36937-65-2Relevant academic research and scientific papers
Design, Synthesis and Evaluation of Thiazolyl-pyrazole Incorporated with Triazole Scaffold for Antimicrobial and Cytotoxic Activity
Bansal, Kushal Kumar,Sharma, Archana,Sharma, Diksha,Sharma, Prabodh Chander
, p. 641 - 648 (2022/01/26)
In the present work, a series of N-{(1-(4-(4-Bromophenyl)thiazol-2-yl)-3-substitutedphenyl-1H-pyrazol-4-yl) methylene}-4H-1, 2, 4-triazol-4-amine analogs were synthesized and examined for their in vitro antimicrobial and cytotoxic action toward MCF-7 and human cervical cancer cell line (HeLa) cell lines. Suitable spectroscopic methods have been used for structural elucidation of synthesized compounds such as infrared and 1H-nuclear magnetic resonance. Biological findings described that compound 5a was the most potent antimicrobial agent substituted with triazole and p-bromo phenyl moiety with minimum inhibitory concentration = 62.5-100 μg/mL in response to bacterial and fungal strains, namely, Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, Streptococcus pyogenes and Candida albicans. The cytotoxic responses showed that the HeLa was more susceptible to the synthesized compounds than the MCF-7. Compound 5a has been endowed with excellent cytotoxic activity with a GI50 value in the concentration of 1.1 μg/mL resistant to HeLa cell lines. The findings confirmed that 1, 3-thiazolyl-pyrazole clubbed triazole compounds demonstrated significant antimicrobial and cytotoxic potential and are remarkable scaffolds for further study in the field of scientific research.
Microwave-assisted synthesis and biological evaluation of new thiazolylhydrazone derivatives as tyrosinase inhibitors and antioxidants
Fu, Xi,Liu, Jinbing,Yan, Yangting,Zhang, Yu
, (2020/02/04)
In this work, we have synthesized a series of 2-thiazolylhydrazone derivatives (1–27) and investigated their biological activities as tyrosinase inhibitors and antioxidants. Some compounds showed potent tyrosinase inhibitory activities and 4-(2-(2-(1-(4-Aminophenyl)ethylidene)-hydrazinyl)thiazol-4-yl) phenol (26) showed more potent inhibitory effect than the standard tyrosinase inhibitor kojic acid (IC50: 9.8 μM vs. 23.6 μM). Compounds 2, 14, and 26 exhibited high antioxidant activities in 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2′-azinobis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) assays. The structure–activity relationship (SAR) indicated that the substitutions of bromine, hydroxyl group, and amino groups cause great effect to the inhibition effect against tyrosinase. The mechanism and kinetic studies demonstrated that the inhibitory effect of compound 26 on the tyrosinase by acting as the reversible and uncompetitive inhibitor. Docking studies suggests that compound 26 interacts strongly with mushroom tyrosinase via hydrogen bonding.
Application of aromatic ketone hydrazone thiazole compound as tyrosinase inhibitor
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Paragraph 0017, (2018/10/19)
The invention discloses an application of an aromatic ketone hydrazone thiazole compound in a tyrosinase inhibitor. The results of the tyrosinase inhibition activity assay show that the synthesized aromatic ketone hydrazone thiazole compounds have better
Novel thiazole clubbed triazole derivatives as antimicrobial, antimalarial, and cytotoxic agents
Bansal, Kushal K.,Sharma, Diksha,Sharma, Archana,Rajak, Harish,Sharma, Prabodh C.
, p. 305 - 312 (2018/09/14)
Thiazole is one of the most potential heterocyclic moieties in bioorganic chemistry and is major tool in drug design and discovery. The present work describes the synthesis of a series of N-{(1-(4-(4bromophenyl) thiazol-2-yl)-3-substitutedphenyl-1H-pyrazo
