The design and synthesis of potent, selective benzodiazepine sulfonamide bombesin receptor subtype 3 (BRS-3) agonists with an increased barrier of atropisomerization
Bombesin receptor subtype 3 (BRS-3) is an orphan G-protein coupled receptor expressed primarily in the hypothalamus which plays a role in the onset of both diabetes and obesity. We report herein our progress made towards identifying a potent, selective bombesin receptor subtype-3 (BRS-3) agonist rel...
Gespeichert in:
| Veröffentlicht in: | Bioorganic & medicinal chemistry 2012-05, Vol.20 (9), p.2845-2849 |
|---|---|
| Hauptverfasser: | , , , , , , , , , , , , , , , , , , , , , , , , , , , , |
| Format: | Artikel |
| Sprache: | eng |
| Schlagworte: | |
| Online-Zugang: | Volltext |
| Tags: |
Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
|
| container_end_page | 2849 |
|---|---|
| container_issue | 9 |
| container_start_page | 2845 |
| container_title | Bioorganic & medicinal chemistry |
| container_volume | 20 |
| creator | Chobanian, Harry R. Guo, Yan Liu, Ping Lanza, Thomas J. Chioda, Marc Chang, Linda Kelly, Theresa M. Kan, Yanqing Palyha, Oksana Guan, Xiao-Ming Marsh, Donald J. Metzger, Joseph M. Raustad, Katie Wang, Sheng-Ping Strack, Alison M. Gorski, Judith N. Miller, Randy Pang, Jianmei Lyons, Kathy Dragovic, Jasminka Ning, Jian G. Schafer, Wes A. Welch, Christopher J. Gong, Xiaoyi Gao, Ying-Duo Hornak, Viktor Reitman, Marc L. Nargund, Ravi P. Lin, Linus S. |
| description | Bombesin receptor subtype 3 (BRS-3) is an orphan G-protein coupled receptor expressed primarily in the hypothalamus which plays a role in the onset of both diabetes and obesity. We report herein our progress made towards identifying a potent, selective bombesin receptor subtype-3 (BRS-3) agonist related to the previously described MK-77251 Chobanian et al. (2012) that would prevent atropisomerization through the increase of steric bulk at the C-2 position. This would thereby make clinical development of this class of compounds more cost effective by inhibiting racemization which can occur over long periods of time at room/elevated temperature. |
| doi_str_mv | 10.1016/j.bmc.2012.03.029 |
| format | Article |
| fullrecord | <record><control><sourceid>proquest_cross</sourceid><recordid>TN_cdi_proquest_miscellaneous_1014101309</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><els_id>S0968089612002192</els_id><sourcerecordid>1009130244</sourcerecordid><originalsourceid>FETCH-LOGICAL-c440t-d752cc1bf85969cd6f05cec6478bd51d30216bc36070abfaf627911d6f7a58da3</originalsourceid><addsrcrecordid>eNqNkc-O0zAQxiMEYsvCA3ABX5AWiRTbcZxEnGDFP2klJHb3bDn2pHWV2FnbXdS-D-_JVC1wQxyskTW_bz57vqJ4zuiSUSbfbpb9ZJacMr6k1ZLy7kGxYEKKsqo69rBY0E62JW07eVY8SWlDKeWiY4-LM45VtIIvip83ayAWklt5or0laefzGq-JhIHMIYPPb0iCEUx290B68Ptgnd7D7DyQtB2H4PXkLLbC1KPQkwgG5hwidvu8m4FU5OLD9-uyek30KniXciI_XF6jH3HeRNAJLOl1jA7iwVbnGGaXwgTR7XV2wT8tHg16TPDsVM-L208fby6_lFffPn-9fH9VGiFoLm1Tc2NYP7R1Jztj5UBrA0aKpu1tzWxFOZO9qSRtqO4HPUjedIwh1-i6tbo6Ly6Oc-cY7raQsppcMjCO2kPYJoVbF3gq2v0HSjsEuRCIsiNqYkgpwqDm6CYddwgdRkq1URikOgSpaKUwSNS8OI3f9hPYP4rfySHw6gToZPQ4RO2NS3-5usXPtRK5l0du0EHpVUTm9hqdakoZo7xpkHh3JAA3e48ZqGQceAPWYZRZ2eD-8dBfutfG_A</addsrcrecordid><sourcetype>Aggregation Database</sourcetype><iscdi>true</iscdi><recordtype>article</recordtype><pqid>1009130244</pqid></control><display><type>article</type><title>The design and synthesis of potent, selective benzodiazepine sulfonamide bombesin receptor subtype 3 (BRS-3) agonists with an increased barrier of