61413-61-4Relevant academic research and scientific papers
Labile, non-heterocyclic quaternary ammonium salt/esters as transient derivatives
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, (2008/06/13)
Labile quaternary ammonium salts of the following formula (I) and (II) are provided: STR1 wherein STR2 represents a tertiary aliphatic amine; wherein STR3 represents an unsaturated amine; wherein R represents a member selected from the group consisting of a hydrogen atom, a C1 -C8 open chain or cyclo alkyl group, a C1 -C8 alkoxyalkyl group, a C1 -C8 acyloxyalkyl group, a C1 -C8 haloalkyl group, a C1 -C8 carboxyalkyl group, a C2 -C8 alkenylphenyl group, an aryl group, and a substituted aryl group, whose substituents are selected from the group consisting of a halogen atom, an O-lower alkyl (C1 -C4) group, an O-acyl group, a nitro group, a carboxyl group, and a carboethoxy group; wherein R1 which may be the same or different, represents any member defined by R above with the proviso that R1 cannot be a hydrogen atom; wherein X is --O-- or --S--; and wherein Y represents a member selected from the group consisting of a halogen atom or any other organic or inorganic monovalent equivalent anion; With the further proviso that STR4 respectively cannot represent trimethylamine and pyridine or quinoline when R represents a hydrogen atom and R1 represents a methyl group or a phenyl group. The compounds described above are characterized by their extreme solubility and resistance to oxidation, dealkylation, and protonation prior to chemical and/or enzymatic hydrolysis. Upon chemical and/or enzymatic hydrolysis, these compounds will "cleave," thus releasing their active constituent or constituents, according to the following general scheme(s): STR5 In other words, the title compounds hydrolyze (chemically or enzymatically) releasing a tertiary amine or unsaturated amine derivative, an aldehyde, a carboxylic acid and a hydrogen halide (HX) per the above reaction scheme.
Labile quaternary ammonium salts useful in binding bile acids in warm-blooded animals
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, (2008/06/13)
Free and conjugated bile acids are effectively bound in warm-blooded animals by administering thereto, a therapeutically effective bile acid binding amount of a quaternary ammonium compound having the formula: STR1 wherein N represents a tertiary open chain or cyclic aliphatic amine; wherein N represents an unsaturated amine; wherein R represents a member selected from the group consisting of a hydrogen atom, a C1 -C20 open chain or cyclo alkyl group, a C1 -C20 alkoxyalkyl group, a C1 -C20 alkanoyloxyalkyl group, a C1 -C20 haloalkyl group, a C1 -C20 carboxyalkyl group, an aryl group, and a substituted aryl group, whose substituents are selected from the group consisting of a halogen atom, an O-C1 -C4 alkyl group, an O-C1 -C8 alkanoyl group, a nitro group, a carboxyl group, and a carboethoxy group; wherein R1, which may be the same or different, represents any member defined by R above with the proviso that R cannot be a hydrogen atom, a STR2 WHEREIN R3, R4, R5 and R6 are each selected from the group consisting of a hydrogen atom, a methyl group or an ethyl group, a C0 -C22 straight or branched STR3 WHEREIN N IN EACH OCCURRENCE AND M REPRESENTS AN INTEGER OF FROM 0 TO 22, AN STR4 WHEREIN A represents a C0 -C22 straight or branched alkyl group as above or a --(CH2 CH2 O)p group, wherein the p represents an integer of from 0 to 22, and the residue of any naturally occurring bile acid or synthetic derivative thereof; and wherein X- represents a halogen atom or any other organic or inorganic monovalent anion are disclosed. These components are relatively nontoxic and substantially bind bile acids in warm-blooded animals and thus reduce the ulcerogenic symptoms exhibited by those characterized as being ulcerprone.
Soft quaternary surface active agents exhibiting antibacterial activity
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, (2008/06/13)
Soft quaternary surface active agents having the formula: EQU1 wherein EQU2 represents a tertiary open chain or cyclic aliphatic amine; wherein EQU3 represents an aromatic amine; wherein R represents a member selected from the group consisting of a hydrogen atom, a C1 -C20 open chain or cyclo alkyl group, a C1 -C20 alkoxyalkyl group, a C1 -C20 acyloxyalkyl group, a C1 -C20 haloalkyl group, a C1 -C20 carboxyalkyl group, an aryl group, and a substituted aryl group, whose substituents are selected from the group consisting of a halogen atom, an O--C1 -C4 alkyl group, an O--C1 -C8 acyl group a nitro group, a carboxyl group, and a carboethoxy group; wherein R1 represents a C9 -C22 straight or branched alkyl group, a EQU4 group, wherein R3, R4, R5 and R6 are each selected from the group consisting of a hydrogen atom, a methyl group or an ethyl group, a C0 -C22 straight or branched SPC1 Group, wherein n in each occurrence and m represent an integer of from 0 to 22, an SPC2 Group, wherein A represents a C0 -C22 straight or branched alkyl group as above or a -(CH2 CH2 O)p group, wherein the p represents an integer of from 0 to 22, and the residue of any naturally occurring bile acid or synthetic derivative thereof; and wherein X represents a halogen atom or any other organic or inorganic movement anion are disclosed. All compounds encompassed within the above-described generic formulae find use as "soft" antibacterial agents of extremely low toxicity.
