401582-66-9Relevant academic research and scientific papers
Design, Synthesis, and Structure–Activity Relationship Analysis of Thiazolo[3,2-a]pyrimidine Derivatives with Anti-inflammatory Activity in Acute Lung Injury
Chen, Lingfeng,Jin, Yiyi,Fu, Weitao,Xiao, Siyang,Feng, Chen,Fang, Bo,Gu, Yugui,Li, Chenglong,Zhao, Yunjie,Liu, Zhiguo,Liang, Guang
, p. 1022 - 1032 (2017/07/11)
Acute lung injury (ALI) has a high lethality rate, and interleukin-6 (IL-6) and tumor necrosis factor-α (TNF-α) contribute most to tissue deterioration in cases of ALI. In this study, we designed and synthesized a new series of thiazolo[3,2-a]pyrimidine derivatives based on a previously identified lead compound, and we evaluated their anti-inflammatory activities. Structure–activity relationship studies led to the discovery of two highly potent inhibitors. The two promising compounds were found to inhibit lipopolysaccharide (LPS)-induced IL-6 and TNF-α release in a dose-dependent manner in mouse primary peritoneal macrophages (MPMs). Furthermore, administration of these compounds resulted in lung histopathological improvements and attenuated LPS-induced ALI in vivo. Taken together, these data indicate that these novel thiazolo[3,2-a]pyrimidine derivatives could be developed as candidate drugs for the treatment of ALI.
An efficient synthesis of some novel bicyclic thiazolopyrimidine derivatives
Mobinikhaledi, Akbar,Zendehdel, Mojgan,Nasab, Mahdia Hamidi,Fard, Mohammad Ali Bodaghi
experimental part, p. 451 - 458 (2010/09/20)
An efficient and rapid synthesis of some thiazolopyrimidine derivatives from pyrimidinthiones and chloroacetyl chloride in refluxing tetrahydrofurane (THF) is described. The method is simple and practical, and generating thiazole derivatives in good isola
