ArticleACS medicinal chemistry letters2016
Dehydrozingerone Inspired Styryl Hydrazine Thiazole Hybrids as Promising Class of Antimycobacterial Agents.
Article in ACS medicinal chemistry letters, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.
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Who cites it
8 citing papers in PubMed.
- Hybrids/Conjugates/Chimera Drugs-Antimicrobial Hybrids: Antibiotics, Antifungals, Antituberculars, Antimalarials.Current medicinal chemistry · 2026Review
- Synthesis, characterization, biological activities, and computational studies of pyrazolyl-thiazole derivatives of thiophene.RSC advances · 2024Article
- Article
- Article
- Identification of Small Molecule Inhibitors against Mycobacteria in Activated Macrophages.Molecules (Basel, Switzerland) · 2022Article
- Design and synthesis of pyrazolone-based compounds as potent blockers of SARS-CoV-2 viral entry into the host cells.Journal of molecular structure · 2021Article
- Novel Hybrids of Podophyllotoxin and Coumarin Inhibit the Growth and Migration of Human Oral Squamous Carcinoma Cells.Frontiers in chemistry · 2020Article
- Alkyne-azide cycloaddition analogues of dehydrozingerone as potential anti-prostate cancer inhibitorsMedChemComm · 2017Article
Corrections and comments
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Authors and funding
5 authors.
Funding
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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.
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