Synthesis and Biological Evaluation of some Novel Pyrano[2,3-d]Pyrimidine Derivatives

P. Talpara, G. Dubal, V. Shah
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引用次数: 1

Abstract

The synthesis of novel Pyrano[2,3-d]pyrimidine derivatives, had been synthesized by three component domino Knoevenagel hetero Diels-Alder reaction. The products were assayed for their in vitro biological assay antibacterial activity against with two Gram-positive bacteria Staphylococcus aureus MTCC-96, Streptococcus pyogenes MTCC 443, two Gram-negative bacteria Escherichia coli MTCC 442, Pseudomonas aeruginosa MTCC 441 and three fungal strains Candida albicans MTCC 227, Aspergillus Niger MTCC 282, Aspergillus clavatus MTCC 1323 taking ampicillin, chloramphenicol, ciprofloxacin, norfloxacin, nystatin, and griseofulvin as standard drugs. Among the various synthesized heterocyclic compounds, 1b, 1c and 1g are display broad spectrum antibacterial and antifungal activities against both gram-positive and gram-negative bacteria as compared with standard drugs.
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一些新型吡喃[2,3-d]嘧啶衍生物的合成及生物学评价
采用三组分Knoevenagel杂Diels-Alder反应合成了新型吡喃[2,3-d]嘧啶衍生物。以氨苄西林、氯霉素、环丙沙星、诺氟沙星、制霉菌素、灰黄霉素为标准药,对2种革兰氏阳性菌金黄色葡萄球菌MTCC-96、化脓性链球菌MTCC 443、2种革兰氏阴性菌大肠埃希菌MTCC 442、铜绿假单胞菌MTCC 441和3种真菌白色念珠菌MTCC 227、黑曲霉MTCC 282、克拉曲霉MTCC 1323进行体外抑菌试验。在各种合成的杂环化合物中,与标准药物相比,1b、1c和1g对革兰氏阳性和革兰氏阴性菌均表现出广谱的抗菌和抗真菌活性。
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