Franchin, Taisa Busaranho published the artcileAssessment of the Physicochemical Properties and Stability for Pharmacokinetic Prediction of Pyrazinoic Acid Derivatives, Recommanded Product: n-Octanol, the main research area is pharmacokinetics pyrazinoic acid stability physicochem property; Pyrazinoic acid; chemical stability; metabolism; permeability; pharmacokinetics; plasma stability.
Background: Tuberculosis (TB) is an infectious disease caused by Mycobacterium tuberculosis, which still has high prevalence worldwide. In addition, cases of drug resistance are frequently observed In the search for new anti-TB drugs, compounds with antimycobacterial activity have been developed, such as derivatives of pyrazinoic acid, which is the main pyrazinamide metabolite. In a previous study, the compounds were evaluated and showed moderate antimycobacterial activity and no important cytotoxic profile; however, information about their pharmacokinetic profile is lacking. Objective: The aim of this work was to perform physicochem., permeability, and metabolic properties of four pyrazinoic acid esters. Method: The compounds were analyzed for their chem. stability, n-octanol:water partition coefficient (logP) and apparent permeability (Papp) in monolayer of Caco-2 cells. The stability of the compounds in rat and human microsomes and in rat plasma was also evaluated. Results: The compounds I, II and IV were found to be hydrophilic, while compound III was the most lipophilic (logP 1.59) compound The apparent permeability measured suggests good intestinal absorption of the compounds Addnl., the compounds showed metabolic stability under action of human and rat microsomal enzymes and stability in rat plasma for at least 6 h. Conclusion: The results bring favorable perspectives for the future development of the evaluated compounds and other pyrazinoic acid derivatives
Current Drug Metabolism published new progress about Bioavailability. 111-87-5 belongs to class alcohols-buliding-blocks, name is n-Octanol, and the molecular formula is C8H18O, Recommanded Product: n-Octanol.
Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts