124313-46-8Relevant academic research and scientific papers
Selective and Potent Monoamine Oxidase Type B Inhibitors: 2-Subtituted 5-Aryltetrazole Derivatives
Lebreton, Luc,Curet, Olivier,Gueddari, Salach,Mazouz, Fathi,Bernard, Suzanne,et al.
, p. 4786 - 4792 (1995)
Twenty new 2-(cyanoalkyl)tetrazoles (15 and 16) and twenty new 2-(hydroxyalkyl)tetrazoles (17 and 18) were synthesized and investigated in vitro for their abilities to inhibit selectivity rat brain monoamine oxidase (MAO) B over MAO A.Most of then were MAO B inhibitors and those bearing a sunstituted 4-(arylmethoxy)phenyl group in the position 5 of the tetrazole ring had IC50 values between 8 νM for 18d and 2 nM for 16a (30 nM for lazabemide) with a selectivity toward MAO B of 37000 for 16a.The reversibility of their inhibitory activity was demonstrated by in vitro dialysis tests.The 5--2-(2-cyanoethyl)-tetrazole (16a) its derivative 16h and the 5--2-(2-hydroxyethyl)-tetrazole (18a) and its derivative 18h were found to be potent, in vitro selective, and competitive MAO B inhibitors.Tetrazole 16a can be considered one of the most active and selective competitive MAO B inhibitors known up to now.This compound was selected for ex vivo experiments and shown to be a strong and reversible MAO B inhibitor with a short duration of action after oral administration at 5 mg/kg.The structure-activity approach gives rise to the great inportance of lipophilicity over electronic effects of the compounds in these series.
Synthesis of polynuclear nonfused azoles
Verkhozina,Kizhnyaev,Vereshchagin,Rokhin,Smirnov
, p. 1792 - 1796 (2007/10/03)
Polynuclear blocks consisting of nonfused heterocycles of the azole series, connected through methylene bridges, were synthesized by successive addition of azole units via cycloaddition of organic azides to the triple bond of N-(2-propynyl)azoles, as well
Synthesis and acidity of 5-phenyltetrazol-2-ylalkanoic acids and the corresponding 5-(5-phenyltetrazol-2-ylalkyl)tetrazoles
Esikov,Zubarev,Bezklubnaya,Malin,Ostrovskii
, p. 986 - 991 (2007/10/03)
We have obtained 5-phenyltetrazol-2-ylalkanoic acids and their derivatives containing terminal nitrile, amide, and tetrazol-5-yl groups. Tetrazolylalkanoic acids with two (pKa 4.93) and three (pKa 5.45) bridging methylene groups are
