Synthesis and Biological Evaluation of Substituted Thiophene Derivatives

A novel series of pyrazolines were synthesized by cycloaddition of various chalcones (prepared by a Claisen-Schmidt condensation of 3-acetyl-2,5-dimethyl thiophene and various aromatic aldehydes) with the phenyl hydrazines in the presence of pyridine and subjected to molecular property prediction by Molinspiration, MolSoft, and Osiris software. The structures of new compounds were established by ¹HNMR, IR, and mass spectral data. Most of the synthesized compounds (1A-E) were found to be in conformity with Lipinski's "rule of five" and other parameters, for their screening for antimicrobial and antifungal activity as oral active leads/drugs. The newly synthesized compounds were evaluated for antibacterial and antifungal activities. Some of the final synthesized compounds have been exhibited promising antibacterial activity and antifungal activity.