Synthesis, Crystal Structure, and Antibacterial Activity of 1,2,4-Triazoles and 1,2,4-Triazol-3-one

Abstract

A straightforward method has been developed for the synthesis of 1,2,4‐triazol‐3‐one 3 and 1,2,4‐triazoles 6a, 6b, 6c, 6d starting from N1‐substituted‐N1‐tosylhydrazonates 2 and hydrazine monohydrate. This methodology affords a number of 1,2,4‐triazol‐3‐one 3 and 1,2,4‐triazoles 6a, 6b, 6c, 6d in reasonable yields. The structures of all new compounds were elucidated using infrared, 1H and 13C NMR, high‐resolution mass spectrometry, elemental analysis, and the X‐ray crystallography (for compounds 3 and 6a). Some of the newly synthesized compounds were screened for their antibacterial activity.

Target-Based Design, Synthesis, and Biological Evaluation of Novel 1,2,4-Triazolone Derivatives as Potential nAChR Modulators

“…1,2,4-Triazolone, an important nitrogen-containing heterocycle, can form strong interactions with proteins thanks to its four polar atoms, namely, three nitrogens and one oxygen. The derivatives of 1,2,4-triazolone (Figure ), exhibit excellent biological activities as pharmaceuticals − and agrochemicals such as herbicides and insecticides . Therefore, the functional 1,2,4-triazolone fragment was added to the central part of the model (red portion; Figure a).…”