluminense/UFF, Rua Mário Viana, 523, 24241-000 Santa Rosa, Niterói, RJ, Brazil.
authors.forename: Igor R L
authors.initials: IR
authors.lastname: Barreto
authors.affiliation: Laboratório de Química Medicinal/LQMed, Faculdade de Farmácia, Universidade Federal Fluminense/UFF, Rua Mário Viana, 523, 24241-000 Santa Rosa, Niterói, RJ, Brazil.
authors.forename: Maria A F
authors.initials: MA
authors.lastname: Vera
authors.affiliation: Laboratório de Química Medicinal/LQMed, Faculdade de Farmácia, Universidade Federal Fluminense/UFF, Rua Mário Viana, 523, 24241-000 Santa Rosa, Niterói, RJ, Brazil.
authors.forename: Estela M F
authors.initials: EM
authors.lastname: Muri
authors.affiliation: Departamento de Análises Clínicas, Toxicológicas e Bromatológicas, Universidade de São Paulo/USP, Faculdade de Ciências Farmacêuticas de Ribeirão Preto/FCFRP, Av. do Café, s/n, 14040-903 Ribeirão Preto, SP, Brazil.
authors.forename: Sérgio DE
authors.initials: S
authors.lastname: Albuquerque
authors.affiliation: Laboratório de Química Medicinal/LQMed, Faculdade de Farmácia, Universidade Federal Fluminense/UFF, Rua Mário Viana, 523, 24241-000 Santa Rosa, Niterói, RJ, Brazil.
authors.forename: Luiza R S
authors.initials: LR
authors.lastname: Dias
mesh_terms: D006834:Hydrazines; D011720:Pyrazoles / Q000737:chemistry*; D011725:Pyridines / Q000737:chemistry*; D014344:Trypanocidal Agents; D014349:Trypanosoma cruzi
chemical_list: C478081:1H-pyrazolo(3,4-b)pyridine; D006834:Hydrazines; D011720:Pyrazoles; D011725:Pyridines; D014344:Trypanocidal Agents; C019289:carbohydrazide