Optimization of orally bioavailable alkyl amine renin inhibitors
Structure-guided drug design led to new alkylamine renin inhibitors with improved in vitro and in vivo potency. Lead compound 21a, has an IC 50 of 0.83 nM for the inhibition of human renin in plasma (PRA). Oral administration of 21a at 10 mg/kg resulted in >20 h reduction of blood pressure in a d...
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| Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2010-01, Vol.20 (2), p.694-699 |
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| creator | Xu, Zhenrong Cacatian, Salvacion Yuan, Jing Simpson, Robert D. Jia, Lanqi Zhao, Wei Tice, Colin M. Flaherty, Patrick T. Guo, Joan Ishchenko, Alexey Singh, Suresh B. Wu, Zhongren McKeever, Brian M. Scott, Boyd B. Bukhtiyarov, Yuri Berbaum, Jennifer Mason, Jennifer Panemangalore, Reshma Cappiello, Maria Grazia Bentley, Ross Doe, Christopher P. Harrison, Richard K. McGeehan, Gerard M. Dillard, Lawrence W. Baldwin, John J. Claremon, David A. |
| description | Structure-guided drug design led to new alkylamine renin inhibitors with improved in vitro and in vivo potency. Lead compound
21a, has an IC
50 of 0.83
nM for the inhibition of human renin in plasma (PRA). Oral administration of
21a at 10
mg/kg resulted in >20
h reduction of blood pressure in a double transgenic rat model of hypertension. |
| doi_str_mv | 10.1016/j.bmcl.2009.11.066 |
| format | Article |
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21a, has an IC
50 of 0.83
nM for the inhibition of human renin in plasma (PRA). Oral administration of
21a at 10
mg/kg resulted in >20
h reduction of blood pressure in a double transgenic rat model of hypertension.</description><identifier>ISSN: 0960-894X</identifier><identifier>EISSN: 1464-3405</identifier><identifier>DOI: 10.1016/j.bmcl.2009.11.066</identifier><identifier>PMID: 19959358</identifier><language>eng</language><publisher>Amsterdam: Elsevier Ltd</publisher><subject>Administration, Oral ; AMINES ; Amines - chemical synthesis ; Amines - chemistry ; Amines - pharmacokinetics ; Animals ; Antihypertensive agents ; Aspartyl protease ; BASIC BIOLOGICAL SCIENCES ; Binding Sites ; Biological and medical sciences ; BLOOD PRESSURE ; Blood Pressure - drug effects ; Carbamates - chemical synthesis ; Carbamates - chemistry ; Carbamates - pharmacokinetics ; Cardiovascular system ; Crystallography, X-Ray ; DESIGN ; Drug Design ; Enzyme Inhibitors - chemical synthesis ; Enzyme Inhibitors - chemistry ; Enzyme Inhibitors - pharmacokinetics ; GENERAL AND MISCELLANEOUS//MATHEMATICS, COMPUTING, AND INFORMATION SCIENCE ; Haplorhini ; Humans ; HYPERTENSION ; IN VITRO ; IN VIVO ; LEAD COMPOUNDS ; Medical sciences ; OPTIMIZATION ; ORAL ADMINISTRATION ; Pharmacology. Drug treatments ; Piperidines - chemical synthesis ; Piperidines - chemistry ; Piperidines - pharmacokinetics ; PLASMA ; Rats ; Rats, Transgenic ; RENIN ; Renin - antagonists & inhibitors ; Renin - blood ; Renin - metabolism ; Structure-Activity Relationship ; Structure-based drug design ; X-ray crystallography</subject><ispartof>Bioorganic & medicinal chemistry letters, 2010-01, Vol.20 (2), p.694-699</ispartof><rights>2009 Elsevier Ltd</rights><rights>2015 INIST-CNRS</rights><rights>Copyright 2009 Elsevier Ltd. All rights reserved.