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Journals / Avrupa Yaşam Bilimleri Dergisi / 2026 / Volume: 3 Issue: 1

COX inhibitory profiles of a series of thiadiazole-benzothiazole hybrids

Ahmet Özdemir(ANADOLU UNIVERSITY, FACULTY OF PHARMACY)0000-0003-0280-5550
Halide Edip Temel(ANADOLU UNIVERSITY, FACULTY OF PHARMACY)0000-0002-5233-1165
Pages
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Publication Date
2024-04-30
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AI Summary & Key Takeaways

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

Taken together, compound 7 can be considered as a potential lead compound for the generation of selective COX-1 inhibitors with enhanced efficacy.

📌 3 Key Takeaways

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Objective & Hypothesis:In an endeavour to identify small molecule COX-1 inhibitors, a colorimetric assay protocol was applied for the in vitro evaluation of COX-1 and 2 inhibitory potential of a series of thiadiazole-benzothiazole hybrids.
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Key Findings & Data:The most potent and selective COX-1 inhibitor in this series was found as 2-[(5-amino-1,3,4-thiadiazol-2-yl)thio]-N-(6-chlorobenzothiazol-2-yl)acetamide (7) (51.36 ± 3.32% at 100 µM) compared to SC-560 (83.64 ± 3.76% at 1 µM).
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Conclusion & Impact:Taken together, compound 7 can be considered as a potential lead compound for the generation of selective COX-1 inhibitors with enhanced efficacy.
🔬Design:Research Article
📍Scope:Comprehensive Sample
⚙️Variables:Benzothiazole · cyclooxygenase · molecular docking

Abstract

In an endeavour to identify small molecule COX-1 inhibitors, a colorimetric assay protocol was applied for the in vitro evaluation of COX-1 and 2 inhibitory potential of a series of thiadiazole-benzothiazole hybrids. The most potent and selective COX-1 inhibitor in this series was found as 2-[(5-amino-1,3,4-thiadiazol-2-yl)thio]-N-(6-chlorobenzothiazol-2-yl)acetamide (7) (51.36 ± 3.32% at 100 µM) compared to SC-560 (83.64 ± 3.76% at 1 µM). Compound 7 exerted weaker inhibitory effect on COX-2 (11.05 ± 1.69% at 100 µM). To explore its binding interactions at the active site of human COX-1 (PDB ID: 6Y3C), molecular docking studies were conducted. Compound 7 could establish hydrogen bonds with proper residues thanks to its amide C=O group. In silico studies were employed to shed light on their pharmacokinetic properties. Taken together, compound 7 can be considered as a potential lead compound for the generation of selective COX-1 inhibitors with enhanced efficacy.

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Cite This Article

Özdemir, A., Temel, H. E. (2024). COX inhibitory profiles of a series of thiadiazole-benzothiazole hybrids. Avrupa Yaşam Bilimleri Dergisi, Volume: 3 Issue: 1. https://doi.org/10.55971/EJLS.1443664

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