TY - JOUR KW - Dapsone KW - Dihydropteroate Synthase KW - Escherichia coli KW - Escherichia coli Infections KW - Humans KW - leprosy KW - Mycobacterium KW - Mycobacterium Infections KW - Tetrahydrofolate Dehydrogenase KW - Trimethoprim AU - Seydel J K AB -

New diaminodiphenylsulfone inhibitors of dihydropteroate synthase are described with increased inhibitory activity against mycobacteria and plasmodia, whereas their side effect of methemoglobin formation could be suppressed. The optimization of diaminobenzylpyrimidines, inhibitors of dihydrofolate reductase, led to derivatives with increased inhibitory effect against mycobacteria, especially M. leprae and plasmodia. Some of these derivatives show autosynergism. Finally the combination of brodimoprim (BDP) and dapsone (DDS) was developed for the treatment of leprosy. First clinical trials in Paraguay and Ethiopia show that combinations of BDP/DDS and BDP/DDS plus rifampicin were highly effective and may become an alternative multi-drug therapy for the treatment of leprosy. The tolerance of the regimens used was generally good.

BT - Journal of chemotherapy (Florence, Italy) C1 - http://www.ncbi.nlm.nih.gov/pubmed/8195833?dopt=Abstract DA - 1993 Dec IS - 6 J2 - J Chemother LA - eng N2 -

New diaminodiphenylsulfone inhibitors of dihydropteroate synthase are described with increased inhibitory activity against mycobacteria and plasmodia, whereas their side effect of methemoglobin formation could be suppressed. The optimization of diaminobenzylpyrimidines, inhibitors of dihydrofolate reductase, led to derivatives with increased inhibitory effect against mycobacteria, especially M. leprae and plasmodia. Some of these derivatives show autosynergism. Finally the combination of brodimoprim (BDP) and dapsone (DDS) was developed for the treatment of leprosy. First clinical trials in Paraguay and Ethiopia show that combinations of BDP/DDS and BDP/DDS plus rifampicin were highly effective and may become an alternative multi-drug therapy for the treatment of leprosy. The tolerance of the regimens used was generally good.

PY - 1993 SP - 422 EP - 9 T2 - Journal of chemotherapy (Florence, Italy) TI - In vitro and in vivo results of brodimoprim and analogues alone and in combination against E. coli and mycobacteria. VL - 5 SN - 1120-009X ER -