Bioorganic and Medicinal Chemistry Letters p. 471 - 475 (2007)
Update date:2022-08-04
Topics:
Choi, Ja Youn
Seo, Han Na
Lee, Min Joo
Park, Seong Jun
Park, Sung Jun
Jeon, Ji Young
Kang, Joo Hi
Pae, Ae Nim
Rhim, Hyewhon
Lee, Jae Yeol
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 μM), was about 5-fold potent (IC50 = 0.26 ± 0.01 μM) for T-type calcium channel (α1G) blocking and its selectivity of T/N-type was also improved (7.5 versus 1.4 of mibefradil).
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