atropisomerization</title><source>MEDLINE</source><source>Elsevier ScienceDirect Journals</source><creator>Chobanian, Harry R. ; Guo, Yan ; Liu, Ping ; Lanza, Thomas J. ; Chioda, Marc ; Chang, Linda ; Kelly, Theresa M. ; Kan, Yanqing ; Palyha, Oksana ; Guan, Xiao-Ming ; Marsh, Donald J. ; Metzger, Joseph M. ; Raustad, Katie ; Wang, Sheng-Ping ; Strack, Alison M. ; Gorski, Judith N. ; Miller, Randy ; Pang, Jianmei ; Lyons, Kathy ; Dragovic, Jasminka ; Ning, Jian G. ; Schafer, Wes A. ; Welch, Christopher J. ; Gong, Xiaoyi ; Gao, Ying-Duo ; Hornak, Viktor ; Reitman, Marc L. ; Nargund, Ravi P. ; Lin, Linus S.</creator><creatorcontrib>Chobanian, Harry R. ; Guo, Yan ; Liu, Ping ; Lanza, Thomas J. ; Chioda, Marc ; Chang, Linda ; Kelly, Theresa M. ; Kan, Yanqing ; Palyha, Oksana ; Guan, Xiao-Ming ; Marsh, Donald J. ; Metzger, Joseph M. ; Raustad, Katie ; Wang, Sheng-Ping ; Strack, Alison M. ; Gorski, Judith N. ; Miller, Randy ; Pang, Jianmei ; Lyons, Kathy ; Dragovic, Jasminka ; Ning, Jian G. ; Schafer, Wes A. ; Welch, Christopher J. ; Gong, Xiaoyi ; Gao, Ying-Duo ; Hornak, Viktor ; Reitman, Marc L. ; Nargund, Ravi P. ; Lin, Linus S.</creatorcontrib><description>Bombesin receptor subtype 3 (BRS-3) is an orphan G-protein coupled receptor expressed primarily in the hypothalamus which plays a role in the onset of both diabetes and obesity. We report herein our progress made towards identifying a potent, selective bombesin receptor subtype-3 (BRS-3) agonist related to the previously described MK-77251 Chobanian et al. (2012) that would prevent atropisomerization through the increase of steric bulk at the C-2 position. This would thereby make clinical development of this class of compounds more cost effective by inhibiting racemization which can occur over long periods of time at room/elevated temperature.</description><identifier>ISSN: 0968-0896</identifier><identifier>EISSN: 1464-3391</identifier><identifier>DOI: 10.1016/j.bmc.2012.03.029</identifier><identifier>PMID: 22494842</identifier><language>eng</language><publisher>Amsterdam: Elsevier Ltd</publisher><subject>Agonist ; agonists ; Animals ; Atropisomerism ; Benzodiazepine ; Benzodiazepine sulfonamide ; Benzodiazepines - chemistry ; Biological and medical sciences ; Bombesin ; Bombesin receptor subtype-3 (BRS-3) ; bombesin receptors ; chemistry ; cost effectiveness ; diabetes ; Diabetes mellitus ; Drug Design ; G protein-coupled receptors ; Gabaergic and benzodiazepinic system ; Humans ; hypothalamus ; Medical sciences ; Mice ; Neuropharmacology ; Neurotransmitters. Neurotransmission. Receptors ; Obesity ; Pharmacology. Drug treatments ; Protein Binding ; Racemization ; Rats ; Receptors, Bombesin - agonists ; Receptors, Bombesin - metabolism ; Stereoisomerism ; Sulfonamides ; Sulfonamides - chemical synthesis ; Sulfonamides - chemistry ; Sulfonamides - pharmacokinetics ; Temperature ; Temperature effects</subject><ispartof>Bioorganic & medicinal chemistry, 2012-05, Vol.20 (9), p.2845-2849</ispartof><rights>2012 Elsevier Ltd</rights><rights>2015 INIST-CNRS</rights><rights>Copyright © 2012 Elsevier Ltd. All rights reserved.</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c440t-d752cc1bf85969cd6f05cec6478bd51d30216bc36070abfaf627911d6f7a58da3</citedby><cites>FETCH-LOGICAL-c440t-d752cc1bf85969cd6f05cec6478bd51d30216bc36070abfaf627911d6f7a58da3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://www.sciencedirect.com/science/article/pii/S0968089612002192$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,776,780,3537,27901,27902,65306</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=25862786$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/22494842$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Chobanian, Harry R.