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Phosphoramidates and phosphonamidates (ProTides) with antiviral activity

Slusarczyk, Magdalena ORCID:, Serpi, Michaela ORCID: and Pertusati, Fabrizio ORCID: 2018. Phosphoramidates and phosphonamidates (ProTides) with antiviral activity. Antiviral Chemistry and Chemotherapy 26 , pp. 1-31. 10.1177/2040206618775243

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Following the first report on the nucleoside phosphoramidate (ProTide) prodrug approach in 1990 by Chris McGuigan, the extensive investigation of ProTide technology has begun in many laboratories. Designed with aim to overcome limitations and the key resistance mechanisms associated with nucleoside analogues used in the clinic (poor cellular uptake, poor conversion to the 5′-monophosphate form), the ProTide approach has been successfully applied to a vast number of nucleoside analogues with antiviral and anticancer activity. ProTides consist of a 5′-nucleoside monophosphate in which the two hydroxyl groups are masked with an amino acid ester and an aryloxy component which once in the cell is enzymatically metabolized to deliver free 5′-monophosphate, which is further transformed to the active 5′-triphosphate form of the nucleoside analogue. In this review, the seminal contribution of Chris McGuigan’s research to this field is presented. His technology proved to be extremely successful in drug discovery and has led to two Food and Drug Administration-approved antiviral agents.

Item Type: Article
Date Type: Published Online
Status: Published
Schools: Pharmacy
Publisher: Nucleus Global
ISSN: 2040-2066
Date of First Compliant Deposit: 31 May 2018
Date of Acceptance: 13 May 2018
Last Modified: 06 Dec 2023 02:06

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