</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c509t-62aefe1d325cc281ebd89a4b91ebb25407d57ccf6016e677356dfd28eec6e3223</citedby><cites>FETCH-LOGICAL-c509t-62aefe1d325cc281ebd89a4b91ebb25407d57ccf6016e677356dfd28eec6e3223</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://www.sciencedirect.com/science/article/pii/S0960894X09016369$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>230,314,776,780,881,3537,27901,27902,65306</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=22389499$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/19959358$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink><backlink>$$Uhttps://www.osti.gov/biblio/1002629$$D View this record in Osti.gov$$Hfree_for_read</backlink></links><search><creatorcontrib>Xu, Zhenrong</creatorcontrib><creatorcontrib>Cacatian, Salvacion</creatorcontrib><creatorcontrib>Yuan, Jing</creatorcontrib><creatorcontrib>Simpson, Robert D.</creatorcontrib><creatorcontrib>Jia, Lanqi</creatorcontrib><creatorcontrib>Zhao, Wei</creatorcontrib><creatorcontrib>Tice, Colin M.</creatorcontrib><creatorcontrib>Flaherty, Patrick T.</creatorcontrib><creatorcontrib>Guo, Joan</creatorcontrib><creatorcontrib>Ishchenko, Alexey</creatorcontrib><creatorcontrib>Singh, Suresh B.</creatorcontrib><creatorcontrib>Wu, Zhongren</creatorcontrib><creatorcontrib>McKeever, Brian M.</creatorcontrib><creatorcontrib>Scott, Boyd B.</creatorcontrib><creatorcontrib>Bukhtiyarov, Yuri</creatorcontrib><creatorcontrib>Berbaum, Jennifer</creatorcontrib><creatorcontrib>Mason, Jennifer</creatorcontrib><creatorcontrib>Panemangalore, Reshma</creatorcontrib><creatorcontrib>Cappiello, Maria Grazia</creatorcontrib><creatorcontrib>Bentley, Ross</creatorcontrib><creatorcontrib>Doe, Christopher P.</creatorcontrib><creatorcontrib>Harrison, Richard K.</creatorcontrib><creatorcontrib>McGeehan, Gerard M.</creatorcontrib><creatorcontrib>Dillard, Lawrence W.</creatorcontrib><creatorcontrib>Baldwin, John J.</creatorcontrib><creatorcontrib>Claremon, David A.</creatorcontrib><creatorcontrib>Argonne National Lab. (ANL), Argonne, IL (United States). Advanced Photon Source (APS)</creatorcontrib><title>Optimization of orally bioavailable alkyl amine renin inhibitors</title><title>Bioorganic & medicinal chemistry letters</title><addtitle>Bioorg Med Chem Lett</addtitle><description>Structure-guided drug design led to new alkylamine renin inhibitors with improved in vitro and in vivo potency. Lead compound
21a, has an IC
50 of 0.83
nM for the inhibition of human renin in plasma (PRA). Oral administration of
21a at 10
mg/kg resulted in >20
h reduction of blood pressure in a double transgenic rat model of hypertension.</description><subject>Administration, Oral</subject><subject>AMINES</subject><subject>Amines - chemical synthesis</subject><subject>Amines - chemistry</subject><subject>Amines - pharmacokinetics</subject><subject>Animals</subject><subject>Antihypertensive agents</subject><subject>Aspartyl protease</subject><subject>BASIC BIOLOGICAL SCIENCES</subject><subject>Binding Sites</subject><subject>Biological and medical sciences</subject><subject>BLOOD PRESSURE</subject><subject>Blood Pressure - drug effects</subject><subject>Carbamates - chemical synthesis</subject><subject>Carbamates - chemistry</subject><subject>Carbamates - pharmacokinetics</subject><subject>Cardiovascular system</subject><subject>Crystallography, X-Ray</subject><subject>DESIGN</subject><subject>Drug Design</subject><subject>Enzyme Inhibitors - chemical synthesis</subject><subject>Enzyme Inhibitors - chemistry</subject><subject>Enzyme Inhibitors - pharmacokinetics</subject><subject>GENERAL AND MISCELLANEOUS//MATHEMATICS, COMPUTING, AND INFORMATION SCIENCE</subject><subject>Haplorhini</subject><subject>Humans</subject><subject>HYPERTENSION</subject><subject>IN