Synthesis, Characterization and in vivo Biological Activity of n-(2-chlorophenyl)-2-(2-methyl-5-nitro-1h-imidazol-1-yl) Acetamide and its Derivatives
Omprakash Arjunrao Londhe1, Rohit Jaysing Bhor1★, Prashant Suresh Ingle2, Zameer Shah Mahemood Shah3, Dipali Rajendra Gade5, Rajshree Dadasaheb Ghogare5★ Corresponding author
- 1Department of Pharmaceutical Chemistry, Pravara Rural College of Pharmacy Pravaranagar, Ahmednagar, Maharashtra, INDIA.
- 2Department of Pharmacology, R. C. Patel Institution of Pharmaceutical Education and Research, Shirpur, Maharashtra, INDIA.
- 3Department of Pharmaceutical Chemistry, Anuradha College of Pharmacy, Chikhli, Buldhana, Maharashtra, INDIA.
- 4Department of Pharmaceutical Chemistry, MUPS College of Pharmacy, Degaon, Resod, Maharashtra, INDIA.
- 5Department of Pharmacology, Pravara Rural College of Pharmacy, Pravaranagar, Ahmednagar, Maharashtra, INDIA.
CORRESPONDENCE
Rohit Jaysing Bhor
Department of Pharmaceutical Chemistry, Pravara Rural College of Pharmacy Pravaranagar, Ahmednagar, Maharashtra, INDIA.
Received: 07-02-2024; Revised: 16-02-2024; Accepted: 14-03-2024.
Volume 16, Issue 2 · pp. 252–260 · PUBLISHED · DOI: 10.5530/jyp.2024.16.33
ABSTRACT
Background:A heterocyclic hydrocarbon with distinct fundamental structural features in its molecular structure is imidazole. In Generalized seizure, patient brain has abnormal electrical activity on both sides of the brain but in partial seizures, it happens when electrical activity surges in one part of brain. In the present work, molecular docking analysis was conducted on proposed protein derivatives from the protein data bank using the Auto Dock for Docking programme. Study on protein binding affinity using N-(2-chlorophenyl)-2-(2-methyl-5-nitro-1H-imidazol-1-yl) acetamide derivatives and the GABA receptor. Even if a number of innovative anticonvulsants have been created in India, some types of seizures are still not adequately controlled by smaller side effects even after the use of modern and revolutionary treatments. The World Health Organisation (WHO) estimates that 65 million people worldwide suffer from epilepsy. Nevertheless, epilepsy is an uncontrollable, neurological seizure. Materials and Methods:2-cholro aniline, 2-nitro aniline, 3-nitro aniline, formic acid, acetamide, benzamide and ethanamide have been employed in this study. Results:Our research led us to the conclusion that a variety of compounds have strong anticonvulsant properties. 2-(2-methyl-5-nitro-1H-imidazol-1-yl)- N-{2-[(3-nitrophenyl)amino]phenyl} acetamide OL4;2-{[(2-methyl-5-nitro-1H-imidazol-1-yl) acetyl]amino}phenyl acetate OL5; 2-{[(2-methyl-5-nitro-1H-imidazol-1-yl)acetyl]amino}phenyl propanoate OL6; N-(2-{[(2-methyl-5-nitro-1H-imidazol-1-yl)acetyl]amino}phenyl)propanamide OL7 gives strong anti-convulsant effects against phenytoin drug. Conclusion:The title compounds and its derivatives were examined for their ability to treat convulsions. Studies of the relationship between structure and activity revealed that compounds containing imidazole derivatives that have an electron-withdrawing group have higher activity than those that have an electron-donating group.
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Londhe, O. A., Bhor, R. J., Ingle, P. S., Shah, Z. S. M., Gade, D. R., & Ghogare, R. D. (). Synthesis, Characterization and in vivo Biological Activity of n-(2-chlorophenyl)-2-(2-methyl-5-nitro-1h-imidazol-1-yl) Acetamide and its Derivatives. Journal of Young Pharmacists, 16(2), 252–260. https://doi.org/10.5530/jyp.2024.16.33
