Der Pharma Chemica
Journal for Medicinal Chemistry, Pharmaceutical Chemistry and Computational Chemistry


The Synthesis of Potential Anti-Inflammatory Substances among 4-Amino-5-(Pyridin-4-yl)-1,2,4-Triazole(4н)-3-yl-Thioacetamides and their Chemical Modification

Author(s): Syrovaya AO, Chalenko NN, Demchenko AM

Synthesis of new 4-amino-5-(pyridin-4-yl)-1,2,4-triazole(4H)-3-ylthio-acetamides and their pyrrolyl derivatives is described in an article. The initial compound – 4-amino-3-thio-5-(pyridin-4-yl)-1,2,4-triazole(4H) were synthesized by esterification of the initial 4-pyridinecarboxylic acid, and further interaction of resulting methyl ester with hydrazide and potassium 4-pyridine dithiocarbazate wjth the following cyclisation with hydrazine hydrate. The acetamides were obtained by alkylation of the 4-amino-3-thio-5-(pyridin- 4-yl)-1,2,4-triazole(4H) with N-arylsubstituted α-chloracetamides in the presence of KOH. Using Paal-Knorr condensation, the amino group at position 4 was modified into the pyrrole fragment by the action of of 2,5-dimethoxytetrahydrofuran in acetic acid. The preliminary prediction of the possible pharmacological activity by computer prognosis (PASS software) was carried out. Due to the prognosis and analysis of logical data, the substances synthesized will be examined as possible anti-inflammatory agents.

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