Synthesis of acetylenic derivatives of a substituted 1, 3, 4-thiadiazole as antibacterial agents

Abstract EN

Thiadiazole is a heterocyclic compound that exhibits a wide variety of pharmacological activities such as anticancer, antibacterial, antifungal, antimicrobial, anti‐inflammatory, analgesic and anticonvulsant.

2, 5 disubstituted 1, 3, 4-thiadiazole constitutes an important class of compounds for new drug development because it acts as "hydrogen binding domain" and "two-electron donor system." It also serves as a constrained pharmacophore.

This research highlights the recently synthesized Schiff base and mannich base derivatives and investigation of their chemical and biological behavior.

Depending on this information’s new derivatives of 1, 3, 4-thiadiazole were synthesized and in the hope of having some activities as antibacterial and antifungal.

These are: 1.

N-(5-((4-(piperidin-1-yl) but-2-yn-1-yl) thio)-1, 3, 4-thiadiazol-2-yl) acetamide compound (4).

2.

1-(4-chlorophenyl)-N-(5-((4-(piperidin-1-yl) but-2-yn-1-yl) thio)-1, 3, 4 thiadiazol-2-yl) methanimine compound (6).

3.

1-(4-chlorophenyl)-N-(5-(prop-2-yn-1-ylthio)-1, 3,4thiadiazol-2-yl)methanimine compound(7).

The characterization of mentioned compounds was performed by FTIR spectroscopy, 1HNMR, measurements of their physical properties, and studying of biological activity of the synthesized compounds by well diffusion method