synthesis of certain pyrimidine derivatives as antimicrobial agents and anti-inflammatory agents某些嘧啶衍生物的合成抗菌药物和抗炎剂.pdfVIP

Molecules 2010, 15, 1882-1890; doi:10.3390/molecule OPEN ACCESS molecules ISSN 1420-3049 /journal/molecules Article Synthesis of Certain Pyrimidine Derivatives as Antimicrobial Agents and Anti-Inflammatory Agents Mosaad S. Mohamed, Samir M. Awad and Amira Ibrahim Sayed * Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Helwan University, Helwan, Egypt * Author to whom correspondence should be addressed; E-Mail: amiraelsaedy@. Received: 11 January 2010; in revised form: 11 March 2010 / Accepted: 12 March 2010 / Published: 15 March 2010 Abstract: A variety of novel bicyclic and tricyclic pyrimidine derivatives was obtained via reaction of 6-amino-2-thioxo-1H-pyrimidine-4-one (1) with a different reagents. The antimicrobial and anti-inflammatory activities of some of the synthesized compounds were tested. Keywords: pyrimidine; 6-amino-2-thioxo-1H-pyrimidine-4-one; antimicrobial; anti- inflammatory 1. Introduction Pyrimidines exhibit a range of pharmacological activity such as antibacterial [1–3], antifungal [4,5], anticancer [6,7], anti-inflammatory [8,9] and cardioprotective effects [10]. These observations led us to attempt the synthesis of some new pyrimidine derivatives using 6-amino-2-thioxo-2,3-dihydro-1H- pyrimidine-4-one (1) as starting material. 2. Results and Discussion The requisite starting material 1 was prepared by the condensation of thiourea with ethylcyanoacetate in sodium ethoxide according to the known procedure [11]. This