Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 12, Issue 5, Pages 1215-1220Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2003.11.006
Keywords
ADS-J1 analogues; fusion inhibitor; gp41; HIV-1
Funding
- NIAID NIH HHS [R01 AI46221] Funding Source: Medline
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A structure-based design approach has been used to optimize a lead HIV-1 entry inhibitor targeted to the envelope glycoprotein gp41. The docking study on this lead compound revealed important structural requirements that need to be preserved as well as structural non-requirements that could be eliminated to substantially reduce the molecular size of the lead compound. Based on the results from docking study, a limited number of analogues were designed and synthesized. This approach yielded a new analogue (compound 4) that retained the anti-HIV-1 activity with reduced molecular size approaching towards more drug-like character. (C) 2003 Elsevier Ltd. All rights reserved.
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