» Articles » PMID: 39860299

The Facile Solid-Phase Synthesis of Thiazolo-Pyrimidinone Derivatives

Overview
Journal Molecules
Publisher MDPI
Date 2025 Jan 25
PMID 39860299
Authors
Affiliations
Soon will be listed here.
Abstract

A thiazolo-pyrimidinone derivative library was developed through a facile solid-phase synthesis method. For the reaction, the thiazolo[4,5-]pyrimidin-7(6)-one structure was synthesized through efficient Thorpe-Ziegler and cyclization reactions. The thiazolo[4,5-]pyrimidin-7(6)-one derivative library with a diversity of three had a total of four synthesis steps and 57 compounds. In addition, the yield per synthesis step was 65-97%, which was very high. The developed synthesis method and compounds will be used to find compounds with biological activity through the thiazole derivative structure-activity relationship.

References
1.
Greco A, Tani S, De Marco R, Gentilucci L . Synthesis and analysis of the conformational preferences of 5-aminomethyloxazolidine-2,4-dione scaffolds: first examples of β(2)- and β(2, 2)-homo-Freidinger lactam analogues. Chemistry. 2014; 20(41):13390-404. DOI: 10.1002/chem.201402519. View

2.
Zhao H, Cui G, Jin J, Chen X, Xu B . Synthesis and Pin1 inhibitory activity of thiazole derivatives. Bioorg Med Chem. 2016; 24(22):5911-5920. DOI: 10.1016/j.bmc.2016.09.049. View

3.
Akhtar J, Khan A, Ali Z, Haider R, Shahar Yar M . Structure-activity relationship (SAR) study and design strategies of nitrogen-containing heterocyclic moieties for their anticancer activities. Eur J Med Chem. 2016; 125:143-189. DOI: 10.1016/j.ejmech.2016.09.023. View

4.
Franzini R, Randolph C . Chemical Space of DNA-Encoded Libraries. J Med Chem. 2016; 59(14):6629-44. DOI: 10.1021/acs.jmedchem.5b01874. View

5.
Roy D, Anas M, Manhas A, Saha S, Kumar N, Panda G . Synthesis, biological evaluation, Structure - Activity relationship studies of quinoline-imidazole derivatives as potent antimalarial agents. Bioorg Chem. 2022; 121:105671. DOI: 10.1016/j.bioorg.2022.105671. View