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From libraries to candidate: The discovery of new ultra long-acting dibasic β2-adrenoceptor agonists
Libraries of dibasic compounds designed around the molecular scaffold of the DA2/β2 dual agonist sibenadet (Viozan™) have yielded a number of promising starting points that have been further optimised into novel potent and selective target molecules with required pharmacokinetic properties. From a s...
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| Published in: | Bioorganic & medicinal chemistry letters 2012-01, Vol.22 (1), p.689-695 |
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| Main Authors: | , , , , , , , , , , , , , , , , |
| Format: | Article |
| Language: | English |
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| cited_by | cdi_FETCH-LOGICAL-c2546-9750592cb80c2d712c0b0a2dffb7a7752a8b160ed3138a82169aa9863392cb773 |
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| cites | cdi_FETCH-LOGICAL-c2546-9750592cb80c2d712c0b0a2dffb7a7752a8b160ed3138a82169aa9863392cb773 |
| container_end_page | 695 |
| container_issue | 1 |
| container_start_page | 689 |
| container_title | Bioorganic & medicinal chemistry letters |
| container_volume | 22 |
| creator | Alcaraz, Lilian Bailey, Andrew Cadogan, Elaine Connolly, Stephen Jewell, Robert Jordan, Stephen Kindon, Nicholas Lister, Andrew Lawson, Mandy Mullen, Alexander Dainty, Ian Nicholls, David Paine, Stuart Pairaudeau, Garry Stocks, Michael J. Thorne, Phillip Young, Alan |
| description | Libraries of dibasic compounds designed around the molecular scaffold of the DA2/β2 dual agonist sibenadet (Viozan™) have yielded a number of promising starting points that have been further optimised into novel potent and selective target molecules with required pharmacokinetic properties. From a shortlist, 31 was discovered as a novel, high potency, and highly efficacious β2-agonist with high selectivity and a duration of action commensurable with once daily dosing. |
| doi_str_mv | 10.1016/j.bmcl.2011.10.049 |
| format | article |
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| fulltext | fulltext |
| identifier | ISSN: 0960-894X |
| ispartof | Bioorganic & medicinal chemistry letters, 2012-01, Vol.22 (1), p.689-695 |
| issn | 0960-894X 1464-3405 |
| language | eng |
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| source | ScienceDirect Freedom Collection |
| subjects | Adrenergic beta-Agonists - chemical synthesis Adrenergic beta-Agonists - pharmacology Adrenoceptor agonist agonists Animals Asthma Asthma - drug therapy beta-adrenergic agonists Biological and medical sciences Bronchodilator Agents - pharmacology Cell Line, Tumor chemistry Chemistry, Pharmaceutical - methods COPD Cyclic AMP - metabolism Drug Design Duration Guinea Pigs Humans Inhaled Inhibitory Concentration 50 LABA Medical sciences Models, Chemical pharmacokinetics Pharmacology. Drug treatments Protein Binding Pulmonary Disease, Chronic Obstructive - drug therapy Thiazoles - pharmacology Time Factors β2-Agonist |
| title | From libraries to candidate: The discovery of new ultra long-acting dibasic β2-adrenoceptor agonists |
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