An article A Novel Prodrug of a nNOS Inhibitor with Improved Pharmacokinetic Potential WOS:000579806900001 published article about NITRIC-OXIDE SYNTHASE; SELECTIVE-INHIBITION; DERIVATIVES; AGENT; IDENTIFICATION; ACETAMIDINES; AMIDOXIME; COMPONENT; THERAPY; AMIDINE in [Maccallini, Cristina; Marinelli, Lisa; Cacciatore, Ivana; Fantacuzzi, Marialuigia; Di Stefano, Antonio; Amoroso, Rosa] Univ G dAnnunzio, Dept Pharm, Via Vestini 31, I-66100 Chieti, Italy; [Indorf, Patrick; Clement, Bernd] Univ Kiel, Inst Pharmaceut, Gutenbergstr 76, D-24118 Kiel, Germany in 2020.0, Cited 48.0. Application In Synthesis of Diphenylmethanamine. The Name is Diphenylmethanamine. Through research, I have a further understanding and discovery of 91-00-9
Under different pathological conditions, aberrant induction of neuronal nitric oxide synthase (nNOS) generates overproduction of NO that can cause irreversible cell damage. The aim of this study was to develop an amidoxime prodrug of a potent nNOS inhibitor, the benzhydryl acetamidine. We synthesized the benzhydryl acetamidoxime, which was evaluatedin vitroto ascertain the potential NOS inhibitory activity, as well as conducting bioconversion into the parent acetamidine. The prodrug was also profiled forin vitrophysicochemical properties, by determining the lipophilicity, passive permeation through the human gastrointestinal tract and across the blood-brain barrier by PAMPA, and chemical, enzymatic, and plasma stability. The obtained data demonstrate that the amidoxime prodrug shows an improved pharmacokinetic profile with respect to the acetamidine nNOS inhibitor, thus suggesting that it could be a promising lead compound to treat all those pathological conditions in which nNOS activity is dysregulated.
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