From Peptide to Non-Peptide. 2. The de Novo Design of Potent, Non-peptidal Inhibitors of Platelet Aggregation Based on a Benzodiazepinedione Scaffold

Design of a Novel Small Peptide Targeted against a Tumor-Specific Receptor

“…Secondly, techniques for evaluating the binding characteristics of peptides are well established and easily performed in the laboratory. Finally, proteaseresistant peptide analogs, or nonpeptidic small molecules, can be designed based on the side-chain chemistries of the original peptide (13).…”

Generation of an LFA-1 Antagonist by the Transfer of the ICAM-1 Immunoregulatory Epitope to a Small Molecule

“…Similar de novo smallmolecule design efforts had been successful in the past from a similarly sized peptide (19)(20)(21). While these design studies were under way, ortho-bromobenzoyl tryptophan (designated compound 1 in Table 1 Table 1)…”

“Multi-component Reactions : Emerging Chemistry in Drug Discovery” ‘From Xylocain to Crixivan’

“…Where will isocyanide based multi-component reactions go in the next decade? With the advent of functional proteomics [72] delivering hundreds of new targets to drug discovery, ultra-high-throughput screening and a premium on novel biologically active entities, it seems reasonable to speculate that the discovery of new IMCRs will continue, spawning multiple post-condensation possibilities via secondary reactions. In addition to rational chemical design, Weber's pioneering 'combinatorial reaction finding' is one way to accelerate this [119].…”

“…Reports of the biological utility of 1,4-benzodiazepine-2,5-diones (BDP's), in particular, have appeared in many areas, including applications as antagonists of the platelet glycoprotein IIb-IIIa [72] and anti-convulsant agents to name but a few [73]. Many routes to libraries of this class of molecule have been developed, including one of the early pioneering solid phase methods reported by Bunin and Ellman [74].…”