Design and discovery of new (3S, 5R)-5-[4-(2-chlorophenyl)-2, 2-dimethyl-5-oxopiperazin-1-yl] piperidine-3-carboxamides as potent renin inhibitors
Y Mori, Y Ogawa, A Mochizuki, Y Nakamura… - Bioorganic & medicinal …, 2012 - Elsevier
… In summary, we have described the design and discovery of (3S,5R)-5-[4-(2-chlorophenyl)-2,2-dimethyl-5-oxopiperazin-1-yl]piperidine-3-carboxamides
as new types of renin inhibitors …
as new types of renin inhibitors …
Synthesis and optimization of novel (3S, 5R)-5-(2, 2-dimethyl-5-oxo-4-phenylpiperazin-1-yl) piperidine-3-carboxamides as orally active renin inhibitors
Y Mori, Y Ogawa, A Mochizuki, Y Nakamura… - Bioorganic & medicinal …, 2013 - Elsevier
… These compounds are potent renin inhibitors and have been described previously. The …
methyl (3S,5R)-5-[4-(2-chlorophenyl)-2,2-dimethyl-5-oxopiperazin-1-yl]piperidine-3-carboxylate (…
methyl (3S,5R)-5-[4-(2-chlorophenyl)-2,2-dimethyl-5-oxopiperazin-1-yl]piperidine-3-carboxylate (…
Recent progress on the discovery of non-peptidic direct renin inhibitors for the clinical management of hypertension
F Yokokawa - Expert opinion on drug discovery, 2013 - Taylor & Francis
… (3S,5R)-18 exhibited highly potent activity against renin (IC … potent inhibition of CYP3A4
(IC 50 = 1.3 μM) Citation[45]. Actelion has further designed 3,4-piperidine-based renin inhibitors …
(IC 50 = 1.3 μM) Citation[45]. Actelion has further designed 3,4-piperidine-based renin inhibitors …
Discovery of TAK-272: a novel, potent, and orally active renin inhibitor
Y Imaeda, H Tokuhara, Y Fukase… - ACS Medicinal …, 2016 - ACS Publications
… than its enantiomer 4, measured either in rh-renin assay (IC 50 = … piperidine 3- and 5-positions
is important in determining renin … design of a new series of N-(piperidin-3-yl)pyrimidine-5-…
is important in determining renin … design of a new series of N-(piperidin-3-yl)pyrimidine-5-…
Decades-old renin inhibitors are still struggling to find a niche in antihypertensive therapy. A fleeting look at the old and the promising new molecules
… of renin inhibitors from several decades, the old discovery of peptides … designed (3S,5R)-5-[4-(2-chlorophenyl)-2,2-dimethyl-5-oxopiperazin-1-yl]piperidine-3-carboxamides
as a potent …
as a potent …
Structure-based design of substituted piperidines as a new class of highly efficacious oral direct renin inhibitors
T Ehara, O Irie, T Kosaka, T Kanazawa… - ACS Medicinal …, 2014 - ACS Publications
… This compound showed high in vitro potency toward human renin with … of inhibitors
bearing the core (3S,4S,5R)-4-hydroxy-3,5-… We have independently discovered 3,5-disubstituted …
bearing the core (3S,4S,5R)-4-hydroxy-3,5-… We have independently discovered 3,5-disubstituted …
Discovery of highly potent renin inhibitors potentially interacting with the S3′ subsite of renin
X Sun, X Wen, Y Chen, C Shi, C Gao, Y Wu… - European journal of …, 2015 - Elsevier
… of renin active site for renin inhibitor design, 42 aliskiren derivatives with modified P2′ portion
were designed, … = 0.7–1.1 nM) were found to be 2–3 fold more potent than ariskiren (IC 50 …
were designed, … = 0.7–1.1 nM) were found to be 2–3 fold more potent than ariskiren (IC 50 …
[引用][C] IC50= 16 µM 140 nM 170 nM
JY Hwang, MP Windisch, S Jo, K Kim, S Kong, HC Kim… - Bioorganic & Medicinal …, 2012