Seboletswe Pule, Cele Nosipho, Singh Parvesh
School of Chemistry and Physics, University of Kwa-Zulu Natal (UKZN) Private Bag X01, Scottsville, Durban, South Africa.
ChemMedChem. 2023 Apr 3;18(7):e202200618. doi: 10.1002/cmdc.202200618. Epub 2023 Feb 6.
Molecular hybridization is deemed an optimistic approach in drug design and the discovery of novel biologically active molecules as it may advance their affinity and potency while concurrently decreasing associated resistance and side effects. Approximately 20 % of approved drugs were developed using this approach in the past few years. Thiazolidinone is one of the privileged pharmacophores in medicinal chemistry and is associated with various biological activities; it forms a functional unit in several FDA-approved drugs. Consequently, this pharmacophore has attracted the attention of many research groups to further explore its pharmacological relevance by coupling it with other pharmacophoric moieties. This review presents a concise account of scholarly research exploits directed at the biological activities of newly synthesized thiazolidinone-tagged molecular hybrids. Focused attention is given to the existing structural activity relationship in each compound library and the toxicity profile of potent compounds including in silico docking studies (where applicable). This work would provide a base on which new pharmaceuticals with improved potency can be modelled.
分子杂交被认为是药物设计和发现新型生物活性分子的一种乐观方法,因为它可以提高它们的亲和力和效力,同时降低相关的耐药性和副作用。在过去几年中,约20%的获批药物是使用这种方法开发的。噻唑烷酮是药物化学中具有优势的药效基团之一,与多种生物活性相关;它在几种FDA批准的药物中形成功能单元。因此,这个药效基团吸引了许多研究小组的关注,通过将其与其他药效基团部分偶联来进一步探索其药理学相关性。本综述简要介绍了针对新合成的噻唑烷酮标记分子杂化物的生物活性的学术研究成果。重点关注每个化合物库中现有的构效关系以及活性化合物的毒性概况,包括(如适用)计算机对接研究。这项工作将为构建效力更高的新药物提供基础。