Please use this identifier to cite or link to this item: https://hdl.handle.net/2440/34452
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Type: Journal article
Title: α-Methylene tetrazole-based peptidomimetics: synthesis and inhibition of HIV protease
Other Titles: alpha-Methylene tetrazole-based peptidomimetics: synthesis and inhibition of HIV protease
Author: May, B.
Abell, A.
Citation: Organic and Biomolecular Chemistry, 2002; 2(2):172-178
Publisher: Royal Society of Chemistry
Issue Date: 2002
ISSN: 1472-7781
1364-5463
Statement of
Responsibility: 
Barnaby C. H. May and Andrew D. Abell
Abstract: An α-methylene tetrazole-based dipeptidomimetic (11) has been prepared as a constrained and non-hydrolysable core for incorporation into peptides. A single crystal X-ray structure determination revealed that its solid-state conformation closely resembles that of the isosteric core of JG-365 bound to HIV protease. The α-methylene tetrazole isosteric unit was then incorporated into a number of peptide sequences and the resulting compounds 6–8 were assayed against HIV protease. The assay results suggest that the longer the C-terminal substitution the greater the potency, a result that reflects the interplay of the geometry of the tetrazole isostere and the C-terminal substituent.
Rights: © The Royal Society of Chemistry 2002
DOI: 10.1039/b109128j
Published version: http://dx.doi.org/10.1039/b109128j
Appears in Collections:Aurora harvest 6
Chemistry publications

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