SYNTHESIS AND QSAR STUDY OF NOVEL THIAZOLE MOIETIES HAVING ANTIOXIDANT ACTIVITYAbstract
Thiazoles derivatives are an important class of heterocyclic compounds, reported to possess a wide spectrum of biological activities. Moreover, thiazole nucleus occupies a very important place in the field of antioxidant agents. The above observations prompted us to synthesize some novel thiazole derivatives with various substitutions at along with heterocyclic rings in the same framework for synergistic action. We here in report the synthesis, antioxidant screening & QSAR studies of the new title compounds. Concentrated research on N-((Substituted) benzylidene)-4-(4-chlorophenyl) thiazole-2-carbohydrazides GS-5i-(a-k) & were synthesized, screened for antioxidant activities & QSAR studies. All new entities have good yield and results. From antioxidant activity results, it was observed that the compounds with both electron donating and electron withdrawing groups on the aldehydic phenyl ring influenced the activity. Among all the compounds tested GS-5i-b, GS-5i-d, GS-5i-e, GS-5i-h & GS-5i-i showed the good % inhibition and were found to be more significant compound among all the compounds tested. Compounds GS-5i-j were showed moderate % inhibition and were found to be significant among all the tested compounds. 2D & 3D-QSAR models with moderate to high predictive ability of thiazole derivatives were derived. The role of hydrophobicity as a 3D property was confirmed and also electrostatic and steric effects were found to contribute to antioxidant activity.
G. A. Kashid *, S. K. Singh and J. Saravanan
Suresh Gyan Vihar University, Mahal Jagatpura, Jaipur, Rajasthan, India.
18 April, 2018
09 July, 2018
13 July, 2018
01 December, 2018