title: 2-(2-Arylphenyl)benzoxazole As a Novel Anti-Inflammatory Scaffold: Synthesis and Biological Evaluation.
abstract: The 2-(2-arylphenyl)benzoxazole moiety has been found to be a new and selective ligand for the enzyme cyclooxygenase-2 (COX-2). The 2-(2-arylphenyl)benzoxazoles 3a-m have been synthesized by Suzuki reaction of 2-(2-bromophenyl)benzoxazole. Further synthetic manipulation of 3f and 3i led to 3o and 3n, respectively. The compounds 3g, 3n, and 3o selectively inhibited COX-2 with selectivity index of 3n much better than that of the COX-2 selective NSAID celecoxib. The in vivo anti-inflammatory potency of 3g and 3n is comparable to that of celecoxib and the nonselective NSAID diclofenac at two different doses, and 3o showed better potency compared to these clinically used NSAIDs.
authors.affiliation: Department of Medicinal Chemistry and Department of Pharmaceutical Technology (Biotechnology), National Institute of Pharmaceutical Education and Research (NIPER) , Sector 67, S. A. S. Nagar 160 062 Punjab, India.
authors.forename: Kapileswar
authors.initials: K
authors.lastname: Seth
authors.affiliation: Department of Medicinal Chemistry and Department of Pharmaceutical Technology (Biotechnology), National Institute of Pharmaceutical Education and Research (NIPER) , Sector 67, S. A. S. Nagar 160 062 Punjab, India.
authors.forename: Sanjeev K
authors.initials: SK
authors.lastname: Garg
authors.affiliation: Department of Medicinal Chemistry and Department of Pharmaceutical Technology (Biotechnology), National Institute of Pharmaceutical Education and Research (NIPER) , Sector 67, S. A. S. Nagar 160 062 Punjab, India.
authors.forename: Raj
authors.initials: R
authors.lastname: Kumar
authors.affiliation: Department of Medicinal Chemistry and Department of Pharmaceutical Technology (Biotechnology), National Institute of Pharmaceutical Education and Research (NIPER) , Sector 67, S. A. S. Nagar 160 062 Punjab, India.
authors.forename: Priyank
authors.initials: P
authors.lastname: Purohit
authors.affiliation: Department of Medicinal Chemistry and Department of Pharmaceutical Technology (Biotechnology), National Institute of Pharmaceutical Education and Research (NIPER) , Sector 67, S. A. S. Nagar 160 062 Punjab, India.
authors.forename: Vachan S
authors.initials: VS
authors.lastname: Meena
authors.affiliation: Indo-Soviet Friendship (ISF) College of Pharmacy, Moga, 142 001 Punjab, India.
authors.forename: Rohit
authors.initials: R
authors.lastname: Goyal
authors.affiliation: Department of Medicinal Chemistry and Department of Pharmaceutical Technology (Biotechnology), National Institute of Pharmaceutical Education and Research (NIPER) , Sector 67, S. A. S. Nagar 160 062 Punjab, India.
authors.forename: Uttam C
authors.initials: UC
authors.lastname: Banerjee
authors.affiliation: Department of Medicinal Chemistry and Department of Pharmaceutical Technology (Biotechnology), National Institute of Pharmaceutical Education and Research (NIPER) , Sector 67, S. A. S. Nagar 160 062 Punjab, India.
authors.forename: Asit K
authors.initials: AK
authors.lastname: Chakraborti
keywords: 2-(2-Arylphenyl)benzoxazoles; 3D QSAR; cyclooxygenase-2 selective; in vivo potency; novel anti-inflammatory scaffold