Discovery of highly selective and orally available benzimidazole-based phosphodiesterase 10 inhibitors with improved solubility and pharmacokinetic properties for treatment of pulmonary arterial hypertension

Yuncong YANG; Sirui ZHANG; Qian ZHOU; Chen ZHANG; Yuqi GAO; Hao WANG; Zhe LI; Deyan WU; Yinuo WU; Yi-You HUANG; Lei GUO; Hai-Bin LUO

Yuncong YANG; Sirui ZHANG; Qian ZHOU; Chen ZHANG; Yuqi GAO; Hao WANG; Zhe LI; Deyan WU; Yinuo WU; Yi-You HUANG; Lei GUO; Hai-Bin LUO.

Acta Pharmaceutica Sinica B ; (6): 2339-2347, 2020.

Article in English | WPRIM | ID: wpr-881115

ABSTRACT

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

Benzimidazole derivatives; Bioavailability; Crystal structure; Inhibitor; Metabolic stability; Phosphodiesterase 10A; Pulmonary arterial hypertension

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Full text: Available Index: WPRIM (Western Pacific) Language: English Journal: Acta Pharmaceutica Sinica B Year: 2020 Type: Article

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Full text: Available Index: WPRIM (Western Pacific) Language: English Journal: Acta Pharmaceutica Sinica B Year: 2020 Type: Article