928006-44-4

Upstream product

• 928006-43-3 N-methyl-5-(pyrrolidin-1-yl)pentan-1-amine 
• 139210-05-2 methyl 3-[2-(phenyliminomethyleneamino)phenyl]acrylate 
• 111-24-0 1,5-dibromo-pentane 
• 139210-05-2 (E)-3-(2-Phenyliminomethyleneamino-phenyl)-acrylic acid methyl ester 
• 954-81-4 N-(5-bromopentyl)phthalimide 
• 928006-41-1 2-(5-(pyrrolidin-1-yl)pentyl)isoindoline-1,3-dione 
• 928006-42-2 t-butyl (5-pyrrolidin-1-ylpentyl)carbamate 
• 71302-71-1 5-(pyrrolidin-1-yl)pentan-1-amine 

Downstream Products

• 928006-46-6 {2-[methyl-(5-pyrrolidin-1-yl-pentyl)-amino]-3-phenyl-3,4-dihydro-quinazolin-4-yl}-acetic acid 

Relevant academic research and scientific papers

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

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).

Synthesis and SAR study of T-type calcium channel blockers. Part II

3,4-Dihydroquinazoline derivatives have been known to be the novel and potent T-type calcium channel blockers. From a systematic variation of 3,4-dihydroquinazoline derivative 5c (KYS05043), plausible SAR results were established. It was revealed that a 5-(dimethylamino)pentylamino group at R 1, a biphenyl group at R2, and a benzyl amido group at R3 in the 3,4-dihydroquinazoline backbone are closely related with the channel selectivity (T/N-type) as well as the potency based on the discovery of 6k (KYS05090).