125744-12-9Relevant articles and documents
New antifolate 4,4'-diaminodiphenyl sulfone substituted 2,4-diamino-5-benzylpyrimidines. Proof of their dual mode of action and autosynergism
Wiese,Schmalz,Seydel
, p. 161 - 168 (2007/10/03)
New 4,4'-diaminodiphenylsulfone substituted 2,4-diamino-5-benzylpyrimidines were synthesized. These compounds are highly active inhibitors of both bacterial dihydrofolate reductase (DHFR) and dihydropteroic acid synthase (SYN). The simultaneous inhibition
Substituted bis-(4-aminophenyl)-sulfones
-
, (2008/06/13)
Disclosed are substituted bis(4-aminophenyl)-sulfones of general formula STR1 wherein R1 is hydrogen, alkyl or cycloalkyl; group, R2 is hydrogen or C1 -C3 alkyl, R3 is nitrile, C1 -C3 alkylaminocarbonyl, di C1 -C3 alkylaminocarbonyl, C3 -C7 N-cycloalkyl-C1 -C3 alkylaminocarbonyl C1 -C3 alkylamino, C1 -C3, di alkylaminocarbonyl alkoxy, alkylaminosulfonyl, di C1 -C3 alkylaminono, diC1 -C3 alkylaminosulfonyl, hydroxy C1 -C3 alkyl, C1 -C3 alkylcarbonyl, amino C1 -C3 alkyl or C1 -C3 alkoxy C1 -C3 alkyl group or, when R1 and R2 are each hydrogen, R3 can be hydroxy, hydroxycarbonyl C1 -C3 alkoxy or di C1 -C3 aminocarbonylalkoxy; or, when R1 is C1 -C3 alkyl or C1 -C3 cycloalkyl and R2 is hydrogen or C1 -C3 alkyl, R3 can also be halogen, trifluoromethyl, nitro, amino, aminosulfonyl, aminocarbonyl, C1 -C3 alkyl, carboxy or C1 -C3 alkoxycarbonyl; and R4 is hydrogen or, when R1 and R2 are each hydrogen and R3 is halogen or hydroxy, R4 can also be halogen, hydroxy or C1 -C3 alkoxy; or a nontoxic, pharmaceutically acceptable salt thereof. Also disclosed are pharmaceutical compositions comprising such compounds alone and in combination with dihydrofolic acid-reductase inhibitors. The compounds and compositions are useful for their inhibiting effect on bacteria, mycobacteria and plasmodia.
