- BETA-STRAND MIMETICS AND METHOD RELATING THERETO
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Conformationally constrained compounds which mimic the secondary structure of ?-strand regions of biologically active peptides and proteins are disclosed. Such ?-strand mimetic structures have utility over a wide range of fields, including use as diagnostic and therapeutic agents. Libraries containing the ?-strand mimetic structures of this invention are also disclosed as well as methods for screening the same to identify biologically active members.
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- Amino acid derived heterocycles: Lewis acid catalyzed and radical cyclizations from peptide acetals
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Bicyclization of peptide acetals via nucleophilic attack of a phenyl group on an endocyclic acyliminium ion 4 was explored as a route to novel amino acid derived heterocycles and peptidomimetic scaffolds. In the presence of protic acid, bridged structures such as 6 are formed readily from phenylalanine derivatives, but the fused-ring analogues 5 could not be obtained in good yield. In contrast, radical cyclization of the bromophenyl dihydropyrazinone 7 provides an effective alternative for the synthesis of 5 (n = 0, 1, 2). Additional versatility in this process was demonstrated by efficient synthesis of a different fused ring system, represented by the antihelmintic praziquantel, 8.
- Todd, Matthew H.,Ndubaku, Chudi,Bartlett, Paul A.
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p. 3985 - 3988
(2007/10/03)
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- 3-Acylamino-1-carboxymethylaminocarbonyl-2-azetidinones
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Antibacterial activity is exhibited by 2-azetidinones having a 3-acylamino substituent and a 1-substituent of the formula STR1 (or a salt or ester thereof).
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