Convenient one-pot synthesis and biological evaluation of phosphoramidates and phosphonates containing heterocycles

Sk. Nayab Rasool, Ch. Subramanyam, D. B. Janakiramudu, P. Supraja, R. Usha, C. N. Raju
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引用次数: 9

Abstract

GRAPHICAL ABSTRACT ABSTRACT A series of new phosphoramidates and phosphonates were synthesized in single step by reacting diethyl phosphorochloridate with various bioactive amines. The newly synthesized compounds 3a-j were tested for antibacterial activity against Gram-positive and Gram-negative bacteria. All the title compounds exhibited good activity. Amongst all the tested compounds, 3b (diethyl(4-(6-fluorobenzo(d)isoxazol-3-yl)piperidin-1-yl)phosphonate), 3c (diethyl 4, 6-difluorobenzo(d)thiazole-2-ylphosphoramidate) and 3d (diethyl 5-nitro-1H-indazol-1-yl- phosphonate) displayed promising antimicrobial activity against Pseudomonas aeruginosa and Trichoderma viride due to the presence of electron with drawing fluoro and nitro groups respectively.
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含杂环磷酰胺酸盐和磷酸盐的便捷一锅合成及生物学评价
摘要以多种生物活性胺为原料,以氯化磷二乙酯为原料,一步合成了一系列新的磷酸酯和膦酸盐。对新合成的化合物3a-j进行了对革兰氏阳性菌和革兰氏阴性菌的抑菌活性测试。标题化合物均表现出良好的活性。在所有被测试的化合物中,3b(二乙基(4-(6-氟苯并(d)异恶唑-3-基)哌啶-1-基)膦酸盐)、3c(二乙基4,6 -二氟苯并(d)噻唑-2-基磷酰胺)和3d(二乙基5-硝基-1-吲哚-1-基膦酸盐)由于分别存在带氟和硝基的电子而对铜绿假单胞菌和绿木霉表现出良好的抗菌活性。
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