Inhibition of Bacterial Dihydrofolate Reductase by 6-Alkyl-2,4-diaminopyrimidines
نویسندگان
چکیده
منابع مشابه
Inhibition of dihydrofolate reductase by mofebutazon.
Mofebutazon, in contrast to phenylbutazon, inhibits dihydrofolate reductase in a concentration-dependent manner. An apparent Ki for mofebutazon and dihydrofolate reductase in the presence of NADPH as electron donor and dihydrofolate as electron acceptor of approximately 0.2 mM was calculated.
متن کاملEvolution of the bacterial dihydrofolate reductase inhibitors.
(1991). Effect of ampicillin-sulbactam on human polymorphnuclear leukocyte function. (1990). Effect of azithromycin, roxithromycin and erythromycin on human polymorphnuclear leukocyte function against Staphylococcus aureus.induced modification of the kinetics of growth of Gram-negative bacteria and susceptibility to phagocytic killing by human neutrophils. (1979). Effects of subminimal inhibito...
متن کاملBiochemical Activities of Propolis-Extracts m . Inhibition of Dihydrofolate Reductase
Elke Strehl, Regina Volpert, and Erich F. E lstner Institut für Botanik und Mikrobiologie, Biochemisches Labor, Technische Universität München, Arcisstraße 21, D-80290 München Z. Naturforsch. 49c, 39-43 (1994); received August 16/October 15,1993 Propolis, Dihydrofolate Reductase, Antiinflammatory Drugs, Caffeic Acid Ethanolic and aqueous extracts of the natural compound PROPOLIS indicate substa...
متن کاملBiochemical activities of propolis-extracts. III. Inhibition of dihydrofolate reductase.
Ethanolic and aqueous extracts of the natural compound PROPOLIS indicate substantial antiinflammatory functions as well as antibiotic activities in vitro and in vivo. The exact mode of physiological or biochemical mechanisms responsible for the medical effects, however, is all but clear. The standardization on the basis of quantitative determination of prominent components of these extracts hav...
متن کاملDevelopment of 2,4-diaminopyrimidines as antimalarials based on inhibition of the S108N and C59R+S108N mutants of dihydrofolate reductase from pyrimethamine-resistant Plasmodium falciparum.
The reduced binding of pyrimethamine to Ser108Asn (S108N) mutants of parasite dihydrofolate reductase (DHFR), which forms the basis of resistance of Plasmodium falciparum to pyrimethamine, is largely due to steric constraint imposed by the bulky side chain of N108 on Cl of the 5-p-Cl-phenyl group. This and other S108 mutants with bulky side chains all showed reduced binding to pyrimethamine and...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
ژورنال
عنوان ژورنال: ChemMedChem
سال: 2012
ISSN: 1860-7179
DOI: 10.1002/cmdc.201200291