EurekaMag.com logo
+ Site Statistics
References:
52,725,316
Abstracts:
28,411,598
+ Search Articles
+ Subscribe to Site Feeds
EurekaMag Most Shared ContentMost Shared
EurekaMag PDF Full Text ContentPDF Full Text
+ PDF Full Text
Request PDF Full TextRequest PDF Full Text
+ Follow Us
Follow on FacebookFollow on Facebook
Follow on TwitterFollow on Twitter
Follow on Google+Follow on Google+
Follow on LinkedInFollow on LinkedIn

+ Translate

Identification of a class of sulfonamides highly active against dihydropteroate synthase from Toxoplasma gondii, Pneumocystis carinii, and Mycobacterium avium


Antimicrobial Agents & Chemotherapy 40(3): 727-733
Identification of a class of sulfonamides highly active against dihydropteroate synthase from Toxoplasma gondii, Pneumocystis carinii, and Mycobacterium avium
Sulfanilanilides with 3',5'-halogen substitutions had K-i values 6- to 57-fold lower than the K-i of sulfamethoxazole when tested against dihydropteroate synthase from Toxoplasma gondii. The compounds acted as competitive inhibitors. These compounds were also active against dihydropteroate synthase from Pneumocystis carinii, Mycobacterium avium, and Escherichia coli but were not significantly more active than sulfamethoxazole. The compounds were significantly more active in culture than were standard agents. Against T. gondii in culture, 50% inhibitory concentrations were 7- to 30-fold lower than that of sulfadiazine; against P. carinii in culture, a concentration of 100 mu-M caused 33 to 95% inhibition of growth, compared with 9% inhibition with 100 mu-M sulfamethoxazole.


Accession: 002863126

PMID: 8851601



Related references

Identification of a class of sulfonamides highly active against dihydropteroate synthase form Toxoplasma gondii, Pneumocystis carinii, and Mycobacterium avium. Antimicrobial Agents and ChemoTherapy 40(3): 727-733, 1996

Inhibition studies of dihydropteroate synthase dhps purified from toxoplasma gondii tg and pneumocystis carinii pc. Clinical Research 36(3): 548A, 1988

Drug evaluation of concurrent Pneumocystis carinii, Toxoplasma gondii, and Mycobacterium avium complex infections in a rat model. Antimicrobial Agents and ChemoTherapy 42(5): 1068-1072, 1998

Activity of bilobalide against Pneumocystis carinii, Toxoplasma gondii, and Mycobacterium avium complex in a rat model of triple infection. Apmis 105(Suppl 77): 22-23, 1997

Rat model of concurrent Pneumocystis carinii, Toxoplasma gondii, and Mycobacterium avium complex infections for assessment of multiple prophylaxis. Apmis 105(Suppl 77): 21-22, 1997

Synthesis of 2,4-diamino-6- oxydibenz azepin-5-yl-methylpteridines as potent and selective inhibitors of Pneumocystis carinii, Toxoplasma gondii, and Mycobacterium avium dihydrofolate reductase. Journal of Medicinal Chemistry 47(10): 2475-2485, May 6, 2004

Interaction of Pneumocystis carinii dihydropteroate synthase with sulfonamides and diaminodiphenyl sulfone (dapsone). Journal of Infectious Diseases 169(2): 456-459, 1994

Synthesis of 2,4-diamino-6-(2'-O-(omega-carboxyalkyl)oxydibenz(b,f)azepin-5-yl)-methylpteridines as potent and selective inhibitors of Pneumocystis carinii, Toxoplasma gondii, and Mycobacterium avium dihydrofolate reductase. Journal of Medicinal Chemistry 47(10): 2475-2485, 2004

Synthesis of 2,4-diamino-6-[2'-O-(omega-carboxyalkyl)oxydibenz[b,f]azepin-5-yl]methylpteridines as potent and selective inhibitors of Pneumocystis carinii, Toxoplasma gondii, and Mycobacterium avium dihydrofolate reductase. Journal of Medicinal Chemistry 47(10): 2475-2485, 2004

Synthesis of new 2,4-diaminopyrido pyrimidine and 2,4-diaminopyrrolo pyrimidine inhibitors of Pneumocystis carinii, Toxoplasma gondii, and Mycobacterium avium dihydrofolate reductase. Bioorganic & Medicinal Chemistry 11(1): 59-67, 2 January, 2003