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高效微波辅助合成、5-苯并咪唑基-2'-脱氧尿苷的抗菌活性和高荧光性。

Efficient microwave-assisted synthesis, antibacterial activity and high fluorescence of 5 benzimidazolyl-2'-deoxyuridines.

机构信息

Laboratoire de Chimie Bioorganique et Macromoléculaire, Faculté des Sciences et Techniques-Guéliz, 40000 Marrakech, Morocco.

出版信息

Bioorg Med Chem. 2012 Jan 1;20(1):480-6. doi: 10.1016/j.bmc.2011.10.041. Epub 2011 Oct 25.

Abstract

A series of novel C-5 benzimidazolyl-2'-deoxyuridines was synthesized in good yields under solvent-free conditions and microwave irradiation from 5-formyl-2'-deoxyuridine and arylenediamine derivatives in the presence of NaHSO(3) as catalyst. Their absorption and fluorescence spectra were measured. They showed intense fluorescence around 400-500nm with quantum yields between 0.3 and 0.5. All compounds studied in this work were screened for their antibacterial activities against a series of Gram positive and negative bacteria. The trifluoromethyl substituted benzimidazole derivatives showed some antibacterial activity.

摘要

在无溶剂条件下并通过微波辐射,以 5-甲酰基-2'-脱氧尿苷和芳二胺衍生物为原料,在 NaHSO3 作为催化剂的条件下,高产率地合成了一系列新型 C-5 苯并咪唑基-2'-脱氧尿嘧啶核苷。测量了它们的吸收和荧光光谱。它们在 400-500nm 左右显示出强烈的荧光,量子产率在 0.3 到 0.5 之间。对所有研究的化合物进行了一系列革兰氏阳性和阴性细菌的抗菌活性筛选。三氟甲基取代的苯并咪唑衍生物表现出一定的抗菌活性。

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