title: A one-pot preparation of N-2-mercaptobenzoyl-amino amides.
abstract: The HIV-1 nucleocapsid (NCp7), structurally defined by zinc-binding domains, participates in crucial stages of the HIV-1 lifecycle and is mutationally nonpermissive, making it an attractive anti-HIV target. Mode of action studies have shown that the secondary structure and activity of NCp7 can be disrupted by acyl transfer from N-2-mercaptobenzoyl-amino amides. We have developed an improved one-pot reaction that affords N-2-mercaptobenzoyl-amino acids on multi-gram scales. This synthetic route allows for rapid modular construction and has greatly expanded the scope of easily accessible potential NCp7 inhibitors.
authors.affiliation: National Institute of Diabetes and Digestive and Kidney Diseases (NIDDK), National Institutes of Health, Bethesda, Maryland, 20892, U.S.A.
authors.forename: Robert J
authors.initials: RJ
authors.lastname: Bahde
authors.forename: Daniel H
authors.initials: DH
authors.lastname: Appella
authors.forename: William C
authors.initials: WC
authors.lastname: Trenkle