80676-35-3Relevant articles and documents
Thiol compounds, their production and use
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, (2008/06/13)
Compounds represented by general formula (1) or salts thereof which have a matrix metalloprotease inhibitory activity and are useful as drugs, wherein the rings A and B represent each an optionally substituted homocycle or heterocycle, etc.; R1s are the same or different and each represents hydrogen, optionally substituted hydrocarbyl, acyl, etc.; X1represents a bond, optionally substituted divalent aliphatic hydrocarbyl, etc.; X2represents a bond, optionally substituted divalent aliphatic hydrocarbyl, —O—, etc.; Ys are the same or different represents hydrogen, optionally substituted hydrocarbyl, oxo, etc.; m is 0 or 1; n is an integer of 1 to 3; q1is an integer of 1 to 2n+4; and q2is an integer of 0 to 2n+3, provided that q1+q2is 2n+4.
Modulation of pharmacological profile of diphenylethane (lefetamine- type) derivatives
Carrara, Maria,Zampiron, Stefano,Pittarello, Demetrio,Cima, Lorenzo,Rampa, Angela,Valenti, Piero,Da Re, Paolo,Giusti, Pietro
, p. 803 - 809 (2007/10/03)
With the aim to split the pharmacological properties of lefetamine (CAS 14148-99-3), some structural modifications of this compound have been studied. The basic group of lefetamine has been shifted from the alkyl chain to the vicinal phenyl ring and the N-substitution has been changed. The dimethylaminomethyl derivatives and chiefly the o-morpholinometyhl exhibited a strong anti-visceral chemical antinociception activity stripped of thermal antinociception properties and physical dependence liability. Furthermore through the introduction of a diethylaminomethyl group in the lefetamine structure some derivatives were selected exhibiting besided a significant increase in the anti-visceral chemical antinociception activity, remarkable local anesthetic properties.