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Relevant academic research and scientific papers

Synthesis, characterization, in vitro tissue-nonspecific alkaline phosphatase (TNAP) and intestinal alkaline phosphatase (IAP) inhibition studies and computational evaluation of novel thiazole derivatives

Alkaline phosphatases (APs) are a class of homodimeric enzymes which physiologically possess the dephosphorylation ability. APs catalyzes the hydrolysis of monoesters into phosphoric acid which in turn catalyze a transphosphorylation reaction. Thiazoles are nitrogen and sulfur containing aromatic heterocycles considered as effective APs inhibitors. In this context, the current research paper presents the successful synthesis, spectroscopic characterization and in vitro alkaline phosphatase inhibitory potential of new thiazole derivatives. The structure activity relationship and molecular docking studies were performed to find out the binding modes of the screened compounds with the target site of tissue non-specific alkaline phosphatase (h-TNAP) as well as intestinal alkaline phosphatase (h-IAP). Compound 5e was found to be potent inhibitor of h-TNAP with IC50 value of 0.17 ± 0.01 μM. Additionally, compounds 5a and 5i were found to be highly selective toward h-TNAP with IC50 values of 0.25 ± 0.01 μM and 0.21 ± 0.02 μM, respectively. In case of h-IAP compound 5f was the most potent inhibitor with IC50 value of 1.33 ± 0.10 μM. The most active compounds were resort to molecular docking studies on h-TNAP and h-IAP to explore the possible binding interactions of enzyme-ligand complexes. Molecular dynamic simulations were carried out to investigate the overall stability of protein in apo and holo state.

Design, Synthesis and Evaluation of Thiazolyl-pyrazole Incorporated with Triazole Scaffold for Antimicrobial and Cytotoxic Activity

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.

Novel thiazole clubbed triazole derivatives as antimicrobial, antimalarial, and cytotoxic agents

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