254433-11-9Relevant 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.
Synthesis of ethyl-5-(substituted phenyl)-7-methyl-3-oxo-3,5-dihydro-2H- thiazolo[3,2-a]-pyrimidine-6-carboxylates
Pathak, Arun,Narayanaswamy, Venugopala Katharigatta,Joshi, Aakanksha,Rao, Gopal Krishna,Devi, Kalpana
experimental part, p. 273 - 276 (2011/12/14)
A series of ethyl-5-(substituted phenyl)-7-methyl-3-oxo-3,5-dihydro-2H- thiazolo [3,2-a] pyrimidine-6-carboxylates (2a-l) were synthesized by cyclocondensation of ethyl-6-methyl-4-(substituted phenyl)-2-thioxo-1,2,3,4- tetrahydropyrimidine-5-carboxylates,
