Ionization Constants of Isoniazid and Benzimidazole

Purpose The aim of this study was to evaluate the physicochemical properties of a series of isoniazid and benzimidazole Potentiometric Shake-Flask 3 Departamento de Química e Bioquímica, Faculdade de Ciências, Universidade de Isoniazid derivatives. The aim of this study was to evaluate the physicochemical properties of a series of isoniazid and benzimidazole derivatives. Some of these derivatives have been shown to have promising anti-tubercular activity by comparison with isoniazid, and retain their activity against a panel of isoniazid-resistant bacteria strains. Their feasibility as drug-like candidates could be evaluated from information about their potency, together with Compound Structure M / g mol-1 pKa (I=0) Potentiometric log Po/w Shake-Flasklog Po/w Isoniazid A 137.14 pK1= 3.53 ± 0.04 pK2=11.14 ± 0.07 logPn= -0.65 ± 0.03 -0.85 ± 0.01 (N=4) NOHNNH2 feasibility as drug-like candidates could be evaluated from information about their potency, together with knowledge of their lipophilicity logPo/w), which models their ability to penetrate biological membranes and their acid dissociation constant (pKa), which affects the charge and therefore the passive transport across the membrane and the activity in the living organism.