Synthesis of N-acetyl derivatives of 5- and 6-ethoxy-2-methylthiobenzimidazole and their cardiotonic activity
The regioselectivity of the N-acetylation of 5- and 6-ethoxy-2-methylthiobenzimidazole for various acetylating agents under various conditions has been investigated. The cardiotonic activity of the 1-acetyl-5-ethoxy- and 1-acetyl-6-ethoxy-2-methylthiobenzimidazoles synthesized and of their 5,6-diethoxy analog has been studied. 1997 Plenum Publishing Corporation.
Brukshtus,Sirvidite,Garalene,Labanauskas
p. 665 - 671
(2007/10/03)
BASICITY AND STRUCTURE OF 5-HYDROXYBENZIMIDAZOLES IN NITROMETHANE
Examination of the acid-base properties of 5-hydroxybenzimidazoles has shown them to exist in nitromethane as the 5-hydroxy-tautomers.Substituents in the 2-position have a predominantly inductive effect on the basicity of the 3-nitrogen, rationalized as in other nitrogen heterocycles by the proximity of the substituents to the reaction center. Keywords: 5-hydroxybenzimidazole, its tautomers and derivatives; acid-base properties and the effect thereon of substituents; Taft and inductive constants.
Korolev, B. A.,Osmolovskaya, L. A.,Kuznetsov, Yu. V.,Stolyarova, L. G.,Smirnov, L. D.
p. 333 - 336
(2007/10/02)
Inhibition of Rat Hepatic Microsomal Aminopyrine N-Demethylase Activity by Benzimidazole Derivatives. Quantitative Structure-Activity Relationships
Eighty-two benzimidazole derivatives have been prepared and tested for the ability to inhibit cytochrome P-450 mediated enzyme activity (aminopyrine N-demethylase) from phenobarbitone-induced rat hepatic microsomes.Using physicochemical parameters and multiple regression analysis, we derived a quantitative structure-activity relationship (QSAR) that describes up to 87percent of the data variance in terms of hydrophobic and electronic effects and the molar refractivity of the substituent in the 2-position of the benzimidazole ring.
Murray, Michael,Ryan, Adrian J.,Little, Peter J.
p. 887 - 892
(2007/10/02)
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