Next Article in Journal
Preparation of Substituted Methyl o-Nitrophenyl Sulfides
Previous Article in Journal
Discovery of a Novel CCR5 Antagonist Lead Compound Through Fragment Assembly
Article Menu

Article Versions

Export Article

Open AccessArticle
Molecules 2008, 13(10), 2442-2461; doi:10.3390/molecules13102442

Design and Synthesis of Bis-amide and Hydrazide-containing Derivatives of Malonic Acid as Potential HIV-1 Integrase Inhibitors

1
Dipartimento Farmaco Chimico Tossicologico, Università di Sassari, Via Muroni 23/A, 07100 Sassari, Italy
2
Dipartimento di Chimica, Università di Sassari, Via Vienna 2, 07100 Sassari, Italy
3
CNR-Istituto di Chimica Biomolecolare, Sassari, 07040 Li Punti, Italy
4
Dipartimento Farmaco Chimico Tecnologico, Università di Siena, Via A. Moro, 53100 Siena, Italy
5
Department of Pharmacology and Pharmaceutical Sciences, University of Southern California, School of Pharmacy, 1985 Zonal Avenue, PSC 304, Los Angeles, California, 90089, USA
*
Authors to whom correspondence should be addressed.
Received: 11 April 2008 / Revised: 19 September 2008 / Accepted: 19 September 2008 / Published: 1 October 2008
View Full-Text   |   Download PDF [1160 KB, uploaded 18 June 2014]   |  

Abstract

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.
Keywords: Bis-amides; Hydrazides; Malonic acid; HIV-1; HIV-1 integrase; Docking studies Bis-amides; Hydrazides; Malonic acid; HIV-1; HIV-1 integrase; Docking studies
Figures

This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

Scifeed alert for new publications

Never miss any articles matching your research from any publisher
  • Get alerts for new papers matching your research
  • Find out the new papers from selected authors
  • Updated daily for 49'000+ journals and 6000+ publishers
  • Define your Scifeed now

SciFeed Share & Cite This Article

MDPI and ACS Style

Sechi, M.; Azzena, U.; Delussu, M.P.; Dallocchio, R.; Dessì, A.; Cosseddu, A.; Pala, N.; Neamati, N. Design and Synthesis of Bis-amide and Hydrazide-containing Derivatives of Malonic Acid as Potential HIV-1 Integrase Inhibitors. Molecules 2008, 13, 2442-2461.

Show more citation formats Show less citations formats

Related Articles

Article Metrics

Article Access Statistics

1

Comments

[Return to top]
Molecules EISSN 1420-3049 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert
Back to Top