2000
DOI: 10.1542/pir.21-11-368
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Review of the Sulfonamides and Trimethoprim

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Cited by 27 publications
(7 citation statements)
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“…Sulphonamides are synthetic compounds based on the industrial dye sulfachrysoidine; 69 they are analogues of p-aminobenzoic acid (PABA) and inhibit folic acid biosynthesis via competitive inhibition of the enzyme dihydropteroate synthetase. 70,71 This competitive inhibition is bacteriostatic, disrupting DNA synthesis and bacterial growth.…”
Section: Sulphonamides (Two In Antibioticdb)mentioning
confidence: 99%
“…Sulphonamides are synthetic compounds based on the industrial dye sulfachrysoidine; 69 they are analogues of p-aminobenzoic acid (PABA) and inhibit folic acid biosynthesis via competitive inhibition of the enzyme dihydropteroate synthetase. 70,71 This competitive inhibition is bacteriostatic, disrupting DNA synthesis and bacterial growth.…”
Section: Sulphonamides (Two In Antibioticdb)mentioning
confidence: 99%
“…All three drugs induce both dose-related toxicity and hypersensitivity, adverse effects on liver, brain, kidney, gastrointestinal and haemopoietic systems. 18–21 The risk of aplastic anemia with the use of other antiepileptic drug like sodium valproate 11 phenytoin 12 and felbamate 22 were found in several case reports. We did not find any significant association of Phenytoin with aplastic anemia.…”
Section: Discussionmentioning
confidence: 99%
“…10 and 14) [88][89][90][91] and while they exhibited excellent ZBG properties for coordination, these moieties often suffer from permeability issues and were produced largely as tool compounds. As a result, more recent compounds utilise groups like hydroxamic acids (9, 11, and 12, this type of coordination is demonstrated in Figure 3B) [90][91][92][93][94][95] and geminal-diol (13) [96][97][98] for the coordination of Zn 2+ . Although targeting the Zn 2+ is essential, the approach raises challenges for selectivity of the parasite target over human homologuesparasite specific inhibitors therefore require the employment of specific interactions with the PfA-M1 S1 and S1 0 subsites [81].…”
Section: Pfa-m1 -Flexible Substrate Pockets Provide Key To Potencymentioning
confidence: 97%
“…Some of the earliest synthetic antimalarials targeted DHFR [11][12][13][14][15]. Cycloguanil (1) and pyrimethamine (Pyr) (2), date back to the 1940s [16,17] but long-term widespread use of these molecules has led to resistance through the evolution of multiple mutations in PfDHFR [18][19][20].…”
Section: Dihydrofolate Reductase -A Resistant Enzyme Made Sensitivementioning
confidence: 99%