Literature DB >> 30995566

Synthesis and biological evaluation of pyrazolo[3,4-b]pyridine-3-yl pyrimidine derivatives as sGC stimulators for the treatment of pulmonary hypertension.

Liang Li1, Wenpeng Zhang2, Feng Lin3, Xinqiang Lu2, Wei Chen2, Xingzhou Li4, Xinbo Zhou4, Ruibin Su2, Lili Wang2, Zhibing Zheng5, Song Li4.   

Abstract

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.
Copyright © 2019 Elsevier Masson SAS. All rights reserved.

Entities:  

Keywords:  Pulmonary hypertension; Riociguat; pyrazolo[3,4-b]pyridine-3-yl pyrimidine derivatives; sGC stimulators

Mesh:

Substances:

Year:  2019        PMID: 30995566     DOI: 10.1016/j.ejmech.2019.04.014

Source DB:  PubMed          Journal:  Eur J Med Chem        ISSN: 0223-5234            Impact factor:   6.514


  3 in total

1.  New pyridine and chromene scaffolds as potent vasorelaxant and anticancer agents.

Authors:  Dina H Dawood; Aladdin M Srour; Dalia O Saleh; Kelley J Huff; Francesca Greco; Helen M I Osborn
Journal:  RSC Adv       Date:  2021-09-02       Impact factor: 3.361

2.  A multicomponent, facile and catalyst-free microwave-assisted protocol for the synthesis of pyrazolo-[3,4-b]-quinolines under green conditions.

Authors:  Mandlenkosi Robert Khumalo; Surya Narayana Maddila; Suresh Maddila; Sreekantha B Jonnalagadda
Journal:  RSC Adv       Date:  2019-09-30       Impact factor: 4.036

3.  High-Pressure Metal-Free Catalyzed One-Pot Two-Component Synthetic Approach for New 5-Arylazopyrazolo[3,4-b]Pyridine Derivatives.

Authors:  AbdElAziz A Nayl; Hamada Mohamed Ibrahim; Kamal M Dawood; Wael A A Arafa; Ahmed I Abd-Elhamid; Ismail M Ahmed; Mohamed A Abdelgawad; Hazim M Ali; Ibrahim Hotan Alsohaimi; Ashraf A Aly; Stefan Bräse; Asmaa Kamal Mourad
Journal:  Molecules       Date:  2022-09-27       Impact factor: 4.927

  3 in total

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