Identification of novel muscarinic M(3) selective antagonists with a conformationally restricted Hyp-Pro spacer
The identification of potent and selective muscarinic M(3) antagonists that are based on the recently discovered triphenylpropioamide derivative, 1, and have a unique amino acid spacer group is described. The introduction of a hydroxyproline-proline group to the spacer site and the use of a propyl o...
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| Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2003-01, Vol.13 (1), p.57-60 |
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| container_issue | 1 |
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| container_title | Bioorganic & medicinal chemistry letters |
| container_volume | 13 |
| creator | Sagara, Yufu Kimura, Toshifumi Fujikawa, Toru Noguchi, Kazuhito Ohtake, Norikazu |
| description | The identification of potent and selective muscarinic M(3) antagonists that are based on the recently discovered triphenylpropioamide derivative, 1, and have a unique amino acid spacer group is described. The introduction of a hydroxyproline-proline group to the spacer site and the use of a propyl or cyclopropylmethyl group as the piperidine N-substituent led to the discovery of the novel M(3) selective antagonists [8c, 8g; K(i)700-fold, M(2)/M(3)>180-fold], which have a more rigid structure than 1. |
| format | Article |
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| fulltext | fulltext |
| identifier | ISSN: 0960-894X |
| ispartof | Bioorganic & medicinal chemistry letters, 2003-01, Vol.13 (1), p.57-60 |
| issn | 0960-894X |
| language | eng |
| recordid | cdi_proquest_miscellaneous_72873918 |
| source | MEDLINE; Elsevier ScienceDirect Journals |
| subjects | Amides Combinatorial Chemistry Techniques Drug Evaluation, Preclinical Humans Hydroxyproline Molecular Conformation Muscarinic Antagonists - chemistry Muscarinic Antagonists - metabolism Protein Binding Receptor, Muscarinic M3 Receptors, Muscarinic - chemistry Receptors, Muscarinic - metabolism Structure-Activity Relationship |
| title | Identification of novel muscarinic M(3) selective antagonists with a conformationally restricted Hyp-Pro spacer |
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