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  • ePoster presentation
  • Open Access

Design, synthesis and biological evaluation on N- heteroaryl compounds as probable NNRTIs against laboratory adapted strains and the primary isolates of HIV-1

  • 1,
  • 1,
  • 1,
  • 1,
  • 2,
  • 2,
  • 2,
  • 2 and
  • 1Email author
BMC Infectious Diseases201414 (Suppl 3) :E15

https://doi.org/10.1186/1471-2334-14-S3-E15

  • Published:

Keywords

  • Pyrimidine
  • Benzimidazole
  • Cell Base Assay
  • Primary Isolate
  • Spectral Technique

Background

The emergence of drug resistant HIV strains and suitability of NNRTIs as potent anti-HIV molecules used in HAART did attract our attention towards developing NNRTIs. We, therefore, focused on developing some new NNRTIs utilizing benzimidazole and pyrimidine moieties to match the hydrophobic nature of the allosteric pocket in HIV-RT.

Methods

Compounds designed on the basis of extensive computational studies, were finally synthesized through facile synthetic route and characterized using various chromatographic and spectral techniques. All synthesized molecules have been screened against HIV-1 using TZM bl assay and laboratory adapted strains HIV-1 IIIB (X4, subtype B), HIV-1 Ada5 (R5, Subtype B) and the primary isolates HIV-1UG070 (X4, Subtype D).

Results

Cell based assay showed that majority of the compounds were active at micro molar concentrations (1.39-17.39 µM) and the SI value ranged between 10.77-17.39 against lab adapted strains and 5.8–13.91 against primary isolates. The studies on structure–activity relationship were also consistent with the experimental data.

Conclusions

In view of the results obtained, these compounds may be developed as potent inhibitors of HIV-1 replication with suitable structural/pharmacophore modifications.

Authors’ Affiliations

(1)
Nucleic Acids & Antiviral Research Laboratory, Department of Chemistry, University of Allahabad, India
(2)
National AIDS Research Institute, Pune, India

Copyright

© Singh et al; licensee BioMed Central Ltd. 2014

This article is published under license to BioMed Central Ltd. This is an Open Access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/4.0), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. The Creative Commons Public Domain Dedication waiver (http://creativecommons.org/publicdomain/zero/1.0/) applies to the data made available in this article, unless otherwise stated.

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