title: Dehydrozingerone Inspired Styryl Hydrazine Thiazole Hybrids as Promising Class of Antimycobacterial Agents.
abstract: Series of styryl hydrazine thiazole hybrids inspired from dehydrozingerone (DZG) scaffold were designed and synthesized by molecular hybridization approach. In vitro antimycobacterial activity of synthesized compounds was evaluated against Mycobacterium tuberculosis H37Rv strain. Among the series, compound 6o exhibited significant activity (MIC = 1.5 μM; IC50 = 0.48 μM) along with bactericidal (MBC = 12 μM) and intracellular antimycobacterial activities (IC50 = <0.098 μM). Furthermore, 6o displayed prominent antimycobacterial activity under hypoxic (MIC = 46 μM) and normal oxygen (MIC = 0.28 μM) conditions along with antimycobacterial efficiency against isoniazid (MIC = 3.2 μM for INH-R1; 1.5 μM for INH-R2) and rifampicin (MIC = 2.2 μM for RIF-R1; 6.3 μM for RIF-R2) resistant strains of Mtb. Presence of electron donating groups on the phenyl ring of thiazole moiety had positive correlation for biological activity, suggesting the importance of molecular hybridization approach for the development of newer DZG clubbed hydrazine thiazole hybrids as potential antimycobacterial agents.
authors.affiliation: Department of Pharmaceutical Chemistry, Discipline of Pharmaceutical Sciences, College of Health Sciences, University of KwaZulu-Natal , Westville Campus, Durban 4000, South Africa.
authors.forename: Girish A
authors.initials: GA
authors.lastname: Hampannavar
authors.affiliation: Department of Pharmaceutical Chemistry, Discipline of Pharmaceutical Sciences, College of Health Sciences, University of KwaZulu-Natal , Westville Campus, Durban 4000, South Africa.
authors.forename: Rajshekhar
authors.initials: R
authors.lastname: Karpoormath
authors.affiliation: Department of Pharmaceutical Chemistry, K.L.E. University College of Pharmacy, Vidyanagar, Hubballi 580031, Karnataka, India; Department of Pharmaceutical Chemistry, Discipline of Pharmaceutical Sciences, College of Health Sciences, University of KwaZulu-Natal, Westville Campus, Durban 4000, South Africa.
authors.forename: Mahesh B
authors.initials: MB
authors.lastname: Palkar
authors.affiliation: Department of Pharmaceutical Chemistry, Discipline of Pharmaceutical Sciences, College of Health Sciences, University of KwaZulu-Natal , Westville Campus, Durban 4000, South Africa.
authors.forename: Mahamadhanif S
authors.initials: MS
authors.lastname: Shaikh
authors.affiliation: Department of Pharmaceutical Chemistry, Discipline of Pharmaceutical Sciences, College of Health Sciences, University of KwaZulu-Natal , Westville Campus, Durban 4000, South Africa.
authors.forename: Balakumar
authors.initials: B
authors.lastname: Chandrasekaran
keywords: Antimycobacterial activity; NIAID; bactericidal; dehydrozingerone; thiazole