Exploration of potential inhibition of newly synthesized derivatives of Methyl Pyridine-4-carboxylate towards COX-1 and COX-2 in the treatment of inflammation and related diseases. | [Abstract Book on International Conference on Food and Applied Sciences (ICFAS-23) 3-5 August 23 • 2023]

Author(s):

1. Muniba Inam: Dept. of Pharmaceutical Chemistry, University of Karachi, Karachi, Pakistan

2. Shazia Haider: Dept. of Pharmaceutical Chemistry, University of Karachi, Karachi, Pakistan

3. Mehreen Lateef: Dept. of Biochemistry, Bahria University, Karachi, Pakistan

4. F. Siddiqui: Dept. of Pharmacology, DOW College of Pharmacy, DOW University of Health Sciences, Karachi, Pakistan

5. Madiha Hamid: Dept. of Pharmaceutical Chemistry, University of Karachi, Karachi, Pakistan; Dept. of Pharmaceutical Chemistry, Faculty of Pharmacy, Hamdard University, Karachi, Pakistan

Abstract:

Biosynthesis of prostaglandins from arachidonic acid (AA) is catalyzed by cyclooxygenase (COX), which exists as COX-1 and COX-2. Elevated levels of multiple prostaglandins have been reported in synovial fluids from patients with rheumatoid arthritis and osteoarthritis. Prostaglandins also play an important role in the pathogenesis of several types of cancers such as breast, liver, and lung with overexpression of cyclooxygenase-2 and overproduction of prostaglandins [1]. The recent prominent discovery involvements of COX-1 and COX-2 are mainly in cancer and inflammation. NSAIDS are the most commonly prescribed medicines in the treatment of pain and inflammation. The long term use of these NSAIDS is associated with various side effects such as gastrointestinal ulcers and cardiotoxicity [2]. In order to reduce the side effects the need of new and effective drug candidates are always desirable. In the present study,five new derivatives of methyl pyridine-4-carboxylate has been synthesized using docking score by MOE and confirmed by different spectroscopic technique to evaluate the potential inhibition of COX-1 and COX-2. The inhibitory potential was explored through in-vitro enzyme inhibition assay. All the synthesized derivatives inhibited both isoforms of COX-1 and COX-2 with IC50values ranging from 20-100µM.

Page(s): 180-180

DOI: DOI not available

Published: Journal: Abstract Book on International Conference on Food and Applied Sciences (ICFAS-23) 3-5 August 23, Volume: 0, Issue: 0, Year: 2023

Keywords:

inflammation , cancer , Prostaglandins , COX1 and COX2 , Pyridine

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