- 1,4-Benzodiazepines as inhibitors of respiratory syncytial virus. The identification of a clinical candidate
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Respiratory syncytial virus (RSV) is the cause of one-fifth of all lower respiratory tract infections worldwide and is increasingly being recognized as representing a serious threat to patient groups with poorly functioning or immature immune systems. Rac
- Henderson, Elisa A.,Alber, Dagmar G.,Baxter, Robert C.,Bithell, Sian K.,Budworth, Joanna,Carter, Malcolm C.,Chubb, Ann,Cockerill, G. Stuart,Dowdell, Verity C. L.,Fraser, Ian J.,Harris, Robert A.,Keegan, Sally J.,Kelsey, Richard D.,Lumley, James A.,Stables, Jeremy N.,Weerasekera, Natasha,Wilson, Lara J.,Powell, Kenneth L.
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p. 1685 - 1692
(2008/02/01)
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- Methods for Drug Discovery: Development of Potent, Selective, Orally Effecive Cholecystokinin Antagonists
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3-(Acylamino)-5-phenyl-2H-1,4-benzodiazepines, antagonists of the peptide hormone cholecystokinin (CCK), are described.Developed by reasoned modification of the known anxiolytic benzodiazepines, these compounds provide highly potent, orally effective ligands selective for peripheral (CCK-A) receptors, with binding affinities approaching or equaling that of the natural ligand CCK-8.The distinction between CCK-A receptors on the one hand and CNS (CCK-B), gastrin, and central benzodiazepine receptors on the other is demonstrated by using the structure-activity profiles of the new compounds.Details of the binding of these agents to CCK-A receptors are examined, and the method of development of these compounds is discussed in terms of its relevance to the general problem of drug discovery.
- Evans, B. E.,Rittle, K. E.,Bock, M. G.,DiPardo, R. M.,Freidinger, R. M.,et al.
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p. 2235 - 2246
(2007/10/02)
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- A NEW AMINE RESOLUTION METHOD AND ITS APPLICATION TO 3-AMINOBENZODIAZEPINES
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A new method for the resolution of amines and its application to 3-aminobenzodiazepines 1 is described.The method involves the synthesis and separation of a pair of phenylalanyl amide diastereomers followed by removal of phenylalanine via the Edman degrad
- Rittle, Kenneth E.,Evans, Ben E.,Bock, Mark G.,DiPardo, Robert M.,Whitter, Willie L.,et al.
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p. 521 - 522
(2007/10/02)
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