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Design and Synthesis of Some Substituted Thiazolo[3,2-a]pyrimidine Derivatives of Potential Biological Activities by Samia G. Abdel Moty; Mostafa A. Hussein; Salah A. Abdel Aziz; Mahrous A. Abou-Salim is a Pharmacology, Toxicology and Pharmaceutics article available to read on EtoBox.

What is Design and Synthesis of Some Substituted Thiazolo[3,2-a]pyrimidine Derivatives of Potential Biological Activities about?

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 __C__log __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 LD~50~ of compounds **2e** and **2v** was determined.

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Author

Samia G. Abdel Moty; Mostafa A. Hussein; Salah A. Abdel Aziz; Mahrous A. Abou-Salim

Published

2013

Language

EN

Field

Pharmacology, Toxicology and Pharmaceutics (Life Sciences)