Program

PO3-9-4

DEHYDROZINGERONE INSPIRED STYRYL HYDRAZINE THIAZOLE HYBRIDS AS PROMISING CLASS OF ANTI-MYCOBACTERIAL AGENTS

[Speaker] Rajeshwar Reddy Aleti:1
[Co-author] Girish A Hampannavar:1, Rajshekhar V Karpoormath:2, Mahamadhanif B Shaikh:3, Balakumar Chandrasekaran:2
1:UKZN, South Africa, 2:Department of Pharmaceutical Chemistry, Discipline of Pharmaceutical Sciences, College of Health Sciences, University of KwaZulu-Natal, Westville Campus, Durban, South Africa, 3:Department of Pharmaceutical Chemistry, K. L. E. University College of Pharmacy, Vidyanagar, Hubballi - 580031, Karnataka, India

Introduction: Tuberculosis (TB) is a chronic necrotizing bacterial infection caused by Mycobacterium tuberculosis (Mtb), which has been a bane of humanity for thousands of years and remains as one of the flourishing health problems in the world. The global resurgence of TB and development of drug resistance imposes for an imperative attention of medicinal chemists to develop innovative anti-mycobacterial agents as no new classes of anti-TB agents.
Aim(s): From literature, it was also found that derivatives resulting by combining cinnamoyl portion with various chemical classes of compounds have been reported to possess promising anti- mycobacterial activity. So, it was aimed to explore Dehydrozingerone (DZG) to such structural hybridizations on the anticipated activity, hoping to discover a new lead structure that would have a promising anti-mycobacterial activity.
Methods: A novel series of styryl hydrazine thiazole hybrids was achieved using DZG and substituted 2-bromo-1-phenylethanones through efficient and versatile synthetic routes. All the compounds were characterized spectroscopically and evaluated for The MIC of test compounds was assessed against five drug resistant isolates (INH-R1, INH-R2, RIF-R1, RIF-R2 and FQ-R1) of Mtb strains under aerobic conditions.
Results: From the evaluated series, that all tested compounds showed excellent anti-mycobacterial activity against INH-R1 and INH-R2, while two compounds exhibited the most promising anti-mycobacterial activity against the tested organisms. In particular, both resistant strains (R1 and R2) of INH and RIF were found to be extreme while these two compounds had an almost comparable activity with that of Levofloxacin against FQ-R1.
Conclusion: In this work synthesis of a series of styryl hydrazine thiazole hybrids derived from dehydrozingerone established and their in vitro anti-TB activity.

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