Anti-HIV Acylthiol & Thioether prodrugs (U.S. Patent Number 12/414,321)

Acronym: Not Available NIDDK Contact: Principal Investigator(s): Daniel Appella

These inventions provide the compositions, pharmaceutical carrier, and usages of the new Acylthiols (E-329-2000 family) and Thioether pro-drug (E-177-2010 family) compounds in treatment of retroviral infections such as HIV. These compounds target the highly-conserved nucleocapsid protein 7 (NCp7) of HIV-1. This protein functions throughout the viral replication cycle and is involved with reverse transcription, integration, and assembly and packaging of the viral genomic material.  This protein is conserved among strains of HIV-1. Activity of these compounds against the nucleocapsid protein leads to inactivation of the virus via disruption of the zinc fingers, integral for infectivity, without significantly affecting cellular proteins.
These compounds can be prepared from inexpensive starting materials and two “one-pot” reactions. Thus, they open the possibility for an effective drug treatment for HIV that could reach underdeveloped countries. These new compounds have the potential to be used both as a systemic drug for the treatment of HIV-1 infection and as a topically-applied or controlled-release barrier to prevent viral transmission.

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