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10.1021/ml200137x http://scihub22266oqcxt.onion/10.1021/ml200137x C4018089!4018089!24900262     free     free     free Deprecated: Implicit conversion from float 231.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 231.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 231.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 231.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 231.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 Deprecated: Implicit conversion from float 231.6 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534       ACS+Med+Chem+Lett 2011 ; 2 (10): 747-51 Nephropedia Template TP {{tp|p=24900262|t=2011. Discovery of VTP-27999, an Alkyl Amine Renin Inhibitor with Potential for Clinical Utility |pdf=|usr=}}{{24900262}} gab.com Text Discovery of VTP-27999, an Alkyl Amine Renin Inhibitor with Potential for Clinical Utility JO: ACS Med Chem Lett http://www.kidney.de/pget.php?&tw=1&pmid=24900262 #FOAvip Structure guided optimization of a series of nonpeptidic alkyl amine renin inhibitors allowed the rational incorporation of additional polar functionality. Replacement of the cyclohexylmethyl group occupying the S1 pocket with a (R)-(tetrahydropyran-3-yl)methyl group and utilization of a different attachment point led to the identification of clinical candidate 9. This compound demonstrated excellent selectivity over related and unrelated off-targets, >15% oral bioavailability in three species, oral efficacy in a double transgenic rat model of hypertension, and good exposure in humans. Twit Text FOAVip Discovery of VTP-27999, an Alkyl Amine Renin Inhibitor with Potential for Clinical Utility ????ACS Med Chem Lett http://www.kidney.de/pget.php?&tw=1&pmid=24900262 #FOAvip Twit Text # Free Paper on # # # # # LINK http://www.kidney.de/pget.php?&tw=1&pmid=24900262 #FOAvip English Wikipedia <ref>{{Cite pmid|24900262}}</ref> Discovery of VTP-27999, an Alkyl Amine Renin Inhibitor with Potential for Clinical Utility #MMPMID24900262 Jia L; Simpson RD; Yuan J; Xu Z; Zhao W; Cacatian S; Tice CM; Guo J; Ishchenko A; Singh SB; Wu Z; McKeever BM; Bukhtiyarov Y; Johnson JA; Doe CP; Harrison RK; McGeehan GM; Dillard LW; Baldwin JJ; Claremon DA ACS Med Chem Lett 2011[Oct]; 2 (10): 747-51 PMID24900262show ga Structure guided optimization of a series of nonpeptidic alkyl amine renin inhibitors allowed the rational incorporation of additional polar functionality. Replacement of the cyclohexylmethyl group occupying the S1 pocket with a (R)-(tetrahydropyran-3-yl)methyl group and utilization of a different attachment point led to the identification of clinical candidate 9. This compound demonstrated excellent selectivity over related and unrelated off-targets, >15% oral bioavailability in three species, oral efficacy in a double transgenic rat model of hypertension, and good exposure in humans. äDiscovery of VTP-27999, an Alkyl Amine Renin Inhibitor with Potential (epmc).pdf DeepDyve Pubget Overpricing