The synthesis, anti-inflammatory and antimicrobial activity evaluation of novel thioanalogs of 3,4-dihydrothiopyrimidin-2(1H)-one derivatives of N-aryl urea
| Autor: | Ashish P. Keche, Girish D. Hatnapure, Rajesh H. Tale, Atish H. Rodge, Rajendra P. Pawar, Kalpana M. Patil |
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| Rok vydání: | 2012 |
| Předmět: |
Chemistry
medicine.drug_class Organic Chemistry Pathogenic bacteria medicine.disease_cause Antimicrobial Anti-inflammatory Proinflammatory cytokine Minimum inhibitory concentration chemistry.chemical_compound Thiourea medicine Urea Organic chemistry Amine gas treating General Pharmacology Toxicology and Pharmaceutics |
| Zdroj: | Medicinal Chemistry Research. 21:4252-4260 |
| ISSN: | 1554-8120 1054-2523 |
| DOI: | 10.1007/s00044-011-9943-3 |
| Popis: | A series of novel thiourea analogs of 3,4-dihydropyrimidin-2(1-H)-one derivatives of biological interest were prepared by sequential Bigineli’s reaction, reduction followed by reaction of resulting amine with different arylisothiocynates. All the synthesized compounds (1–23) were screened against the proinflammatory cytokines (TNF-α and IL-6) and antimicrobial activity (antibacterial and antifungal). Biological data revealed that among all the compounds screened, compounds 6, 10, 11, 12, 13, 14, 17, and 20 found to have promising anti-inflammatory activity (42–78% TNF-α and 54–96% IL-6 inhibitory activity at 10 μM). Remarkably, compounds 3, 4, 5, 6, 15, 22, and 23 revealed promising antimicrobial activity at minimum inhibitory concentration of 10–40 μg/ml against selected pathogenic bacteria and fungi. |
| Databáze: | OpenAIRE |
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