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2000
Volume 33, Issue 5
  • ISSN: 0929-8673
  • E-ISSN: 1875-533X

Abstract

Introduction

Tyrosinase, a copper-containing enzyme, is responsible for melanin production, and its overactivity can lead to hyperpigmentation.

Methods

This study aimed to evaluate triazolothiadiazoles (, ) and triazolothiadiazines () against human and mushroom tyrosinase isozymes.

Results

Several derivatives, such as , , , , and were identified as potent and selective inhibitors of mushroom tyrosinase, with IC values ranging from 1.9 to 15.2 µM. Similarly, compounds , , , and effectively inhibited human tyrosinase, with IC values between 12.6 and 18.5 µM. Mechanism-based studies revealed that these active compounds exhibited competitive inhibition against both isozymes without any cytotoxic effects. analysis further demonstrated that these compounds fit well into the active site of both tyrosinase isozymes.

Conclusion

Additionally, the pharmacokinetic profile of these compounds highlighted promising drug-like properties, making them potential candidates for the development of effective therapeutics for skin disorders.

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2025-08-06
2026-02-28

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Discovery of Furan-tethered Triazolothiadiazoles and Triazolothiadiazines as Potent Tyrosinase Inhibitors for the Treatment of Skin Diseases: Insights from Kinetics Data and Computational Modeling
Curr. Med. Chem. 33, 1035 (2026); https://doi.org/10.2174/0109298673349818250302105830
/content/journals/cmc/10.2174/0109298673349818250302105830
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  • Article Type:     Research Article
Keyword(s): cytotoxicity; enzyme kinetics; fused heterocycles; melanin synthesis; molecular docking; Tyrosinase inhibitors

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