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Journals / Turkish Journal of Chemistry / 2017 / Cilt: 41 - Sayı: 5

Synthesis and MAO inhibitory activity of novel thiazole-hydrazones

Özlem ATLI
Yusuf ÖZKAY
Pages
685–699
Publication Date
2022-11-05
DOI
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AI Summary & Key Takeaways

AI Insight
⚡ TL;DR(Too Long; Didn't Read)

The ADME prediction of the compounds revealed that they may have good pharmacokinetic profiles, which is necessary for drug candidates.

📌 3 Key Takeaways

🎯
Objective & Hypothesis:A series of new thiazole-hydrazones (3a 3n) were synthesized, characterized, and screened for their hMAOA and hMAO-B inhibitory activity by an in vitro fluorometric method.
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Key Findings & Data:Selectivity indexes (SIs) were expressed as IC50 (MAO-A) / IC50 (MAO-B).
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Conclusion & Impact:The ADME prediction of the compounds revealed that they may have good pharmacokinetic profiles, which is necessary for drug candidates.
🔬Design:Research Article
📍Scope:Comprehensive Sample
⚙️Variables:Domain Parameters

Abstract

A series of new thiazole-hydrazones (3a 3n) were synthesized, characterized, and screened for their hMAOA and hMAO-B inhibitory activity by an in vitro fluorometric method. Selectivity indexes (SIs) were expressed as IC50 (MAO-A) / IC50 (MAO-B). Compound 3f showed promising hMAO-A inhibition with an IC50 value of 1.20 µM and displayed a very significant SI of 0.04 towards hMAO-A. The mechanism of hMAO-A inhibition was investigated by enzyme kinetics using Lineweaver Burk graphics. Compound 3f was further screened for its cytotoxicity by using a healthy NIH/3T3 mouse embryonic fibroblast cell line (ATCC CRL1658) and was evaluated as nontoxic at its effective concentration against hMAO-A. The ADME prediction of the compounds revealed that they may have good pharmacokinetic profiles, which is necessary for drug candidates.

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Cite This Article

ATLI, Ö., ÖZKAY, Y. (2022). Synthesis and MAO inhibitory activity of novel thiazole-hydrazones. Turkish Journal of Chemistry, Cilt: 41 - Sayı: 5, 685–699. https://ajindex.com/articles/601900

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