4.1 Article Proceedings Paper

IMPDH as a biological probe for RNA antiviral drug discovery: Synthesis, enzymology, molecular docking, and antiviral activity of new ribonucleosides with surrogate bases

Journal

NUCLEOSIDES NUCLEOTIDES & NUCLEIC ACIDS
Volume 26, Issue 6-7, Pages 651-654

Publisher

TAYLOR & FRANCIS INC
DOI: 10.1080/15257770701490506

Keywords

IMPDH inhibitors; synthesis; antiviral

Funding

  1. NATIONAL INSTITUTE OF ALLERGY AND INFECTIOUS DISEASES [U19AI056540] Funding Source: NIH RePORTER
  2. NIAID NIH HHS [AI056540] Funding Source: Medline

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Our interest in the discovery of molecules with antiviral activity against RNA viruses led us to the design of ribonucleosides with surrogate bases with the intent Of using inhibition of inosine monophosphate dehydrogenase (IMPDH) as a probe for antiviral drug discovery. A general methodology for the preparation of these compounds is discussed. Kinetic parameters of the inhibition studies with IMPDH, which were carried out spectrophotometrically by monitoring the formation of NADH, are given. Antiviral information and correlation of activity with IMPDH inhibition are discussed.

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