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10.1021/acsmedchemlett.6b00251 http://scihub22266oqcxt.onion/10.1021/acsmedchemlett.6b00251 C5066151!5066151!27774132     free     free     free Deprecated: Implicit conversion from float 235.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 235.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 235.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534       ACS+Med+Chem+Lett 2016 ; 7 (10): 933-8 Nephropedia Template TP {{tp|p=27774132|t=2016. Discovery of TAK-272: A Novel, Potent, and Orally Active Renin Inhibitor |pdf=|usr=}}{{27774132}} gab.com Text Discovery of TAK-272: A Novel, Potent, and Orally Active Renin Inhibitor JO: ACS Med Chem Lett http://www.kidney.de/pget.php?&tw=1&pmid=27774132 #FOAvip The aspartic proteinase renin is an attractive target for the treatment of hypertension and cardiovascular/renal disease such as chronic kidney disease and heart failure. We introduced an S1? site binder into the lead compound 1 guided by structure-based drug design (SBDD), and further optimization of physicochemical properties led to the discovery of benzimidazole derivative 10 (1-(4-methoxybutyl)-N-(2-methylpropyl)-N-[(3S,5R)-5-(morpholin-4-yl)carbonylpiper idin-3-yl]-1H-benzimidazole-2-carboxamide hydrochloride, TAK-272) as a highly potent and orally active renin inhibitor. Compound 10 demonstrated good oral bioavailability (BA) and long-lasting efficacy in rats. Compound 10 is currently in clinical trials. Twit Text FOAVip Discovery of TAK-272: A Novel, Potent, and Orally Active Renin Inhibitor ????ACS Med Chem Lett http://www.kidney.de/pget.php?&tw=1&pmid=27774132 #FOAvip Twit Text # Free Paper on # # # # # LINK http://www.kidney.de/pget.php?&tw=1&pmid=27774132 #FOAvip English Wikipedia <ref>{{Cite pmid|27774132}}</ref> Discovery of TAK-272: A Novel, Potent, and Orally Active Renin Inhibitor #MMPMID27774132 Imaeda Y; Tokuhara H; Fukase Y; Kanagawa R; Kajimoto Y; Kusumoto K; Kondo M; Snell G; Behnke C; Kuroita T ACS Med Chem Lett 2016[Oct]; 7 (10): 933-8 PMID27774132show ga The aspartic proteinase renin is an attractive target for the treatment of hypertension and cardiovascular/renal disease such as chronic kidney disease and heart failure. We introduced an S1? site binder into the lead compound 1 guided by structure-based drug design (SBDD), and further optimization of physicochemical properties led to the discovery of benzimidazole derivative 10 (1-(4-methoxybutyl)-N-(2-methylpropyl)-N-[(3S,5R)-5-(morpholin-4-yl)carbonylpiper idin-3-yl]-1H-benzimidazole-2-carboxamide hydrochloride, TAK-272) as a highly potent and orally active renin inhibitor. Compound 10 demonstrated good oral bioavailability (BA) and long-lasting efficacy in rats. Compound 10 is currently in clinical trials. äDiscovery of TAK-272: A Novel, Potent, and Orally Active Renin Inhibit(epmc).pdf DeepDyve Pubget Overpricing