Recent Progress on Synthesis and Bio-activities of Tetrahydropyrimidine-2-one derivatives

Mayuresh Bhosale, K. Sarvanan, N. Dighe
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Abstract

This review covers up synthesis, characterization and Pharmacological activities of various derivatives of 1,2,3,4-Tetrahydropyrimidine-2-one, including recent mechanistic advances, new building blocks and new pharmacological disclosures. Tetrahydropyrimidines (THPs) are one of the most important systems among the heterocycles. These compounds reported to have less toxicity to human and animals. Various synthesis strategies have been reported for different derivatives of Tetrahydropyrimidines, mainly these involves Biginelli reaction (condensation) consisting of one pot synthesis of 1,2,3,4-Tetrahydropyrimidine derivatives using urea, β-keto ester and aldehyde. These derivatives also forms important part as intermediate in the manufacture of various Pharmaceuticals. Techniques such as infrared spectroscopy, liquid chromatography-mass spectrometry, 1H NMR and 13C NMR spectrometry along with single crystal X-ray diffraction has been reported for structural characterization of these derivatives. U.S. National Library of Medicines, NIH and European PMC have reported many these derivatives. Some of derivatives have reported to have promising anti-bacterial, cytotoxic, antifungal, anti-inflammatory activities. Recently Ultrasound and Microwave promoted synthesis has shown promising results in synthesis of these derivatives. Many exciting prospects await for its exploitation in this fields.
四氢嘧啶-2- 1衍生物的合成及生物活性研究进展
本文综述了1,2,3,4-四氢嘧啶-2- 1衍生物的合成、表征和药理活性,包括最近的机制进展、新的构建模块和新的药理发现。四氢嘧啶(THPs)是杂环化合物中最重要的体系之一。据报道,这些化合物对人类和动物的毒性较小。不同的四氢嘧啶衍生物的合成方法有多种,主要是用尿素、β-酮酯和醛一锅合成1,2,3,4-四氢嘧啶衍生物的Biginelli缩合反应。这些衍生物在各种药品的生产中也作为中间体构成了重要的组成部分。红外光谱、液相色谱-质谱、1H NMR和13C NMR谱以及单晶x射线衍射等技术已被报道用于这些衍生物的结构表征。美国国家药物图书馆,美国国立卫生研究院和欧洲PMC报告了许多这些衍生物。据报道,一些衍生物具有良好的抗菌、细胞毒、抗真菌、抗炎活性。近年来,超声和微波促进合成在这些衍生物的合成中显示出良好的效果。在这一领域有许多令人振奋的开发前景。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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