Symmetrical Phosphinic Acids: Synthesis and Esterification Optimization toward Potential HIV Prodrugs.

ABSTRACT: A highly efficient method to synthesize diverse symmetrical phosphinic acids with the potential to act as pivotal candidates in the design of HIV-1 protease inhibitors has been developed. Such compounds have been designed based on the enzyme-substrate specificity, and their elongated analogues are expected to demonstrate significant inhibition against the HIV-1 protease with IC₅₀ values in the low nanomolar range. Moreover, a highly efficient esterification protocol with carbohydrates and flavonoids has been devised to address the inherent absorption challenges associated with phosphinic-based drugs. These esters not only exhibit low toxicity but also have the potential to generate flavonoid moieties in situ, which are associated with hepatoprotective effects, or naturally occur

SUBMITTER: Hayat K 

PROVIDER: S-EPMC11465283 | biostudies-literature | 2024 Oct

REPOSITORIES: biostudies-literature