</creatorcontrib><creatorcontrib>Guo, Yan</creatorcontrib><creatorcontrib>Liu, Ping</creatorcontrib><creatorcontrib>Lanza, Thomas J.</creatorcontrib><creatorcontrib>Chioda, Marc</creatorcontrib><creatorcontrib>Chang, Linda</creatorcontrib><creatorcontrib>Kelly, Theresa M.</creatorcontrib><creatorcontrib>Kan, Yanqing</creatorcontrib><creatorcontrib>Palyha, Oksana</creatorcontrib><creatorcontrib>Guan, Xiao-Ming</creatorcontrib><creatorcontrib>Marsh, Donald J.</creatorcontrib><creatorcontrib>Metzger, Joseph M.</creatorcontrib><creatorcontrib>Raustad, Katie</creatorcontrib><creatorcontrib>Wang, Sheng-Ping</creatorcontrib><creatorcontrib>Strack, Alison M.</creatorcontrib><creatorcontrib>Gorski, Judith N.</creatorcontrib><creatorcontrib>Miller, Randy</creatorcontrib><creatorcontrib>Pang, Jianmei</creatorcontrib><creatorcontrib>Lyons, Kathy</creatorcontrib><creatorcontrib>Dragovic, Jasminka</creatorcontrib><creatorcontrib>Ning, Jian G.</creatorcontrib><creatorcontrib>Schafer, Wes A.</creatorcontrib><creatorcontrib>Welch, Christopher J.</creatorcontrib><creatorcontrib>Gong, Xiaoyi</creatorcontrib><creatorcontrib>Gao, Ying-Duo</creatorcontrib><creatorcontrib>Hornak, Viktor</creatorcontrib><creatorcontrib>Reitman, Marc L.</creatorcontrib><creatorcontrib>Nargund, Ravi P.</creatorcontrib><creatorcontrib>Lin, Linus S.</creatorcontrib><title>The design and synthesis of potent, selective benzodiazepine sulfonamide bombesin receptor subtype 3 (BRS-3) agonists with an increased barrier of atropisomerization</title><title>Bioorganic & medicinal chemistry</title><addtitle>Bioorg Med Chem</addtitle><description>Bombesin receptor subtype 3 (BRS-3) is an orphan G-protein coupled receptor expressed primarily in the hypothalamus which plays a role in the onset of both diabetes and obesity. We report herein our progress made towards identifying a potent, selective bombesin receptor subtype-3 (BRS-3) agonist related to the previously described MK-77251 Chobanian et al. (2012) that would prevent atropisomerization through the increase of steric bulk at the C-2 position. This would thereby make clinical development of this class of compounds more cost effective by inhibiting racemization which can occur over long periods of time at room/elevated temperature.</description><subject>Agonist</subject><subject>agonists</subject><subject>Animals</subject><subject>Atropisomerism</subject><subject>Benzodiazepine</subject><subject>Benzodiazepine sulfonamide</subject><subject>Benzodiazepines - chemistry</subject><subject>Biological and medical sciences</subject><subject>Bombesin</subject><subject>Bombesin receptor subtype-3 (BRS-3)</subject><subject>bombesin receptors</subject><subject>chemistry</subject><subject>cost effectiveness</subject><subject>diabetes</subject><subject>Diabetes mellitus</subject><subject>Drug Design</subject><subject>G protein-coupled receptors</subject><subject>Gabaergic and benzodiazepinic system</subject><subject>Humans</subject><subject>hypothalamus</subject><subject>Medical sciences</subject><subject>Mice</subject><subject>Neuropharmacology</subject><subject>Neurotransmitters. Neurotransmission. Receptors</subject><subject>Obesity</subject><subject>Pharmacology. Drug treatments</subject><subject>Protein Binding</subject><subject>Racemization</subject><subject>Rats</subject><subject>Receptors, Bombesin - agonists</subject><subject>Receptors, Bombesin - metabolism</subject><subject>Stereoisomerism</subject><subject>Sulfonamides</subject><subject>Sulfonamides - chemical synthesis</subject><subject>Sulfonamides - chemistry</subject><subject>Sulfonamides - pharmacokinetics</subject><subject>Temperature</subject><subject>Temperature effects</subject><issn>0968-0896</issn><issn>1464-3391</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2012</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqNkc-O0zAQxiMEYsvCA3ABX5AWiRTbcZxEnGDFP2klJHb3bDn2pHWV2FnbXdS-D-_JVC1wQxyskTW_bz57vqJ4zuiSUSbfbpb9ZJacMr6k1ZLy7kGxYEKKsqo69rBY0E62JW07eVY8SWlDKeWiY4-LM45VtIIvip83ayAWklt5or0laefzGq-JhIHMIYPPb0iCEUx290B68Ptgnd7D7DyQtB2H4PXkLLbC1KPQkwgG5hwidvu8m4FU5OLD9-uyek30KniXciI_XF6jH3HeRNAJLOl1jA7iwVbnGGaXwgTR7XV2wT8tHg16TPDsVM-L208fby6_lFffPn-9fH9VGiFoLm1Tc2NYP7R1Jztj5UBrA0aKpu1tzWxFOZO9qSRtqO4HPUjedIwh1-i6tbo6Ly6Oc-cY7raQsppcMjCO2kPYJoVbF3gq2v0HSjsEuRCIsiNqYkgpwqDm6CYddwgdRkq1URikOgSpaKUwSNS8OI3f9hPYP4rfySHw6gToZPQ4RO2NS3-5usXPtRK5l0du0EHpVUTm9hqdakoZo7xpkHh3JAA3e48ZqGQceAPWYZRZ2eD-8dBfutfG_A</recordid><startdate>20120501</startdate><enddate>20120501</enddate><creator>Chobanian, Harry R.</creator><creator>Guo, Yan</creator><creator>Liu, Ping</creator><creator>Lanza, Thomas J.</creator><creator>Chioda, Marc</creator><creator>Chang, Linda</creator><creator>Kelly, Theresa M.</creator><creator>Kan, Yanqing</creator><creator>Palyha, Oksana</creator><creator>Guan, Xiao-Ming</creator><creator>Marsh, Donald J.</creator><creator>Metzger, Joseph M.</creator><creator>Raustad, Katie</creator><creator>Wang, Sheng-Ping</creator><creator>Strack, Alison M.</creator><creator>Gorski, Judith N.</creator><creator>Miller, Randy</creator><creator>Pang, Jianmei</creator><creator>Lyons, Kathy</creator><creator>Dragovic, Jasminka</creator><creator>Ning, Jian G.</creator><creator>Schafer, Wes A.</creator><creator>Welch, Christopher J.</creator><creator>Gong, Xiaoyi</creator><creator>Gao, Ying-Duo</creator><creator>Hornak, Viktor</creator><creator>Reitman, Marc L.</creator><creator>Nargund, Ravi P.</creator><creator>Lin, Linus S.</creator><general>Elsevier Ltd</general><general>Elsevier</general><scope>FBQ</scope><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>7X8</scope><scope>7QO</scope><scope>8FD</scope><scope>FR3</scope><scope>P64</scope></search><sort><creationdate>20120501</creationdate><title>The design and synthesis of potent, selective benzodiazepine sulfonamide bombesin receptor subtype 3 (BRS-3) agonists with an increased barrier of atropisomerization</title><author>Chobanian, Harry R. ; Guo, Yan ; Liu, Ping ; Lanza, Thomas J. ; Chioda, Marc ; Chang, Linda ; Kelly, Theresa M. ; Kan, Yanqing ; Palyha, Oksana ; Guan, Xiao-Ming ; Marsh, Donald J. ; Metzger, Joseph M. ; Raustad, Katie ; Wang, Sheng-Ping ; Strack, Alison M. ; Gorski, Judith N. ; Miller, Randy ; Pang, Jianmei ; Lyons, Kathy ; Dragovic, Jasminka ; Ning, Jian G. ; Schafer, Wes A. ; Welch, Christopher J. ; Gong, Xiaoyi ; Gao, Ying-Duo ; Hornak, Viktor ; Reitman, Marc L. ; Nargund, Ravi P. ; Lin, Linus S.