• Users Online: 1224
  • Print this page
  • Email this page
Year : 2018  |  Volume : 2  |  Issue : 1  |  Page : 31-38

Identification and development of oxoquinazoline derivatives as novel mycobacterial inhibitors targeting cell wall synthesis enzyme

Department Pharmacy, Birla Institute of Technology and Science, Hyderabad, Telangana, India

Correspondence Address:
Prof. Dhramarajan Sriram
Department of Pharmacy, Birla Institute of Technology and Science, Pilani - Hyderabad Campus, Shameerpet, Jawahar Nagar, Ranga Reddy, Hyderabad - 500 078, Telangana
Login to access the Email id

Source of Support: None, Conflict of Interest: None

DOI: 10.4103/bbrj.bbrj_101_17

Rights and Permissions

Background: Tuberculosis (TB) still remains the leading cause of death worldwide and was unanswered till date. Available treatment strategies have many drawbacks such as longer treatment period, side effects, and drug interactions, which result in patient noncompliance. In the present work, we thrived to develop inhibitors against unexplored key target glutamate racemase. Methods: Lead was identified from in-house database using differential scanning fluorimetry, inhibitors were developed by lead derivatization technique and evaluated them by various biological assays. Results: In oxoquinazoline series, compounds 18 (10.1 ± 0.62 μM) and 22 (5.23 ± 0.34 μM) were found to be the most promising potent inhibitors among all. These compounds also showed their inhibition on replicating and nonreplicating bacteria. Conclusion: Our attempt to develop the potent novel inhibitors against Mycobacterium tuberculosis resulted in developing few promising inhibitors, yet these compounds need further studies to answer all questions in drug discovery. Further optimization of compounds can result in still better compounds for treating TB.

Print this article     Email this article
 Next article
 Previous article
 Table of Contents

 Similar in PUBMED
   Search Pubmed for
   Search in Google Scholar for
 Related articles
 Citation Manager
 Access Statistics
 Reader Comments
 Email Alert *
 Add to My List *
 * Requires registration (Free)

 Article Access Statistics
    PDF Downloaded255    
    Comments [Add]    

Recommend this journal