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Whilst ยต-opioid antagonists have been used for many years in the treatment of drug abuse, ฮบ antagonists might provide a more effective and longer-lasting treatment and novel agents provide an attractive target for drug discovery. The library described in this publication was based on 3,4-dimethyl-4-(3hydroxyphenyl)piperidine (1), a pharmacophore known to give non-selective opioid activity, and two other components, an N-substituted or unsubstituted Boc-protected amino acid and a range of substituted aryl carboxylic acids in a parallel solution-phase approach.
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The sarcodictyins A (1, R = Me) and B (1, R = Et), originally isolated from a soft coral, are complex natural products with potent antitumour activity through a taxol-like mode of action (tubulin polymerisation and microtubule stabilisation). In a recent paper, a solid-phase synthetic route to the s
## Bicyclic Guanidine Libraries A novel method for the solid-phase synthesis of bicyclic guanidines has been described in a recent publication (J.M. Ostresh et al., J. Org. Chem., 63, (1998), 8622-8623). Following the preparation of acylated dipeptides (1) on methylbenzhydrylamine-derivatised poly
Obesity is an increasingly common disease in the western world and incidence has been associated with a range of other diseases including hypertension, atherosclerosis and type II (non-insulin dependent) diabetes. However, little is known about the proteins that mediate gene control of lipid metabol