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嘧啶非核苷类似物:嘧啶类新型N-取代氨基和N-磺酰胺衍生物的直接合成。

Pyrimidine non-nucleoside analogs: A direct synthesis of a novel class of N-substituted amino and N-sulfonamide derivatives of pyrimidines.

作者信息

Elgemeie Galal H, Salah Ali M, Abbas Nermeen S, Hussein Hoda A, Mohamed Reham A

机构信息

a Chemistry Department , Faculty of Science, Helwan University , Helwan , Cairo , Egypt.

b Chemistry Department , Faculty of Science, Taibah University , Saudi Arabia.

出版信息

Nucleosides Nucleotides Nucleic Acids. 2017 Mar 4;36(3):213-223. doi: 10.1080/15257770.2016.1257808. Epub 2017 Jan 19.

DOI:10.1080/15257770.2016.1257808
PMID:28102765
Abstract

A convenient method for the regioselective synthesis of pyrimidine non-nucleoside analogs was developed. This study reports a novel and efficient method for the synthesis of a new type of N-substituted amino methylsulfanylpyrimidines and the corresponding pyrazolo[3,4-d]pyrimidines. This series of compounds was designed through the reaction of dimethyl N-cyanodithioiminocarbonate with 2-cyano-N'-(thiophen-2-yl-, furan-2-yl- and pyridin-4-ylmethylene)acetohydrazide and N'-(2-cyanoacetyl)arylsulfonohydrazides. The scope and limitation of the method are demonstrated. The antibacterial and antifungal activities of the synthesized compounds were also evaluated.

摘要

开发了一种用于区域选择性合成嘧啶非核苷类似物的简便方法。本研究报道了一种新型高效的合成新型N-取代氨基甲硫基嘧啶及相应吡唑并[3,4-d]嘧啶的方法。该系列化合物是通过二甲基N-氰基二硫代亚氨基碳酸酯与2-氰基-N'-(噻吩-2-基、呋喃-2-基和吡啶-4-基亚甲基)乙酰肼以及N'-(2-氰基乙酰基)芳基磺酰肼反应设计而成。证明了该方法的适用范围和局限性。还评估了合成化合物的抗菌和抗真菌活性。

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