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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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