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2,3-dihydro-6,7-dihydroxy-1H-isoindol-1-one-based HIV-1 integrase inhibitors

  1. Author:
    Zhao, X. Z.
    Semenova, E. A.
    Vu, B. C.
    Maddali, K.
    March, C.
    Hughes, S. H.
    Pommier, Y.
    Burke, T. R.

  2. Author Address

    Zhao, Xue Zhi, Burke, Terrence R., Jr.] NCI, Canc Res Ctr, Med Chem Lab, Frederick, MD 21701 USA. [Vu, B. Christie, Hughes, Stephen H.] NCI, Canc Res Ctr, HIV Drug Resistance Program, Frederick, MD 21701 USA. [Zhao, Xue Zhi, Semenova, Elena A.; Vu, B. Christie, Maddali, Kasthuraiah, Marchand, Christophe, Hughes, Stephen H.; Pommier, Yves, Burke, Terrence R., Jr.] Natl Inst Hlth, Frederick, MD 21702 USA. [Semenova, Elena A.; Maddali, Kasthuraiah, Marchand, Christophe, Pommier, Yves] NCI, NIH, Mol Pharmacol Lab, Bethesda, MD 20892 USA.
    1. Year: 2008
  2. Journal: Journal of Medicinal Chemistry
    1. 51
    2. 2
    3. Pages: 251-259
  4. Type of Article: Article
  1. Abstract:

    The bis-salicylhydrazides class of HIV-1 integrase (IN) inhibitors has been postulated to function by metal chelation. However, members of this series exhibit potent inhibition only when Mn2+ is used as cofactor. The current study found that bis-aroylhydrazides could acquire inhibitory potency in Mg2+ using dihydroxybenzoyl substituents as both the right and left components of the hydrazide moiety. Employing a 2,3-dihydro-6,7-dihydroxy-1H-isoindol-1-one ring system as a conformationally constrained 2,3-dihydroxybenzoyl equivalent provided good selectivity for IN-catalyzed strand transfer versus the 3'-processing reactions as well as antiviral efficacy in cells using HIV-1 based vectors.

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External Sources

  1. PMID: 18095643

Library Notes

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