Synthesis and Trypanocidal Evaluation of News 5-[N-(3-(5-Substituted)- 1,3,4-Thiadiazolyl)]Amino-1-Methyl-4-Nitroimidazoles

A. S. Carvalho; D. Gibaldi; A. C. Pinto; M. Bozza; N. Boechat

doi:10.2174/157018006775789667

ISSN: 1570-1808
E-ISSN: 1875-628X

Synthesis and Trypanocidal Evaluation of News 5-[N-(3-(5-Substituted)- 1,3,4-Thiadiazolyl)]Amino-1-Methyl-4-Nitroimidazoles
Authors: A. S. Carvalho¹, D. Gibaldi², A. C. Pinto³, M. Bozza⁴ and N. Boechat⁵
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¹ Departamento de Sintese Organica, Farmanguinhos, Fundacao Oswaldo Cruz, R. Sizenando Nabuco, n0 100, Manguinhos, Rio de Janeiro, 21041.250-Brazil. ² Departamento de Sintese Organica, Farmanguinhos, Fundacao Oswaldo Cruz, R. Sizenando Nabuco, n0 100, Manguinhos, Rio de Janeiro, 21041.250-Brazil. ³ Departamento de Sintese Organica, Farmanguinhos, Fundacao Oswaldo Cruz, R. Sizenando Nabuco, n0 100, Manguinhos, Rio de Janeiro, 21041.250-Brazil. ⁴ Departamento de Sintese Organica, Farmanguinhos, Fundacao Oswaldo Cruz, R. Sizenando Nabuco, n0 100, Manguinhos, Rio de Janeiro, 21041.250-Brazil. ⁵ Departamento de Sintese Organica, Farmanguinhos, Fundacao Oswaldo Cruz, R. Sizenando Nabuco, n0 100, Manguinhos, Rio de Janeiro, 21041.250-Brazil.
Source: Letters in Drug Design & Discovery, Volume 3, Issue 2, Mar 2006, p. 98 - 101
DOI: https://doi.org/10.2174/157018006775789667
- Available online: 01 Mar 2006

Abstract

A new series of 5-[N-(3-(5-substituted)-1,3,4-thiadiazolyl)]amino-1-methyl-4-nitroimidazoles (6ah) has been designed, synthesized and examined for their ability against Trypanosoma cruzi. The compounds were prepared by nucleophilic aromatic substitution. Several bases were investigated as proton scavengers, and lithium diisopropylamide (LDA) was found to be the best base giving products in good yields.

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2006-03-01

2025-09-22

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Article Type: Research Article

Keyword(s): 1,3,4-thiadiazole derivative; megazol; nucleophilic aromatic substitution; trypanocidal activity

Synthesis and Trypanocidal Evaluation of News 5-[N-(3-(5-Substituted)- 1,3,4-Thiadiazolyl)]Amino-1-Methyl-4-Nitroimidazoles

Abstract

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