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

• Main Authors: Yuncong Yang (Author), Sirui Zhang (Author), Qian Zhou (Author), Chen Zhang (Author), Yuqi Gao (Author), Hao Wang (Author), Zhe Li (Author), Deyan Wu (Author), Yinuo Wu (Author), Yi-You Huang (Author), Lei Guo (Author), Hai-Bin Luo (Author)
• Format: Book
• Published: Elsevier, 2020-12-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.

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 A. As a result, a potent and highly selective...