PMID- 9005816
OWN - NLM
STAT- MEDLINE
DCOM- 19970130
LR  - 20190905
IS  - 0365-6233 (Print)
IS  - 0365-6233 (Linking)
VI  - 329
IP  - 3
DP  - 1996 Mar
TI  - New antifolate 4,4'-diaminodiphenyl sulfone substituted 
      2,4-diamino-5-benzylpyrimidines. Proof of their dual mode of action and 
      autosynergism.
PG  - 161-8
AB  - 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 of both enzymes leads to autosynergism in whole cells in 
      the same way as known for combinations of sulfonamides with trimethoprim. The 
      inhibitory activity is demonstrated in cell-free systems of DHFR and SYN derived 
      from various species (M. lufu, E. coli, C. albicans) and in whole cell systems of 
      the mycobacterial strain M. lufu. The compounds are rare examples for the 
      combination of two mechanisms of action in one molecule.
FAU - Wiese, M
AU  - Wiese M
AD  - Forschungszentrum Borstel, Zentrum fur Medizin und Biowissenschaften, Germany.
FAU - Schmalz, D
AU  - Schmalz D
FAU - Seydel, J K
AU  - Seydel JK
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
PL  - Germany
TA  - Arch Pharm (Weinheim)
JT  - Archiv der Pharmazie
JID - 0330167
RN  - 0 (Bacterial Proteins)
RN  - 0 (Enzyme Inhibitors)
RN  - 0 (Folic Acid Antagonists)
RN  - 0 (Pyrimidines)
RN  - 17615-73-5 (SDDS)
RN  - 8W5C518302 (Dapsone)
RN  - EC 2.5.1.15 (Dihydropteroate Synthase)
SB  - IM
MH  - Bacterial Proteins/metabolism
MH  - Dapsone/*analogs & derivatives/chemical synthesis/pharmacology
MH  - Dihydropteroate Synthase/antagonists & inhibitors
MH  - Drug Synergism
MH  - Enzyme Inhibitors/chemical synthesis/*pharmacology
MH  - Folic Acid Antagonists/chemical synthesis/*pharmacology
MH  - Microbial Sensitivity Tests
MH  - Pyrimidines/chemical synthesis/*pharmacology
EDAT- 1996/03/01 00:00
MHDA- 1996/03/01 00:01
CRDT- 1996/03/01 00:00
PHST- 1996/03/01 00:00 [pubmed]
PHST- 1996/03/01 00:01 [medline]
PHST- 1996/03/01 00:00 [entrez]
AID - 10.1002/ardp.19963290309 [doi]
PST - ppublish
SO  - Arch Pharm (Weinheim). 1996 Mar;329(3):161-8. doi: 10.1002/ardp.19963290309.