Highly potent and selective cannabinoid receptor 2 agonists: Initial hit optimization of an adamantyl hit series identified from high-through-put screening
A series of highly potent & selective adamantane derived CB2 agonists was identified in a high-throughput screen. A SAR was established and physicochemical properties were significantly improved. This was accompanied by potency of the compounds on the Q63R variant and varying β-arrestin data whi...
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| Published in | Bioorganic & medicinal chemistry letters Vol. 23; no. 5; pp. 1177 - 1181 |
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| Main Authors | , , , , , , , , , , |
| Format | Journal Article |
| Language | English |
| Published |
OXFORD
Elsevier Ltd
01.03.2013
Elsevier |
| Subjects | |
| Online Access | Get full text |
| ISSN | 0960-894X 1464-3405 1464-3405 |
| DOI | 10.1016/j.bmcl.2013.01.044 |
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| Abstract | A series of highly potent & selective adamantane derived CB2 agonists was identified in a high-throughput screen. A SAR was established and physicochemical properties were significantly improved. This was accompanied by potency of the compounds on the Q63R variant and varying β-arrestin data which will support the insight into their relevance for the in vivo situation. |
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| AbstractList | A series of highly potent & selective adamantane derived CB2 agonists was identified in a high-throughput screen. A SAR was established and physicochemical properties were significantly improved. This was accompanied by potency of the compounds on the Q63R variant and varying β-arrestin data which will support the insight into their relevance for the in vivo situation. A series of highly potent & selective adamantane derived CB2 agonists was identified in a high-throughput screen. A SAR was established and physicochemical properties were significantly improved. This was accompanied by potency of the compounds on the Q63R variant and varying β-arrestin data which will support the insight into their relevance for the in vivo situation.A series of highly potent & selective adamantane derived CB2 agonists was identified in a high-throughput screen. A SAR was established and physicochemical properties were significantly improved. This was accompanied by potency of the compounds on the Q63R variant and varying β-arrestin data which will support the insight into their relevance for the in vivo situation. A series of highly potent & selective adamantane derived CB2 agonists was identified in a high-through-put screen. A SAR was established and physicochemical properties were significantly improved. This was accompanied by potency of the compounds on the Q63R variant and varying beta-arrestin data which will support the insight into their relevance for the in vivo situation. (C) 2013 Elsevier Ltd. All rights reserved. |
| Author | Röver, Stephan Schuler, Franz Fingerle, Jürgen Kimbara, Atsushi Rogers-Evans, Mark Grether, Uwe Nettekoven, Matthias Püllmann, Bernd Ullmer, Christoph Grüner, Sabine Schulz-Gasch, Tanja |
| Author_xml | – sequence: 1 givenname: Matthias surname: Nettekoven fullname: Nettekoven, Matthias email: matthias.nettekoven@roche.com organization: F. Hoffmann-La Roche Ltd, Pharma Research & Early Development, Medicinal Chemistry, Grenzacher Str. 124, 4070 Basel, Switzerland – sequence: 2 givenname: Jürgen surname: Fingerle fullname: Fingerle, Jürgen organization: F. Hoffmann-La Roche Ltd, Pharma Research & Early Development, Discovery Biology, Grenzacher Str. 124, 4070 Basel, Switzerland – sequence: 3 givenname: Uwe surname: Grether fullname: Grether, Uwe organization: F. Hoffmann-La Roche Ltd, Pharma Research & Early Development, Medicinal Chemistry, Grenzacher Str. 124, 4070 Basel, Switzerland – sequence: 4 givenname: Sabine surname: Grüner fullname: Grüner, Sabine organization: F. Hoffmann-La Roche Ltd, Pharma Research & Early Development, Discovery Biology, Grenzacher Str. 124, 4070 Basel, Switzerland – sequence: 5 givenname: Atsushi surname: Kimbara fullname: Kimbara, Atsushi organization: F. Hoffmann-La Roche Ltd, Pharma Research & Early Development, Medicinal Chemistry, Grenzacher Str. 124, 4070 Basel, Switzerland – sequence: 6 givenname: Bernd surname: Püllmann fullname: Püllmann, Bernd organization: F. Hoffmann-La Roche Ltd, Pharma Research & Early Development, Medicinal Chemistry, Grenzacher Str. 124, 4070 Basel, Switzerland – sequence: 7 givenname: Mark surname: Rogers-Evans fullname: Rogers-Evans, Mark organization: F. Hoffmann-La Roche Ltd, Pharma Research & Early Development, Medicinal Chemistry, Grenzacher Str. 124, 4070 Basel, Switzerland – sequence: 8 givenname: Stephan surname: Röver fullname: Röver, Stephan organization: F. Hoffmann-La Roche Ltd, Pharma Research & Early Development, Medicinal Chemistry, Grenzacher Str. 124, 4070 Basel, Switzerland – sequence: 9 givenname: Franz surname: Schuler fullname: Schuler, Franz organization: F. Hoffmann-La Roche Ltd, Pharma Research & Early Development, DMPK, Grenzacher Str. 124, 4070 Basel, Switzerland – sequence: 10 givenname: Tanja surname: Schulz-Gasch fullname: Schulz-Gasch, Tanja organization: F. Hoffmann-La Roche Ltd, Pharma Research & Early Development, Medicinal Chemistry, Grenzacher Str. 124, 4070 Basel, Switzerland – sequence: 11 givenname: Christoph surname: Ullmer fullname: Ullmer, Christoph organization: F. Hoffmann-La Roche Ltd, Pharma Research & Early Development, Discovery Biology, Grenzacher Str. 124, 4070 Basel, Switzerland |
| BackLink | https://www.ncbi.nlm.nih.gov/pubmed/23380378$$D View this record in MEDLINE/PubMed |
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| Keywords | β-Arrestin Adamantane Cannabinoid receptor Hit optimization TARGET DRUG DISCOVERY ENDOCANNABINOID SYSTEM CB2 RECEPTORS DISEASES LIGANDS ABSORPTION beta-Arrestin MODULATION PERMEATION INDEXES |
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| Snippet | A series of highly potent & selective adamantane derived CB2 agonists was identified in a high-throughput screen. A SAR was established and physicochemical... A series of highly potent & selective adamantane derived CB2 agonists was identified in a high-through-put screen. A SAR was established and physicochemical... |
| Source | Web of Science |
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| StartPage | 1177 |
| SubjectTerms | Adamantane Adamantane - analogs & derivatives Adamantane - pharmacology agonists Cannabinoid receptor Cannabinoid Receptor Agonists - chemistry Cannabinoid Receptor Agonists - pharmacology cannabinoids Chemistry Chemistry, Medicinal Chemistry, Organic Drug Evaluation, Preclinical - methods High-Throughput Screening Assays - methods Hit optimization Humans Life Sciences & Biomedicine Models, Molecular Pharmacology & Pharmacy Physical Sciences physicochemical properties Receptor, Cannabinoid, CB2 - agonists Science & Technology screening Structure-Activity Relationship β-Arrestin |
| Title | Highly potent and selective cannabinoid receptor 2 agonists: Initial hit optimization of an adamantyl hit series identified from high-through-put screening |
| URI | https://dx.doi.org/10.1016/j.bmcl.2013.01.044 http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcApp=Summon&SrcAuth=ProQuest&DestApp=WOS&DestLinkType=FullRecord&UT=000314693400003 https://www.ncbi.nlm.nih.gov/pubmed/23380378 https://www.proquest.com/docview/1288312370 https://www.proquest.com/docview/1678566273 |
| Volume | 23 |
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