Antimicrobial pyrimidinones II: synthesis and antimicrobial evaluation of certain novel 5,6-disubstituted 2-(substituted amino)alkylthiopyrimidin-4(3H)-ones

被引：16
作者：
Attia, Mohamed I. [1 ,2 ]
Kansoh, Amany L. [3 ]
El-Brollosy, Nasser R. [1 ,4 ]
机构：
[1] King Saud Univ, Dept Pharmaceut Chem, Coll Pharm, Riyadh 11451, Saudi Arabia
[2] Natl Res Ctr, Pharmaceut & Drug Ind Res Div, Med & Pharmaceut Chem Dept, Giza 12622, Egypt
[3] Natl Res Ctr, Genet Engn & Biotechnol Div, Microbial Chem Dept, Giza 12622, Egypt
[4] Tanta Univ, Dept Chem, Fac Sci, Tanta 31527, Egypt
来源：
MONATSHEFTE FUR CHEMIE | 2014年 / 145卷 / 11期
关键词：
Pyrimidinones; Uracils; Reformatsky reaction; Alkylation; Antimicrobials; URACIL NONNUCLEOSIDE DERIVATIVES; HIV DRUGS EMIVIRINE; ANTIBACTERIAL ACTIVITY; ANTITUMOR-ACTIVITY; ANALOGS; NUCLEOSIDES; INHIBITORS; MKC-442; DESIGN; PYRIMIDINE-5-CARBONITRILES;
D O I：
10.1007/s00706-014-1253-2
中图分类号：
O6 [化学];
学科分类号：
0703 ;
摘要：
A convenient synthesis of certain novel 5,6-disubstituted 2-(substituted amino)alkylthiopyrimidin-4(3H)-ones is reported. 5,6-Disubstituted-2-thiouracils were allowed to react with the appropriate (2-chloroethyl/propyl) amine/imide to give the corresponding 5,6-disubstituted 2-(substituted amino)alkylthiopyrimidin-4(3H)-one derivatives in moderate yields. The antimicrobial potential of the target compounds was determined towards Gram-positive bacteria (Staphylococus aureus, Bacillus subtilis, and Bacillus cereus) and pathogenic fungi (Candida albicans and Aspergillus niger). The obtained data were expressed as diameter of the growth inhibition zone and minimum inhibition concentration (MIC) for the test compounds. The most active compound exhibited dual antibacterial (against S. aureus) and antifungal (against C. albicans) effects with MIC value = 0.0524 A mu mol/cm(3).
引用
收藏
页码：1825 / 1837
页数：13
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