Dihydrofolate reductase inhibitors among pteridine and fu-ro[3,2-g]pteridine derivatives
نویسندگان
چکیده
Keywords: DHFR-inhibiting activity, pteridine, furo[3,2-g]pteridine, molecular docking, QSAR-analysis
منابع مشابه
The roles of pteridine reductase 1 and dihydrofolate reductase-thymidylate synthase in pteridine metabolism in the protozoan parasite Leishmania major.
Trypanosomatid protozoans depend upon exogenous sources of pteridines (pterins or folates) for growth. A broad spectrum pteridine reductase (PTR1) was recently identified in Leishmania major, whose sequence places it in the short chain alcohol dehydrogenase protein family although its enzymatic activities resemble dihydrofolate reductases. The properties of PTR1 suggested a role in essential pt...
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There is an urgent need for the development of new drugs to treat Chagas' disease, which is caused by the protozoan parasite Trypanosoma cruzi. The enzyme dihydrofolate reductase (DHFR) has been a very successful drug target in a number of diseases and we decided to investigate it as a potential drug target for Chagas' disease. A homology model of the enzyme was used to search the Cambridge Str...
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The binding of substrates and inhibitors to dihydrofolate reductase was studied by steady-state kinetics and high-field 1H-n.m.r. spectroscopy. A series of 5-substituted 2,4-diaminopyrimidines were examined and were found to be 'tightly binding' inhibitors of the enzyme (Ki less than 10(-9) M). Studies on the binding of 4-substituted benzenesulphonamides and benzenesulphonic acids also establis...
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The program DOCK3.5 was used to search the Cambridge Structural Database for novel inhibitors of Leishmanial dihydrofolate reductase. A number of compounds were obtained and screened against the enzyme and against the intact parasite Leishmania donovani and the related organisms Trypanosoma brucei and Trypanosoma cruzi. The compounds screened showed weak activity in both the enzyme assays and t...
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(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...
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ژورنال
عنوان ژورنال: Biopolymers & Cell
سال: 2021
ISSN: ['1993-6842', '0233-7657']
DOI: https://doi.org/10.7124/bc.000a51