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(Reference retrieved automatically from Web of Science through information on FAPESP grant and its corresponding number as mentioned in the publication by the authors.)

Piperamides and their derivatives as potential anti-trypanosomal agents

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Cotinguiba, Fernando [1] ; Regasini, Luis Octavio [1] ; Bolzani, Vanderlan da Silva [1] ; Debonsi, Hosana Maria [2] ; Passerini, Gabriela Duo [3] ; Barretto Cicarelli, Regina Maria [3] ; Kato, Massuo Jorge [4] ; Furlan, Maysa [1]
Total Authors: 8
[1] Univ Estadual Paulista UNESP, Inst Quim, BR-14801970 Araraquara, SP - Brazil
[2] Univ Sao Paulo, Fac Ciencias Farmaceut, BR-14040903 Ribeirao Preto, SP - Brazil
[3] Univ Estadual Paulista UNESP, Fac Ciencias Farmaceut, BR-14801902 Araraquara, SP - Brazil
[4] Univ Sao Paulo, Inst Quim, BR-05508900 Sao Paulo - Brazil
Total Affiliations: 4
Document type: Journal article
Source: MEDICINAL CHEMISTRY RESEARCH; v. 18, n. 9, p. 703-711, DEC 2009.
Web of Science Citations: 49

We describe herein an evaluation of the trypanocidal effect of eight piperamides (1-8) isolated from Piper tuberculatum bearing dihydropyridone, piperidine, and isobutyl moieties against epimastigote forms of Trypanosoma cruzi, the causative agent of Chagas' disease. Based on such results, three hydrogenated and two hydrolyzed derivatives (10-14) were prepared and evaluated as well. The dihydropyridone amides (1-3) displayed higher anti-trypanosomal activity. The (Z)-piplartine (1) showed higher activity with a 50% inhibition concentration (IC(50)) value of 10.5 mu M, almost four times more potent than the positive control, benznidazole (IC(50) = 42.7 mu M), and should be further evaluated as a suitable hit for the design of new antiprotozoal agents. (AU)

FAPESP's process: 03/00886-7 - Phytochemical study of Pterogyne nitens (Leguminosae), synthesis and pharmacological evaluation of natural guandine alkaloids and of potential antitumoral analogues
Grantee:Luis Octávio Regasini
Support type: Scholarships in Brazil - Doctorate (Direct)