天然棕榈酸衍生的一系列具有重要药理学意义的精子形两亲杂环化合物的设计、合成和表征

A. Rabie
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引用次数: 0

摘要

天然棕榈酸是一种关键的饱和脂肪酸,用于人类和各种生物的许多生化过程,因为它是最常见的天然长链羧酸,其无与伦比的两亲性精子状骨架,具有惰性的单15-C脂肪链(尾部或载体)和非常活跃的一个羧基(头部),代表了多种有机/药物化学和制药应用中丰富的活性实体和载体,涉及药物设计和配方。1,3,4-恶二唑衍生物及其1,3,4-噻二唑和1,2,4-三唑类似物具有广泛的药理活性。根据杂化化学中众所周知的杂化原理和掺入规范,如果上述三种取代的含氮杂环芳烃核在羧基上直接连接到简单的直棕榈酸主链上,则所生成的分子应该具有很强的生物活性。本研究首次高效设计、合成和表征了四种单尾含氮棕榈酸结构杂环衍生物,引入了一种具有生物相容性的两亲性精子形杂芳香结构的新型生物重要药效团。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Design, Synthesis, and Characterization of Novel Series of Pharmacologically-important Sperm-shaped Amphiphilic Heterocyclic Compounds derived from Natural Palmitic Acid
Natural palmitic acid is a pivotal saturated fatty acid used in many biochemical processes occurring in humans and diverse living creatures, as it is the most common natural long-chain carboxylic acid whose unrivaled amphiphilic sperm-like skeleton with the inert single 15-C aliphatic chain (tail or carrier) and the very active one carboxyl group (head) represent a rich reactive entity and carrier for several organic/medicinal chemistry and pharmaceutics applications with respect to drug design and formulation. Derivatives of 1,3,4-oxadiazoles along with their 1,3,4-thiadiazoles and 1,2,4-triazoles analogs exhibit a broad spectrum of substantial pharmacological activities. Agreeing with the well-known hybridization principles and incorporation norms in hybrid chemistry, if a substituted nitrogenous heterocyclic aromatic nucleus of the three aforementioned kinds is straightway attached to the simple straight palmitic acid backbone at the position of the carboxyl group, the produced molecules are supposed to be very bioactive. This research work reports for the first once the efficient design/synthesis and characterization/elucidation of four one-tailed nitrogen-containing heterocyclic derivatives of palmitic acid constructure, which introduce a novel biologically-important pharmacophore having biocompatible amphiphilic sperm-shaped heteroaromatic structure.
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