106747-44-8Relevant articles and documents
METHOD OF USING (H+/K+)ATPASE INHIBITORS AS ANTIVIRAL AGENTS
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, (2008/06/13)
A class of compounds which are (H+/K+) ATPase inhibitors can be used for the treatment of viral infections. Compounds of particular interest are defined by Formula III: wherein D is N or CH; wherein R7 is one or more radicals selected from hydrido, alkoxy, amino, cyano, nitro, hydroxyl, alkyl, halo, haloalkyl, carboxyl, alkanoyl, nitro, amino, alkylamino, aminocarbonyl , aminosulfonyl , alkylaminocarbonyl, alkylcarbonylamino, alkoxycarbonyl, alkylaminosulfonyl, alkylsulfonylamino, alkylthio, alkyl-sulfinyl and alkylsulfonyl; wherein R8 is selected from hydrido, alkyl and cycloalkyl; wherein R9 is one or more radicals selected from hydrido, alkoxy, amino, alkyl, halo, cyano, nitro, hydroxyl, haloalkyl, nitro, carboxyl, alkanoyl, amino, alkylamino, dialkylamino, aminocarbonyl , alkylaminocarbonyl, alkylcarbonylamino, aminosulfonyl, alkylaminosulfonyl, alkylsulfonylamino, alkoxycarbonyl, alkylthio, alkylsulfinyl and alkylsulfonyl; and wherein R10 and R11 are independently selected from hydrido, alkyl, aryl, alkylcarbonyl and arylcarbonyl wherein the aryl ring may be further substituted with one or more radicals selected from alkyl, halo, hydrazidylcarbonyl, aminocarbonyl and alkoxy; or wherein R10 and R11 together with the nitrogen atom form a heterocyclic ring
Substituted 2-anilines as Potential Inhibitors of H+/K+ ATPase
Adelstein, Gilbert W.,Yen, Chung H.,Haack, Richard A.,Yu, Stella,Gullikson, Gary,et al.
, p. 1215 - 1220 (2007/10/02)
A series of substituted 2-anilines were synthesized as potential inhibitors of the acid secretory enzyme H+/K+ ATPase.Substitutions on the aniline nitrogen atom resulted in potent enzyme inhibition in vitro but weak activity in gastric fistula dogs.Electron-donating substituents on the aniline ring enhanced in vitro and in vivo potency relative to the unubstituted analogue.The potency showed a correlation to the calculated pKa of the aniline nitrogen atom.Substitutions on the aniline and benzimidazole rings did not further enhance potency.Di- and trisubstituted aniline derivatives were potent inhibitors of the enzyme system.The preferred combination of substituents were a methoxy group on the benzimidazole ring and a single alkyl group on the aniline ring.One such compound, 76, was an effective inhibitor of acid secretion in the dog and was selected for further pharmacological study.
