Discovery of highly selective and orally available benzimidazole-based phosphodiesterase 10 inhibitors with improved solubility and pharmacokinetic properties for treatment of pulmonary arterial hypertension.
- Author:
Yuncong YANG
1
;
Sirui ZHANG
1
;
Qian ZHOU
1
;
Chen ZHANG
1
;
Yuqi GAO
1
;
Hao WANG
1
;
Zhe LI
1
;
Deyan WU
1
;
Yinuo WU
1
;
Yi-You HUANG
1
;
Lei GUO
1
;
Hai-Bin LUO
1
Author Information
- Publication Type:Journal Article
- Keywords: Benzimidazole derivatives; Bioavailability; Crystal structure; Inhibitor; Metabolic stability; Phosphodiesterase 10A; Pulmonary arterial hypertension
- From: Acta Pharmaceutica Sinica B 2020;10(12):2339-2347
- CountryChina
- Language:English
- Abstract: Optimization efforts were devoted to discover novel PDE10A inhibitors in order to improve solubility and pharmacokinetics properties for a long-term therapy against pulmonary arterial hypertension (PAH) starting from the previously synthesized inhibitor
