EurekaMag.com logo
+ Translate

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


, : 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

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.

(PDF 0-2 workdays service)

Accession: 002863126

PMID: 8851601

Submit PDF Full Text: Here


Submit PDF Full Text

No spam - Every submission is manually reviewed

Due to poor quality, we do not accept files from Researchgate

Submitted PDF Full Texts will always be free for everyone
(We only charge for PDFs that we need to acquire)

Select a PDF file:
Close
Close

Related references

Chio, L.C.; Bolyard, L.A.; Nasr, M.; Queener, S.F., 1996: Identification of a class of sulfonamides highly active against dihydropteroate synthase form Toxoplasma gondii, Pneumocystis carinii, and Mycobacterium avium. Sulfanilanilides with 3',5'-halogen substitutions had Ki values 6- to 57-fold lower than the Ki of sulfamethoxazole when tested against dihydropteroate synthase from Toxoplasma gondii. The compounds acted as competitive inhibitors. These...

Allegra C.; Boarman D.; Kovacs J.; Beaver J.; Lewis M.; Masur H.; Chabner B., 1988: Inhibition studies of dihydropteroate synthase dhps purified from toxoplasma gondii tg and pneumocystis carinii pc. Clinical Research 36(3): 548A

Brun-Pascaud, M.; Rajagopalan-Levasseur, P.; Chau, F.; Bertrand, G.; Garry, L.; Derouin, F.; Girard, P.M., 1998: Drug evaluation of concurrent Pneumocystis carinii, Toxoplasma gondii, and Mycobacterium avium complex infections in a rat model. We present a new experimental model for the simultaneous evaluation of the activities of drugs against Pneumocystis carinii, Toxoplasma gondii, and Mycobacterium avium complex infections. Rats latently infected with P. carinii were challenged with...

Brun Pascaud, M.; Bertrand, G.; Chau, F.; Rajagopalan Levasseur, P.; Derouin, F.; Girard, P.M.; Atzori, C.; Angeli, E.; Cargnel, A., 1997: 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

Brun Pascaud, M.; Bertrand, G.; Chau, F.; Rajagopalan Levasseur, P.; Garry, L.; Derouin, F.; Girard, P.M., 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

Rosowsky, A.; Fu, H.; Chan, D.C.M.; Queener, S.F., 2004: 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. Six previously undescribed N-(2,4-diaminopteridin-6-yl)methyldibenz (b,f) azepines with water-solubilizing O-carboxyalkyloxy or O-carboxybenzyloxy side chains at the 2'-position were synthesized and compared with trimethoprim (TMP) and piritr...

Voeller, D.; Kovacs, J.; Andrawis, V.; Chu, E.; Masur, H.; Allegra, C., 1994: Interaction of Pneumocystis carinii dihydropteroate synthase with sulfonamides and diaminodiphenyl sulfone (dapsone). The stability of dihydropteroate synthase, its kinetic constants with respect to substrates and the 50% inhibitory concentration (IC50) of several sulfonamides and the sulfone dapsone were characterized using both cell-free and intact organism ass...

Rosowsky, A.; Fu, H.; Chan, D., C.M.; Queener, S., F., 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. Six previously undescribed N-(2,4-diaminopteridin-6-yl)methyldibenz (b,f) azepines with water-solubilizing O-carboxyalkyloxy or O-carboxybenzyloxy side chains at the 2'-position were synthesized and compared with trimethoprim (TMP) and piritr...

Rosowsky, A.; Fu, H.; Chan, D.C.M.; Queener, S.F., 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. Six previously undescribed N-(2,4-diaminopteridin-6-yl)methyldibenz[b,f]azepines with water-solubilizing O-carboxyalkyloxy or O-carboxybenzyloxy side chains at the 2'-position were synthesized and compared with trimethoprim (TMP) and piritrex...

Rosowsky, A.; Chen, H.; Fu, H.; Queener, S.F., 2003: Synthesis of new 2,4-diaminopyrido pyrimidine and 2,4-diaminopyrrolo pyrimidine inhibitors of Pneumocystis carinii, Toxoplasma gondii, and Mycobacterium avium dihydrofolate reductase. A concise new route allowing easy access to five previously unreported 2,4-diamino-6-(substituted benzyl)pyrido(2,3-d)pyrimidines (2a-e) was developed, involving condensation of 2,4-dipivaloylamino-5-bromopyrido(2,3-d)pyrimidine (6) with an organo...