Saha, Mrinmoy; Scerba, Michael T.; Shank, Nathaniel I.; Hartman, Tracy L.; Buchholz, Caitlin A.; Buckheit, Robert W. Jr.; Durell, Stewart R.; Appella, Daniel H. published the artcile< Probing Mercaptobenzamides as HIV Inactivators via Nucleocapsid Protein 7>, Electric Literature of 112-63-0, the main research area is mercaptobenzamide prodrug preparation antiviral HIV nucleocapsid protein NCp7 target; HIV; antiviral agents; mercaptobenzamides; nucleocapsid protein 7; prodrugs.
Human immunodeficiency virus type 1 (HIV-1) nucleocapsid protein 7 (NCp7), a zinc finger protein, plays critical roles in viral replication and maturation and is an attractive target for drug development. However, the development of drug-like mols. that inhibit NCp7 has been a significant challenge. In this study, a series of novel 2-mercaptobenzamide prodrugs were investigated for anti-HIV activity in the context of NCp7 inactivation. The mols. were synthesized from the corresponding thiosalicylic acids, and they are all crystalline solids and stable at room temperature Derivatives with a range of amide side chains and aromatic substituents were synthesized and screened for anti-HIV activity. Wide ranges of antiviral activity were observed, with IC50 values ranging from 1 to 100 μM depending on subtle changes to the substituents on the aromatic ring and side chain. Results from these structure-activity relationships were fit to a probable mode of intracellular activation and interaction with NCp7 to explain variations in antiviral activity. The authors’ strategy to make a series of mercaptobenzamide prodrugs represents a general new direction to make libraries that can be screened for anti-HIV activity.
ChemMedChem published new progress about Acetylation. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Electric Literature of 112-63-0.
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