Cover Picture: Design, Synthesis, and Structure–Activity Relationship Analysis of Thiazolo[3,2‐a]pyrimidine Derivatives with Anti‐inflammatory Activity in Acute Lung Injury (ChemMedChem 13/2017)

• Published in: ChemMedChem Vol. 12; no. 13; p. 1013
• Main Authors: Chen, Lingfeng, Jin, Yiyi, Fu, Weitao, Xiao, Siyang, Feng, Chen, Fang, Bo, Gu, Yugui, Li, Chenglong, Zhao, Yunjie, Liu, Zhiguo, Liang, Guang
• Format: Journal Article
• Language: English
• Published: Weinheim Wiley Subscription Services, Inc 06-07-2017
• Subjects: acute lung injury; Alveoli; anti-inflammatory; Anti-inflammatory agents; Bioactive; Bronchus; Cytokines; Derivatives; Inflammation; interleukins; Lipopolysaccharides; Lungs; Mice; Pretreatment; Rodents; Sepsis; thiazolo[3,2-a]pyrimidines; Ventilators
• ISSN: 1860-7179; 1860-7187
• DOI: 10.1002/cmdc.201700367

The front cover picture shows a series of newly discovered compounds with high inhibitory activities against lipopolysaccharide (LPS)‐induced cytokine expression. By performing systematic structure–activity relationship (SAR) studies of the lead compound, two thiazolo[3,2‐a]pyrimidine analogues (11e and 11l) were identified as the most potent anti‐inflammatory compounds. Pretreatment with them in vivo potently decreased the cytokine levels in bronchoalveolar lavage fluid and improved the histopathological changes of the lung in LPS‐stimulated acute lung injury (ALI) mice. These results provide potential anti‐inflammatory candidates for the treatment of ALI and sepsis. More information can be found in the Full Paper by Guang Liang et al. on page 1022 in Issue 13, 2017 (DOI: 10.1002/cmdc.201700175).