Donetti, Arturo published the artcileN-(Fluoroethyl)(imidazolylphenyl)formamidines. The issue of the active species of mifentidine, SDS of cas: 359-38-6, the main research area is fluoroethylaminomethyleneaminophenylimidazole preparation antihistaminic; mifentidine fluorinated analog antihistaminic; substituent fluorine mifentidine analog; basicity fluorinated analog mifentidine.
(Imidazolylphenyl)formamidines I (R = CH2F, CHF2, CF3) were prepared to test the effect of F substitution on basicity and, then, on H2-antagonist affinity in comparison with I (R = Me) taken as a model of mifentidine. Imidazolylphenyl isothiocyanate, obtained by reaction of 4-(aminophenyl)imidazole with CS2 and ClCO2Et, was condensed with RCH2NH2.HCl to give thioureas. Desulfurization of these thioureas by Raney Ni furnished I. Increasing F substitution in I decreased the basicity of the formamidino group substantially while having a modest effect on the imidazole portion. Affinity at the H2 receptors, evaluated from antagonism of histamine-stimulated chronotropic response on guinea pig atria, increased with F substitution. Thus, H2-receptor antagonist affinity in the mifentidine series is mostly dependent on the availability of the neutral species, supporting the hypothesis that mifentidine acts through the neutral species.
Journal of Medicinal Chemistry published new progress about Antihistamines. 359-38-6 belongs to class amides-buliding-blocks, name is 2,2-Difluoroacetamide, and the molecular formula is C2H3F2NO, SDS of cas: 359-38-6.
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