Synthetic & Natural Products Discovery (SNPD) Laboratory, Department of Chemistry, Government College Women University, Faisalabad, 38000, Pakistan.
Future Med Chem. 2024;16(19):1949-1969. doi: 10.1080/17568919.2024.2389767. Epub 2024 Sep 12.
By keeping in aspects, the pharmacological potential of heterocyclic compounds, pyrimidine-based compounds were designed, synthesized and evaluated for α-amylase inhibitory potential. Five new series 1a-l, 2a-d, 3a-d, 4a-d and 5a-d of 1,2,3,4-tetrahydroprimidine-5-carboxylate derivatives were designed by method by taking Alogliptin as reference compound. Here in we describe synthesis and characterization of compounds as potential α-amylase inhibitor. Structure activity relationship (SAR), analysis and molecular modelling approaches generate compounds and as potential lead with good α-amylase inhibitory selection. However, compound failed the criteria of optimization as drug lead by ADME studies while all other compounds showed optimum range for all ADME parameters. Therefore, these compounds can serve as potential lead candidate in developing anti-diabetic therapy.
通过保留各方面的特点，本研究设计、合成并评估了嘧啶类化合物的药理学潜力，以评估其对α-淀粉酶抑制潜力。以阿格列汀为参考化合物，通过 方法设计了五个新的 1a-l、2a-d、3a-d、4a-d 和 5a-d 系列 1,2,3,4-四氢嘧啶-5-羧酸酯衍生物。在这里，我们描述了作为潜在α-淀粉酶抑制剂的化合物的合成和表征。构效关系（SAR）分析和分子建模方法生成了化合物 和 作为具有良好α-淀粉酶抑制选择性的潜在先导物。然而，化合物 由于 ADME 研究未能达到药物先导优化标准，而所有其他化合物在所有 ADME 参数方面均表现出最佳范围。因此，这些化合物可以作为开发抗糖尿病治疗的潜在先导候选物。
