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The ฮฒ-lactam ring is the key reactive functionality of all penicillin and cephalosporin antibiotics and has subsequently attracted attention as a target for combinatorial chemistry. However, solid-phase synthetic approaches to these molecules that might permit the synthesis of a library of analogues has barely been reported. A recent paper describes a resin-supported approach to 1-oxacephams; compounds that offer potential biological activity (B.
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## Highlights from other journals -December 2000 Small molecule binding at the Src SH2 domain A variety of proteins involved in signal transduction contain non-catalytic Src homology-2 (SH2) domains that function as mediators of intracellular protein-protein interactions. These SH2 domains (~100 a
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
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-