Haveliwala Dhaval D, Kamdar Nimesh R, Mistry Prashant T, Patel Saurabh K
a Department of Chemistry Veer Narmad South Gujarat University , Surat , Gujarat , India.
Nucleosides Nucleotides Nucleic Acids. 2014;33(2):80-91. doi: 10.1080/15257770.2013.873128.
The preparation of a series of novel chromone-fused cytosine analogues, i.e., chromeno[2,3-d]pyrimidines has been carried out from substituted 2-amino-4-oxo-4H-chromene-3-carbonitriles with urea, thiourea, and guanidine under different reaction conditions. These chromone-fused cytosine analogues were evaluated for their in vitro activity against Mycobacterium tuberculosis H37Rv strain and different microbial pathogenic strains in cell culture for their structure-activity relationships, respectively. Among the synthesized compounds, 2d, 3a, and 4e showed better results against Mycobacterium tuberculosis H37Rv. The compounds 2a, 2b, and 3a showed potential antibacterial activity against E. coli and P. aeruginosa, while the majority of compounds were found to be active against S. aureus as compared to ampicillin. The synthesized cytosine analogues having an imine (-C&dbnd;NH) have been less sensitive to the bacterial and fungal strains but have a more beneficial effect on Mycobacterium tuberculosis H37Rv.
一系列新型色酮稠合胞嘧啶类似物，即色烯并[2,3 - d]嘧啶，已通过在不同反应条件下，使取代的2 - 氨基 - 4 - 氧代 - 4H - 色烯 - 3 - 腈与尿素、硫脲和胍反应来制备。分别在细胞培养中评估了这些色酮稠合胞嘧啶类似物对结核分枝杆菌H37Rv菌株和不同微生物致病菌株的体外活性，以研究其构效关系。在合成的化合物中，2d、3a和4e对结核分枝杆菌H37Rv显示出较好的结果。化合物2a、2b和3a对大肠杆菌和铜绿假单胞菌显示出潜在的抗菌活性，而与氨苄西林相比，大多数化合物对金黄色葡萄球菌有活性。具有亚胺（-C&dbnd;NH）的合成胞嘧啶类似物对细菌和真菌菌株的敏感性较低，但对结核分枝杆菌H37Rv有更有益的作用。
