Prasher Parteek, Sharma Mousmee
UGC Sponsored Centre for Advanced Studies , Department of Chemistry , Guru Nanak Dev University , Amritsar 143005 , India . Email:
Department of Chemistry , University of Petroleum & Energy Studies , Dehradun 248007 , India.
Medchemcomm. 2019 May 14;10(8):1302-1328. doi: 10.1039/c9md00218a. eCollection 2019 Aug 1.
Contemporary drug discovery approaches rely on library synthesis coupled with combinatorial methods and high-throughput screening to identify leads. However, due to the multitude of components involved, a majority of optimization techniques face persistent challenges related to the efficiency of synthetic processes and the purity of compound libraries. These methods have recently found an upgradation as fragment-based approaches for target-guided synthesis of lead molecules with active involvement of their biological target. The click chemistry approach serves as a promising tool for tailoring the therapeutically relevant biomolecules of interest, improving their bioavailability and bioactivity and redirecting them as efficacious drugs. 1,2,3-1-Triazole nucleus, being a planar and biologically acceptable scaffold, plays a crucial role in the design of biomolecular mimetics and tailor-made molecules with therapeutic relevance. This versatile scaffold also forms an integral part of the current fragment-based approaches for drug design, kinetic target guided synthesis and bioorthogonal methodologies.
当代药物发现方法依赖于库合成与组合方法以及高通量筛选相结合来识别先导化合物。然而，由于涉及的成分众多，大多数优化技术在合成过程的效率和化合物库的纯度方面面临持续挑战。这些方法最近已升级为基于片段的方法，用于在其生物靶标的积极参与下进行先导分子的靶向合成。点击化学方法是一种很有前景的工具，可用于定制感兴趣的治疗相关生物分子，提高其生物利用度和生物活性，并将它们重新导向为有效的药物。1,2,3-1-三唑核作为一种平面且生物学上可接受的支架，在生物分子模拟物和具有治疗相关性的定制分子的设计中起着至关重要的作用。这种多功能支架也是当前基于片段的药物设计、动力学靶点导向合成和生物正交方法的一个组成部分。
