Discovery of a novel orally active TRPV4 inhibitor: Part 1. Optimization from an HTS hit

Bioorg Med Chem. 2019 Sep 1;27(17):3775-3787. doi: 10.1016/j.bmc.2019.05.041. Epub 2019 May 31.

Authors

Yuichi Sami¹, Masataka Morita², Hirokazu Kubota², Ryoji Hirabayashi², Ryushi Seo², Nobuaki Nakagawa²

Affiliations

¹ Institute for Drug Discovery Research, Astellas Pharma Inc., 21 Miyukigaoka, Tsukuba, Ibaraki 305-8585, Japan. Electronic address: yuichi.sami@astellas.com.
² Institute for Drug Discovery Research, Astellas Pharma Inc., 21 Miyukigaoka, Tsukuba, Ibaraki 305-8585, Japan.

PMID: 31327678
DOI: 10.1016/j.bmc.2019.05.041

No abstract available

MeSH terms

Administration, Oral
Animals
Dose-Response Relationship, Drug
Drug Discovery*
Female
HEK293 Cells
Humans
Molecular Structure
Piperazines / administration & dosage
Piperazines / chemistry
Piperazines / pharmacology*
Rats
Rats, Inbred Lew
Structure-Activity Relationship
TRPV Cation Channels / antagonists & inhibitors*
TRPV Cation Channels / metabolism

Substances

Piperazines
TRPV Cation Channels
TRPV4 protein, human
Trpv4 protein, rat