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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)
Author(s) -
Chen Lingfeng,
Jin Yiyi,
Fu Weitao,
Xiao Siyang,
Feng Chen,
Fang Bo,
Gu Yugui,
Li Chenglong,
Zhao Yunjie,
Liu Zhiguo,
Liang Guang
Publication year - 2017
Publication title -
chemmedchem
Language(s) - English
Resource type - Reports
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201700367
Subject(s) - bronchoalveolar lavage , in vivo , cytokine , lipopolysaccharide , pyrimidine , lung , chemistry , pharmacology , front cover , tumor necrosis factor alpha , stereochemistry , medicine , cover (algebra) , immunology , biology , mechanical engineering , engineering , microbiology and biotechnology
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).