Synthesis of new celecoxib derivatives: A search for novel cyclooxygenase-2 inhibitors as anti-inflammatory agents

2^nd World Chemistry Conference

August 08-10, 2016 Toronto, Canada

Madlen B Labib, Khaled R A Abdellatif , Mohamed A Abdelgawad and Taha H Zidan

Beni Suef University, Egypt

Posters & Accepted Abstracts: Chem Sci J

Abstract :

A new group of COX-2 inhibitors containing (SO2CH3 3a-p or/ and SO2NH2 3i-p), the most important COX-2 pharmacophore were synthesized. Refluxing propen-1-one derivatives with different phenyl hydrazine hydrochloride derivatives in ethanol afforded triaryl pyrazoline derivatives 3a-p. Their structures were confirmed by elemental analysis, IR, 1H NMR, 13C NMR and mass spectral data. All prepared compounds were evaluated for their in vitro COX-1/COX-2 inhibitory activity and the in vivo anti-inflammatory activity. All compounds were more selective for COX-2 isozyme than COX-1 isozyme and showed good in vivo anti-inflammatory activity. Compounds 3g, 3j and 3o showed the highest anti-inflammatory activity and were less ulcerogenic (Ulcer Index=6.85, 7.7, 5.92 respectively) than indomethacin (Ulcer Index=12.3) and comparable to celecoxib (Ulcer Index=4.85).

Biography :

Madlen B Labib has done her BSc in Pharmacy and Pharmaceutical Sciences from Cairo University, Egypt. She completed her MSc in 2006 from Cairo University (Organic Chemistry) and finished her PhD from Beni Suef University (Pharmaceutical Organic Chemistry). She has done her Post-doctoral studies from Beni Suef University, Faculty of Pharmacy. Currently, she is a Lecturer for Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Beni Suef University, Egypt.
Email:madlenwannas@gmail.com