2. Academic Validation
  3. Synthesis and biological evaluation of novel T-type calcium channel blockers

Synthesis and biological evaluation of novel T-type calcium channel blockers

  • Bioorg Med Chem Lett. 2007 Jan 15;17(2):471-5. doi: 10.1016/j.bmcl.2006.10.024.
Ja Youn Choi 1,  Han Na Seo,  Min Joo Lee,  Seong Jun Park,  Sung Jun Park,  Ji Young Jeon,  Joo Hi Kang,  Ae Nim Pae,  Hyewhon Rhim,  Jae Yeol Lee
Affiliations

Affiliation

  • 1 Research Institute for Basic Sciences and Department of Chemistry, College of Sciences, Kyung Hee University, 1 Hoegi-Dong, Seoul 130-701, Republic of Korea.
PMID: 17064894 DOI: 10.1016/j.bmcl.2006.10.024
Abstract

3,4-Dihydroquinazoline analogues substituted by N-methyl-N-(5-pyrrolidinopentyl)amine at the 2-position were synthesized and their blocking effects were evaluated for T- and N-type calcium channels. Compound 11b (KYS05080), compared to mibefradil (IC50=1.34+/-0.49 microM), was about 5-fold potent (IC50=0.26+/-0.01 microM) for T-type calcium channel (alpha1G) blocking and its selectivity of T/N-type was also improved (7.5 versus 1.4 of mibefradil).

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