Quinolone 3-carboxylic acid pharmacophore: design of second generation HIV-1 integrase inhibitors.

@article{Dayam2008Quinolone3A,
  title={Quinolone 3-carboxylic acid pharmacophore: design of second generation HIV-1 integrase inhibitors.},
  author={Raveendra Dayam and Laith Q. Al-Mawsawi and Zahrah Zawahir and Myriam Witvrouw and Zeger Debyser and Nouri Neamati},
  journal={Journal of medicinal chemistry},
  year={2008},
  volume={51 5},
  pages={1136-44}
}
Two decades of intensive research efforts have led to the discovery of a large number of HIV-1 integrase (IN) inhibitors. Recently, the United States Food and Drug Administration (US FDA) approved MK-0518, or raltegravir ( 1), as the first IN inhibitor for HIV/AIDS treatment. Growing clinical evidence also demonstrates that the emergence of HIV-1 virus strains bearing IN amino acid substitutions that confer resistance to IN inhibitors is inevitable. The discovery of second generation inhibitors… CONTINUE READING

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