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c440t-d752cc1bf85969cd6f05cec6478bd51d30216bc36070abfaf627911d6f7a58da3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2012</creationdate><topic>Agonist</topic><topic>agonists</topic><topic>Animals</topic><topic>Atropisomerism</topic><topic>Benzodiazepine</topic><topic>Benzodiazepine sulfonamide</topic><topic>Benzodiazepines - chemistry</topic><topic>Biological and medical sciences</topic><topic>Bombesin</topic><topic>Bombesin receptor subtype-3 (BRS-3)</topic><topic>bombesin receptors</topic><topic>chemistry</topic><topic>cost effectiveness</topic><topic>diabetes</topic><topic>Diabetes mellitus</topic><topic>Drug Design</topic><topic>G protein-coupled receptors</topic><topic>Gabaergic and benzodiazepinic system</topic><topic>Humans</topic><topic>hypothalamus</topic><topic>Medical sciences</topic><topic>Mice</topic><topic>Neuropharmacology</topic><topic>Neurotransmitters. Neurotransmission. Receptors</topic><topic>Obesity</topic><topic>Pharmacology. Drug treatments</topic><topic>Protein Binding</topic><topic>Racemization</topic><topic>Rats</topic><topic>Receptors, Bombesin - agonists</topic><topic>Receptors, Bombesin - metabolism</topic><topic>Stereoisomerism</topic><topic>Sulfonamides</topic><topic>Sulfonamides - chemical synthesis</topic><topic>Sulfonamides - chemistry</topic><topic>Sulfonamides - pharmacokinetics</topic><topic>Temperature</topic><topic>Temperature effects</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Chobanian, Harry R.</creatorcontrib><creatorcontrib>Guo, Yan</creatorcontrib><creatorcontrib>Liu, Ping</creatorcontrib><creatorcontrib>Lanza, Thomas J.</creatorcontrib><creatorcontrib>Chioda, Marc</creatorcontrib><creatorcontrib>Chang, Linda</creatorcontrib><creatorcontrib>Kelly, Theresa M.</creatorcontrib><creatorcontrib>Kan, Yanqing</creatorcontrib><creatorcontrib>Palyha, Oksana</creatorcontrib><creatorcontrib>Guan, Xiao-Ming</creatorcontrib><creatorcontrib>Marsh, Donald J.</creatorcontrib><creatorcontrib>Metzger, Joseph M.</creatorcontrib><creatorcontrib>Raustad, Katie</creatorcontrib><creatorcontrib>Wang, Sheng-Ping</creatorcontrib><creatorcontrib>Strack, Alison M.</creatorcontrib><creatorcontrib>Gorski, Judith N.</creatorcontrib><creatorcontrib>Miller, Randy</creatorcontrib><creatorcontrib>Pang, Jianmei</creatorcontrib><creatorcontrib>Lyons, Kathy</creatorcontrib><creatorcontrib>Dragovic, Jasminka</creatorcontrib><creatorcontrib>Ning, Jian G.</creatorcontrib><creatorcontrib>Schafer, Wes A.</creatorcontrib><creatorcontrib>Welch, Christopher J.</creatorcontrib><creatorcontrib>Gong, Xiaoyi</creatorcontrib><creatorcontrib>Gao, Ying-Duo</creatorcontrib><creatorcontrib>Hornak, Viktor</creatorcontrib><creatorcontrib>Reitman, Marc L.</creatorcontrib><creatorcontrib>Nargund, Ravi P.</creatorcontrib><creatorcontrib>Lin, Linus S.</creatorcontrib><collection>AGRIS</collection><collection>Pascal-Francis</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><collection>Biotechnology Research Abstracts</collection><collection>Technology Research Database</collection><collection>Engineering Research Database</collection><collection>Biotechnology and BioEngineering Abstracts</collection><jtitle>Bioorganic & medicinal chemistry</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Chobanian, Harry R.</au><au>Guo, Yan</au><au>Liu, Ping</au><au>Lanza, Thomas J.</au><au>Chioda, Marc</au><au>Chang, Linda</au><au>Kelly, Theresa M.</au><au>Kan, Yanqing</au><au>Palyha, Oksana</au><au>Guan, Xiao-Ming</au><au>Marsh, Donald J.</au><au>Metzger, Joseph M.</au><au>Raustad, Katie</au><au>Wang, Sheng-Ping</au><au>Strack, Alison M.</au><au>Gorski, Judith N.</au><au>Miller, Randy</au><au>Pang, Jianmei</au><au>Lyons, Kathy</au><au>Dragovic, Jasminka</au><au>Ning, Jian G.</au><au>Schafer, Wes A.</au><au>Welch, Christopher J.</au><au>Gong, Xiaoyi</au><au>Gao, Ying-Duo</au><au>Hornak, Viktor</au><au>Reitman, Marc L.</au><au>Nargund, Ravi P.</au><au>Lin, Linus S.