| Autor: |
Abdel Moty SG; Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Assiut University, Assiut 71526, Egypt., Hussein MA; Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Assiut University, Assiut 71526, Egypt., Abdel Aziz SA; Department of Pharmaceutical Medecinal Chemistry, Faculty of Pharmacy, Al Azhar University, Assiut, Egypt., Abou-Salim MA; Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Al Azhar University, Assiut, Egypt. |
| Jazyk: |
angličtina |
| Zdroj: |
Saudi pharmaceutical journal : SPJ : the official publication of the Saudi Pharmaceutical Society [Saudi Pharm J] 2016 Mar; Vol. 24 (2), pp. 119-32. Date of Electronic Publication: 2013 Dec 28. |
| DOI: |
10.1016/j.jsps.2013.12.016 |
| Abstrakt: |
In continuation to our previous work, thiazolopyrimidines 2a-x were synthesized through intramolecular cyclization of 2-phenacylthio-dihydropyrimidine hydrobromides 1a-x using polyphosphoric acid. On the other hand, thiazolo[3,2-a]pyrimidine-3-one 3 was coupled with aryldiazonium salts or condensed with isatin to afford compounds 4a-c or 5, respectively. Chemical structure of the target compounds was substantiated by IR, FT-IR, (1)H-, (13)C and DEPT-(13)C NMR, MS as well as microanalyses. Moreover, the lipophilicity of the target compounds is expressed as Clog P. The antimicrobial screening of the test compounds 2a-x, 4a-c and 5 revealed moderate activity in comparison to reference drugs. Compounds 2a-c, 2e, 2o and 2v showed a gradual increase in their anti-inflammatory activity reaching its maximum at 5 h compared to indomethacin. Furthermore, the analgesic activity of compounds 2a-c, 2e, 2o and 2v revealed a maximum activity after 5 h of injection compared to aspirin and the LD50 of compounds 2e and 2v was determined. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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