119601-29-5

Upstream product

• 110-89-4 piperidine 
• 962-39-0 L-Phenylalanine benzyl ester 
• 503-38-8 trichloromethyl chloroformate 
• 13939-69-0 piperidine carbamoyl chloride 

Downstream Products

• 119601-30-8 N-piperidinocarbonyl-L-phenylalanine 

Relevant academic research and scientific papers

DIOXACYCLOALKANE COMPOUND HAVING RENIN-INHIBITORY ACTIVITY

Dioxacycloalkane compounds of the formula [1] STR1 wherein A is STR2 wherein W is STR3 X is--CO--or--SO 2--; Y is--CH. sub.2--,--O--or--NR 25--; and R 1 is an aralkyl which may be substituted by lower alkoxy;R 2 is a hydrogen atom or a lower alkyl;R 3 is--(CH 2)d-SR 26 or STR4 R. sup.4 and R 5 are each a hydrogen atom or a lower alkyl; and E is--C(R. sup.29)(R 30)--or--CH 2 CH 2--, pharmaceutically acceptable salts thereof, intermediates for producing said compounds, and methods for producing said intermediates. The compounds of the formula [1] have a strong inhibitory activity against renin and show continuous hypotensive action by oral administration. They are useful as hypotensive agents or therapeutic agents for heart failure.

Novel renin inhibitors containing (2S,3S,5S)-2-amino-1-cyclohexyl-6- methyl-3,5-heptanediol fragment as a transition-state mimic at the P1-P1' cleavage site

A series of renin inhibitors containing the (2S,3S,5S)-2-amino-1- cyclohexyl-6-methyl-3,5-heptanediol (2-amino-3,5-anti-diol) fragment as a novel transition-state mimic was synthesized, and their biological activities were evaluated. All of the synthesized compounds containing the 2-amino-3,5- anti-diol fragment at the P1-P1' position showed high in vitro renin- inhibitory activity with IC50 values in the 10-8-10-10 M range, and most of them caused a reduction of blood pressure when administered orally to salt-depleted, conscious marmosets. The inhibitor (29) with the 4- hydroxypiperidine residue at the P4 position showed the highest activity in terms of both potency and duration of the blood pressure-lowering effect.