Structural hybridization of pyrrolidine-based T-type calcium channel inhibitors and exploration of their analgesic effects in a neuropathic pain model

Woo Seung Son, Kyu Sung Jeong, Sang Min Lim, Ae Nim Pae

Research output: Contribution to journalArticlepeer-review

Abstract

Highly effective and safe drugs for the treatment of neuropathic pain are urgently required and it was shown that blocking T-type calcium channels can be a promising strategy for drug development for neuropathic pain. We have developed pyrrolidine-based T-type calcium channel inhibitors by structural hybridization and subsequent assessment of in vitro activities against Ca v 3.1 and Ca v 3.2 channels. Profiling of in vitro ADME properties of compounds was also carried out. The representative compound 17h showed comparable in vivo efficacy to gabapentin in the SNL model, which indicates T-type calcium channel inhibitors can be developed as effective therapeutics for neuropathic pain.

Original languageEnglish
Pages (from-to)1168-1172
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume29
Issue number10
DOIs
Publication statusPublished - 2019 May 15

Bibliographical note

Funding Information:
This work was supported by the Korea government (MSIP) under the National Research Council of Science & Technology (NST) grant [No. CRC-15-04-KIST ].

Publisher Copyright:
© 2019

All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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