Author/Authors :
Hee-Kyung Jung، نويسنده , , Munikumar Reddy Doddareddy، نويسنده , , Joo Hwan Cha، نويسنده , , Hyewhon Rhim، نويسنده , , Yong Seo Cho، نويسنده , , Hun Yeong Koh، نويسنده , , Bong Young Jung، نويسنده , , Ae Nim Pae، نويسنده ,
Abstract :
A small molecule library of piperazinylalkylisoxazole derivatives containing about 600 compounds was designed, synthesized and evaluated for blocking effects on T-type Ca2+ channel. Several ligands were identified to possess high inhibitory activity against the T-type Ca2+ channel. The compound 21 with trifluoromethyl substituents at C3-position of phenyl group (R1) and C2-position of phenyl group (R2) showed the highest inhibitory activity with IC50 value of 1.02 μM, which is comparable to that of mibefradil.