VITRO</subject><subject>IN VIVO</subject><subject>LEAD COMPOUNDS</subject><subject>Medical sciences</subject><subject>OPTIMIZATION</subject><subject>ORAL ADMINISTRATION</subject><subject>Pharmacology. Drug treatments</subject><subject>Piperidines - chemical synthesis</subject><subject>Piperidines - chemistry</subject><subject>Piperidines - pharmacokinetics</subject><subject>PLASMA</subject><subject>Rats</subject><subject>Rats, Transgenic</subject><subject>RENIN</subject><subject>Renin - antagonists & inhibitors</subject><subject>Renin - blood</subject><subject>Renin - metabolism</subject><subject>Structure-Activity Relationship</subject><subject>Structure-based drug design</subject><subject>X-ray crystallography</subject><issn>0960-894X</issn><issn>1464-3405</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2010</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kU2LFDEQhoMo7uzoH_AgjeB66jZJJ-kO7EFZ_IKFvSh4C-l0NVtjOhmTnoXx15tmBr3tqXJ4qipPvYS8YrRhlKn3u2aYnW84pbphrKFKPSEbJpSoW0HlU7KhWtG61-LnBbnMeUcpE1SI5-SCaS11K_sN-XC3X3DGP3bBGKo4VTFZ74_VgNE-WPR28FBZ_-voKztjgCpBwFBhuMcBl5jyC_Jssj7Dy3Pdkh-fP32_-Vrf3n35dvPxtnaS6qVW3MIEbGy5dI73DIax11YMurwGLgXtRtk5N6kiBqrrWqnGaeQ9gFPQct5uyZvT3JgXNNnhAu7exRDALYZRyhXXBXp3gvYp_j5AXsyM2YH3NkA8ZNO1ba-lLGVLrh4lOROi69i6l59Al2LOCSazTzjbdCxLzRqD2Zk1BrPGYBgzJYbS9Po8_TDMMP5vOd-9AG_PgM3O-inZ4DD_44pviU2vQtcnDsppHxDSag7BwYhpFR8jPvaPvwt5pZk</recordid><startdate>20100115</startdate><enddate>20100115</enddate><creator>Xu, Zhenrong</creator><creator>Cacatian, Salvacion</creator><creator>Yuan, Jing</creator><creator>Simpson, Robert D.</creator><creator>Jia, Lanqi</creator><creator>Zhao, Wei</creator><creator>Tice, Colin M.</creator><creator>Flaherty, Patrick T.</creator><creator>Guo, Joan</creator><creator>Ishchenko, Alexey</creator><creator>Singh, Suresh B.</creator><creator>Wu, Zhongren</creator><creator>McKeever, Brian M.</creator><creator>Scott, Boyd B.</creator><creator>Bukhtiyarov, Yuri</creator><creator>Berbaum, Jennifer</creator><creator>Mason, Jennifer</creator><creator>Panemangalore, Reshma</creator><creator>Cappiello, Maria Grazia</creator><creator>Bentley, Ross</creator><creator>Doe, Christopher P.</creator><creator>Harrison, Richard K.</creator><creator>McGeehan, Gerard M.</creator><creator>Dillard, Lawrence W.</creator><creator>Baldwin, John J.</creator><creator>Claremon, David A.</creator><general>Elsevier Ltd</general><general>Elsevier</general><scope>IQODW</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7QO</scope><scope>8FD</scope><scope>FR3</scope><scope>P64</scope><scope>7X8</scope><scope>OTOTI</scope></search><sort><creationdate>20100115</creationdate><title>Optimization of orally bioavailable alkyl amine renin inhibitors</title><author>Xu, Zhenrong ; Cacatian, Salvacion ; Yuan, Jing ; Simpson, Robert D. ; Jia, Lanqi ; Zhao, Wei ; Tice, Colin M. ; Flaherty, Patrick T. ; Guo, Joan ; Ishchenko, Alexey ; Singh, Suresh B. ; Wu, Zhongren ; McKeever, Brian M. ; Scott, Boyd B. ; Bukhtiyarov, Yuri ; Berbaum, Jennifer ; Mason, Jennifer ; Panemangalore, Reshma ; Cappiello, Maria Grazia ; Bentley, Ross ; Doe, Christopher P. ; Harrison, Richard K. ; McGeehan, Gerard M. ; Dillard, Lawrence W. ; Baldwin, John J. ; Claremon, David A.