Document Detail

Design and synthesis of bis-amide and hydrazide-containing derivatives of malonic acid as potential HIV-1 integrase inhibitors.
MedLine Citation:
PMID:  18830166     Owner:  NLM     Status:  MEDLINE    
HIV-1 integrase (IN) is an attractive and validated target for the development of novel therapeutics against AIDS. In the search for new IN inhibitors, we designed and synthesized three series of bis-amide and hydrazide-containing derivatives of malonic acid. We performed a docking study to investigate the potential interactions of the title compounds with essential amino acids on the IN active site.
Mario Sechi; Ugo Azzena; Maria Paola Delussu; Roberto Dallocchio; Alessandro Dessì; Alessia Cosseddu; Nicolino Pala; Nouri Neamati
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Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2008-10-01
Journal Detail:
Title:  Molecules (Basel, Switzerland)     Volume:  13     ISSN:  1420-3049     ISO Abbreviation:  Molecules     Publication Date:  2008  
Date Detail:
Created Date:  2008-10-02     Completed Date:  2008-12-10     Revised Date:  2009-10-27    
Medline Journal Info:
Nlm Unique ID:  100964009     Medline TA:  Molecules     Country:  Switzerland    
Other Details:
Languages:  eng     Pagination:  2442-61     Citation Subset:  IM    
Dipartimento Farmaco Chimico Tossicologico, Università di Sassari, Via Muroni 23/A, 07100 Sassari, Italy.
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MeSH Terms
Anti-HIV Agents / chemical synthesis,  chemistry,  pharmacology
Catalytic Domain
Computer Simulation
Drug Design
HIV Integrase Inhibitors / chemistry*,  pharmacology
Malonates / chemical synthesis*,  chemistry,  pharmacology*
Protein Binding
Structure-Activity Relationship
Reg. No./Substance:
0/Amides; 0/Anti-HIV Agents; 0/Azides; 0/HIV Integrase Inhibitors; 0/Malonates; 141-82-2/malonic acid

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