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>The design and synthesis of potent, selective benzodiazepine sulfonamide bombesin receptor subtype 3 (BRS-3) agonists with an increased barrier of atropisomerization</atitle><jtitle>Bioorganic & medicinal chemistry</jtitle><addtitle>Bioorg Med Chem</addtitle><date>2012-05-01</date><risdate>2012</risdate><volume>20</volume><issue>9</issue><spage>2845</spage><epage>2849</epage><pages>2845-2849</pages><issn>0968-0896</issn><eissn>1464-3391</eissn><abstract>Bombesin receptor subtype 3 (BRS-3) is an orphan G-protein coupled receptor expressed primarily in the hypothalamus which plays a role in the onset of both diabetes and obesity. We report herein our progress made towards identifying a potent, selective bombesin receptor subtype-3 (BRS-3) agonist related to the previously described MK-77251 Chobanian et al. (2012) that would prevent atropisomerization through the increase of steric bulk at the C-2 position. This would thereby make clinical development of this class of compounds more cost effective by inhibiting racemization which can occur over long periods of time at room/elevated temperature.</abstract><cop>Amsterdam</cop><pub>Elsevier Ltd</pub><pmid>22494842</pmid><doi>10.1016/j.bmc.2012.03.029</doi><tpages>5</tpages></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0968-0896 |
| ispartof | Bioorganic & medicinal chemistry, 2012-05, Vol.20 (9), p.2845-2849 |
| issn | 0968-0896 1464-3391 |
| language | eng |
| recordid | cdi_proquest_miscellaneous_1014101309 |
| source | MEDLINE; Elsevier ScienceDirect Journals |
| subjects | Agonist agonists Animals Atropisomerism Benzodiazepine Benzodiazepine sulfonamide Benzodiazepines - chemistry Biological and medical sciences Bombesin Bombesin receptor subtype-3 (BRS-3) bombesin receptors chemistry cost effectiveness diabetes Diabetes mellitus Drug Design G protein-coupled receptors Gabaergic and benzodiazepinic system Humans hypothalamus Medical sciences Mice Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Obesity Pharmacology. Drug treatments Protein Binding Racemization Rats Receptors, Bombesin - agonists Receptors, Bombesin - metabolism Stereoisomerism Sulfonamides Sulfonamides - chemical synthesis Sulfonamides - chemistry Sulfonamides - pharmacokinetics Temperature Temperature effects |
| title | The design and synthesis of potent, selective benzodiazepine sulfonamide bombesin receptor subtype 3 (BRS-3) agonists with an increased barrier of atropisomerization |
| url | https://sfx.bib-bvb.de/sfx_tum?ctx_ver=Z39.88-2004&ctx_enc=info:ofi/enc:UTF-8&ctx_tim=2025-02-08T10%3A41%3A17IST&url_ver=Z39.88-2004&url_ctx_fmt=infofi/fmt:kev:mtx:ctx&rfr_id=info:sid/primo.exlibrisgroup.com:primo3-Article-proquest_cross&rft_val_fmt=info:ofi/fmt:kev:mtx:journal&rft.genre=article&rft.atitle=The%20design%20and%20synthesis%20of%20potent,%20selective%20benzodiazepine%20sulfonamide%20bombesin%20receptor%20subtype%203%20(BRS-3)%20agonists%20with%20an%20increased%20barrier%20of%20atropisomerization&rft.jtitle=Bioorganic%20&%20medicinal%20chemistry&rft.au=Chobanian,%20Harry%20R.&rft.date=2012-05-01&rft.volume=20&rft.issue=9&rft.spage=2845&rft.epage=2849&rft.pages=2845-2849&rft.issn=0968-0896&rft.eissn=1464-3391&rft_id=info:doi/10.1016/j.bmc.2012.03.029&rft_dat=%3Cproquest_cross%3E1009130244%3C/proquest_cross%3E%3Curl%3E%3C/url%3E&disable_directlink=true&sfx.directlink=off&sfx.report_link=0&rft_id=info:oai/&rft_pqid=1009130244&rft_id=info:pmid/22494842&rft_els_id=S0968089612002192&rfr_iscdi=true |