Manuscript Title:

SYNTHESIS OF QUINOLONE DRUG ANALOGUES AND COPPER COMPLEXES: COMPARISON OF BIOLOGICAL ACTIVITIES

Author:

BREENA AWAN, MOHSIN ABBAS KHAN, IRSHAD AHMAD, ANUM MASOOD, ASIM RAZA, SAHARISH KHALIQ, JAVED AHMED, FARHAT ULLAH

DOI Number:

DOI:10.17605/OSF.IO/HTZKG

Published : 2023-04-23

About the author(s)

1. BREENA AWAN - Department of Pharmaceutical Chemistry, Faculty of Pharmacy, The Islamia University of Bahawalpur, Pakistan.
2. MOHSIN ABBAS KHAN - Department of Pharmaceutical Chemistry, Faculty of Pharmacy, The Islamia University of Bahawalpur, Pakistan.
3. IRSHAD AHMAD - Department of Pharmaceutical Chemistry, Faculty of Pharmacy, The Islamia University of Bahawalpur, Pakistan.
4. ANUM MASOOD - Department of Pharmaceutical Chemistry, Faculty of Pharmacy, The Islamia University of Bahawalpur, Pakistan.
5. ASIM RAZA - Department of Pharmaceutical Chemistry, Faculty of Pharmacy, The Islamia University of Bahawalpur, Pakistan.
6. SAHARISH KHALIQ - Department of Pharmaceutical Chemistry, Faculty of Pharmacy, The Islamia University of Bahawalpur, Pakistan.
7. JAVED AHMED - Department of Pharmaceutical Chemistry, Faculty of Pharmacy, The Islamia University of Bahawalpur, Pakistan.
8. FARHAT ULLAH - Department of Pharmaceutical Chemistry, Faculty of Pharmacy, The Islamia University of Bahawalpur, Pakistan.

Full Text : PDF

Abstract

In recent research, we have correlated the chemistry of metals and esters in a single molecular framework by synthesizing new ester ligands derived from the esterification of Quinolone drug with three different aliphatic and aromatic alcohols. Further, these ester ligands were chelated with Cu (II) metal sulfates. Structure elucidation and chemical characterization were done through spectral (1HNMR, FTIR, 13CNMR) and CHNS analysis. In vitro biological evaluation revealed that 5b against Bacillus pumilus and Staphylococcus aureus, 3b for Pseudomonas aeruginosa, 3c & 5c against Escherichia coli showed excellent antibacterial action. The derivative 3c with IC50=1.25±0.54 against urease enzyme was found as the most potent derivative among all the synthesized compounds even more than the parent drug. The 5c gave the highest score (74%) for DPPH (1, 1 diphenyl-2-picrylhydrazyl) radical scavenging activity. So, it is concluded that the most active derivatives can be served as a lead compound for the treatment of gastroenteritis, appendicitis, and crohn’s disease as well as for other bacterial infections.


Keywords

Esters, Metals, Spectral, Enzyme Inhibition, Gastroenteritis, Bacterial.