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c509t-62aefe1d325cc281ebd89a4b91ebb25407d57ccf6016e677356dfd28eec6e3223</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2010</creationdate><topic>Administration, Oral</topic><topic>AMINES</topic><topic>Amines - chemical synthesis</topic><topic>Amines - chemistry</topic><topic>Amines - pharmacokinetics</topic><topic>Animals</topic><topic>Antihypertensive agents</topic><topic>Aspartyl protease</topic><topic>BASIC BIOLOGICAL SCIENCES</topic><topic>Binding Sites</topic><topic>Biological and medical sciences</topic><topic>BLOOD PRESSURE</topic><topic>Blood Pressure - drug effects</topic><topic>Carbamates - chemical synthesis</topic><topic>Carbamates - chemistry</topic><topic>Carbamates - pharmacokinetics</topic><topic>Cardiovascular system</topic><topic>Crystallography, X-Ray</topic><topic>DESIGN</topic><topic>Drug Design</topic><topic>Enzyme Inhibitors - chemical synthesis</topic><topic>Enzyme Inhibitors - chemistry</topic><topic>Enzyme Inhibitors - pharmacokinetics</topic><topic>GENERAL AND MISCELLANEOUS//MATHEMATICS, COMPUTING, AND INFORMATION SCIENCE</topic><topic>Haplorhini</topic><topic>Humans</topic><topic>HYPERTENSION</topic><topic>IN VITRO</topic><topic>IN VIVO</topic><topic>LEAD COMPOUNDS</topic><topic>Medical sciences</topic><topic>OPTIMIZATION</topic><topic>ORAL ADMINISTRATION</topic><topic>Pharmacology. 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(ANL), Argonne, IL (United States). Advanced Photon Source (APS)</aucorp><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Optimization of orally bioavailable alkyl amine renin inhibitors</atitle><jtitle>Bioorganic & medicinal chemistry letters</jtitle><addtitle>Bioorg Med Chem Lett</addtitle><date>2010-01-15</date><risdate>2010</risdate><volume>20</volume><issue>2</issue><spage>694</spage><epage>699</epage><pages>694-699</pages><issn>0960-894X</issn><eissn>1464-3405</eissn><abstract>Structure-guided drug design led to new alkylamine renin inhibitors with improved in vitro and in vivo potency. Lead compound
21a, has an IC
50 of 0.83
nM for the inhibition of human renin in plasma (PRA). Oral administration of
21a at 10
mg/kg resulted in >20
h reduction of blood pressure in a double transgenic rat model of hypertension.</abstract><cop>Amsterdam</cop><pub>Elsevier Ltd</pub><pmid>19959358</pmid><doi>10.1016/j.bmcl.2009.11.066</doi><tpages>6</tpages></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0960-894X |
| ispartof | Bioorganic & medicinal chemistry letters, 2010-01, Vol.20 (2), p.694-699 |
| issn | 0960-894X 1464-3405 |
| language | eng |
| recordid | cdi_osti_scitechconnect_1002629 |
| source | MEDLINE; Elsevier ScienceDirect Journals Complete |
| subjects | Administration, Oral AMINES Amines - chemical synthesis Amines - chemistry Amines - pharmacokinetics Animals Antihypertensive agents Aspartyl protease BASIC BIOLOGICAL SCIENCES Binding Sites Biological and medical sciences BLOOD PRESSURE Blood Pressure - drug effects Carbamates - chemical synthesis Carbamates - chemistry Carbamates - pharmacokinetics Cardiovascular system Crystallography, X-Ray DESIGN Drug Design Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacokinetics GENERAL AND MISCELLANEOUS//MATHEMATICS, COMPUTING, AND INFORMATION SCIENCE Haplorhini Humans HYPERTENSION IN VITRO IN VIVO LEAD COMPOUNDS Medical sciences OPTIMIZATION ORAL ADMINISTRATION Pharmacology. Drug treatments Piperidines - chemical synthesis Piperidines - chemistry Piperidines - pharmacokinetics PLASMA Rats Rats, Transgenic RENIN Renin - antagonists & inhibitors Renin - blood Renin - metabolism Structure-Activity Relationship Structure-based drug design X-ray crystallography |
| title | Optimization of orally bioavailable alkyl amine renin inhibitors |
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