Design, in-silico study and biological evaluation of newly synthesized 3-chlorobenzofuran congeners as antitubercular agents

Arabian Journal of Chemistry

Md Rafi Haider¹  Nasir A. Siddiqui²  Mohammad Mustaqeem Abdullah³  M. Shahar Yar⁴  Shahid Karim⁵  Fahd A. Nasr⁵  Adnan J. Al-Rehaily⁵  Omer M. Almarfadi⁵  Ramzi A. Mothana⁵  Kashif Haider⁶ 

[1] Corresponding authors at: Deptt. of Pharmacology, Faculty of Medicine, King Abdulaziz University, Jeddah 21589, Saudi Arabia (Shahid Karim).;Research, Bareilly, Uttar Pradesh, India;;ANA Institute of Pharmaceutical Science &Department of Pharmaceutical Chemistry, School of Pharmaceutical Education and Research (SPER), Jamia Hamdard, Hamdard Nagar, New Delhi 110062, India;Department of Pharmacognosy, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia;Department of Pharmacology, College of Medicine, King Abdul Aziz University, Jeddah, Saudi Arabia;

关键词: Benzofuran;    Pyrazole;    Anti-tubercular;    Structure activity relationship;    In-silico study;   

DOI  :  

来源: DOAJ

【 摘 要 】

Benzofuran is a heterocyclic scaffold present in various natural products and possess excellent pharmacological properties including anti-tubercular activity as well. A novel series 26 compound containing 3-chlorobenzofuran derivatives are designed, synthesized and spectroscopically characterized. In vitro screening of compounds was done against multidrug resistant Mycobacterium tuberculosis H37Rv strains. Out of these compounds 3a, 3b, 3c, 4b and 4c exhibited excellent inhibitory potency with IC 50 values in the range of 43–104 μM. Compound 3b was found to be the most potent with IC 50 value of 51.24 μM and IC 90 value of 88.04 μM. The compound may serve as lead for future development of potential and effective anti-tubercular agent.

【 授权许可】

Unknown