Rationally designed hybrid molecules with appreciable COX-2 inhibitory and anti-nociceptive activities

Palwinder Singh; Shaveta; Surbhi Sharma; Rajbir Bhatti

doi:10.1016/j.bmcl.2013.11.080

Rationally designed hybrid molecules with appreciable COX-2 inhibitory and anti-nociceptive activities

Bioorg Med Chem Lett. 2014 Jan 1;24(1):77-82. doi: 10.1016/j.bmcl.2013.11.080. Epub 2013 Dec 4.

Authors

Palwinder Singh¹, Shaveta², Surbhi Sharma³, Rajbir Bhatti³

Affiliations

¹ Department of Chemistry, Guru Nanak Dev University, Amritsar 143005, India. Electronic address: palwinder_singh_2000@yahoo.com.
² Department of Chemistry, Guru Nanak Dev University, Amritsar 143005, India.
³ Department of Pharmaceutical Sciences, Guru Nanak Dev University, Amritsar 143005, India.

PMID: 24332492
DOI: 10.1016/j.bmcl.2013.11.080

Abstract

Six molecules were obtained by the combination of three biologically and medicinally significant moieties-indole, chrysin and pyrazole. Bio-evaluation of these hybrid molecules showed significant inhibition of COX-2 enzymatic activity over that of COX-1 and appreciable anti-nociceptive activity, checked at swiss albino mice.

Keywords: Anti-inflammatory; Anti-nociceptive; Chrysin; Indole; Molecular modeling.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Animals
Anti-Inflammatory Agents, Non-Steroidal / chemical synthesis
Anti-Inflammatory Agents, Non-Steroidal / chemistry
Anti-Inflammatory Agents, Non-Steroidal / pharmacology*
Cyclooxygenase 2 / metabolism*
Cyclooxygenase 2 Inhibitors / chemical synthesis
Cyclooxygenase 2 Inhibitors / chemistry
Cyclooxygenase 2 Inhibitors / pharmacology*
Dose-Response Relationship, Drug
Drug Design*
Female
Male
Mice
Models, Molecular
Molecular Structure
Structure-Activity Relationship

Substances

Anti-Inflammatory Agents, Non-Steroidal
Cyclooxygenase 2 Inhibitors
Cyclooxygenase 2