The rational development of small molecule tachykinin NK3 receptor selective antagonists - the utilisation of a dipeptide chemical library in drug design
| Autor: | J.M. Eden, J. Hodgson, P. Boden, Ratcliffe Giles S, Alexander T. McKnight, David Christopher Horwell, Martyn Clive Pritchard, Jenny Raphy, N. Suman-Chauhan, John Hughes, Kenneth G. Meecham, Geoffrey N. Woodruff, William Howson |
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| Rok vydání: | 1994 |
| Předmět: |
Drug
Dipeptide Nk3 receptor Stereochemistry media_common.quotation_subject Organic Chemistry Clinical Biochemistry Pharmaceutical Science Ligand (biochemistry) Biochemistry Combinatorial chemistry Small molecule Chemical library chemistry.chemical_compound chemistry Drug Discovery Molecular Medicine Urea derivatives Molecular Biology IC50 media_common |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 4:1679-1684 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/s0960-894x(00)80360-1 |
| Popis: | Boc(S)Phe(S)PheNH2 (1c) was identified from the biological screening of an in-house dipeptide chemical library as a micromolar NK3 receptor selective ligand (IC50=1150nM). This lead structure has subsequently been developed into a series of potent and selective NK3 receptor antagonists an example of which is the urea derivative Boc(S)Phe(R)αMePheNH(CH2)7NHCOHNH2 (11d, PD157672) (IC50=16nM). |
| Databáze: | OpenAIRE |
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