Despite a formidable repertoire of approved HIV inhibitors, drug resistance has complicated efforts to manage viral progression. Moreover, only 46% of infected patients have access to antiretroviral therapy (ART). As such, development of novel inhibitors that are inexpensive and mutation-resistant remains critical. Toward this end, our lab has developed novel mercaptobenzamide thioesters as viral acetylome modulators. To facilitate mechanism of action studies, we report a scalable (&gt;100 g) synthesis of mercaptobenzamide thioester SAMT-247, along with spectroscopically determined physical parameters, such as pKa, nucleophilicity, and thioester hydrolysis rates.

Scalable synthesis and spectroscopic analysis of mercaptobenzamide thioester (SAMT) HIV inhibitors

254th National Meeting (2017)

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