期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 173, 期 -, 页码 107-116出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2019.04.014
关键词
Riociguat; pyrazolo[3,4-b]pyridine-3-yl pyrimidine derivatives; sGC stimulators; Pulmonary hypertension
资金
- Major New Drugs Innovation and Development [2015ZX09102003]
A series of new pyrazolo[3,4-b]pyridin-3-yl pyrimidine derivatives were synthesized and evaluated for the activation of sGC. Compared with riociguat, compound 13a exhibited equivalent in vitro activity on preconstricted rat thoracic aorta rings and in Rat heart Langendorff preparation. Compound 13a also showed acceptable PK profiles, which might become a promising candidate for the treatment of pulmonary hypertension. (C) 2019 Elsevier Masson SAS. All rights reserved.
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