Synthesis, evaluation and modeling of some triazolothienopyrimidinones as anti-inflammatory and antimicrobial agents
| Autor: | Tamer M. Ibrahim, Mai S. El-Shoukrofy, Ahmed M. Farghaly, Alaa El-Din A. Bekhit, R. M. Shafik, Adnan A. Bekhit, Mona M. El-Semary |
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| Rok vydání: | 2017 |
| Předmět: |
Male
Models Molecular Staphylococcus aureus Antifungal Agents medicine.drug_class Microbial Sensitivity Tests Pharmacology medicine.disease_cause 01 natural sciences Anti-inflammatory Rats Sprague-Dawley Ampicillin Drug Discovery Candida albicans medicine Escherichia coli Animals Stomach Ulcer chemistry.chemical_classification Molecular Structure 010405 organic chemistry Anti-Inflammatory Agents Non-Steroidal Biological activity Antimicrobial Anti-Ulcer Agents 0104 chemical sciences Anti-Bacterial Agents Rats 010404 medicinal & biomolecular chemistry Enzyme Biochemistry chemistry Docking (molecular) Molecular Medicine medicine.drug |
| Zdroj: | Future medicinal chemistry. 9(9) |
| ISSN: | 1756-8927 |
| Popis: | Aim: New triazolotetrahydrobenzothienopyrimidinone derivatives were synthesized. Experimental: Their structures were confirmed, and their anti-inflammatory, antimicrobial activities and ulcerogenic potentials were evaluated. Results: Compounds 7a, 10a and 11a showed minimal ulcerogenic effect and high selectivity toward human recombinant COX-2 over COX-1 enzyme with IC50 values of 1.39, 1.22 and 0.56 μM, respectively. Their docking outcome correlated with their biological activity and confirmed the high selectivity binding toward COX-2. Compound 12b displayed antimicrobial activity comparable to that of ampicillin against Escherichia coli while compounds 6 and 11c were similar to ampicillin against Staphylococcus aureus. In addition, compounds 7a, 9a, 10b and 11c showed dual anti-inflammatory/antimicrobial activities. Conclusion: This work represents a promising matrix for developing new potential anti-inflammatory, antimicrobial and dual antimicrobial/anti-inflammatory candidates. [Formula: see text] |
| Databáze: | OpenAIRE |
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