Literature DB >> 2445281

Activity of lipid-soluble inhibitors of dihydrofolate reductase against Pneumocystis carinii in culture and in a rat model of infection.

S F Queener1, M S Bartlett, M A Jay, M M Durkin, J W Smith.   

Abstract

Trimetrexate and BW301U (piritrexim isethionate), lipid-soluble inhibitors of dihydrofolate reductase, are potent inhibitors of the growth of Pneumocystis carinii in culture with WI-38 cells. Inhibition was observed with 0.1 microgram of trimetrexate or BW301U per ml. Trimethoprim is ineffective at 100 micrograms/ml in this culture system. Both trimetrexate and BW301U were effective as prophylactic agents against P. carinii pneumonia in rats; trimetrexate at 7.5 mg/kg protected 9 of 10 rats, and BW301U at 5 mg/kg protected 4 of 10.

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Year:  1987        PMID: 2445281      PMCID: PMC174935          DOI: 10.1128/AAC.31.9.1323

Source DB:  PubMed          Journal:  Antimicrob Agents Chemother        ISSN: 0066-4804            Impact factor:   5.191


  18 in total

1.  Latent Pneumocystis infection of rats, relapse, and chemotherapy.

Authors:  J K Frenkel; J T Good; J A Shultz
Journal:  Lab Invest       Date:  1966-10       Impact factor: 5.662

2.  Antimicrobial susceptibility of Pneumocystis carinii in culture.

Authors:  M S Bartlett; R Eichholtz; J W Smith
Journal:  Diagn Microbiol Infect Dis       Date:  1985-09       Impact factor: 2.803

3.  Successful treatment of lethal protozoal infections with the ornithine decarboxylase inhibitor, alpha-difluoromethylornithine.

Authors:  A Sjoerdsma; J A Golden; P J Schechter; J L Barlow; D V Santi
Journal:  Trans Assoc Am Physicians       Date:  1984

4.  2,4-diamino-5-methyl-6-[(3,4,5-trimethoxyanilino)methyl]quinazoline (tmq), a potent non-classical folate antagonist inhibitor--I effect on dihydrofolate reductase and growth of rodent tumors in vitro and in vivo.

Authors:  J R Bertino; W L Sawicki; B A Moroson; A R Cashmore; E F Elslager
Journal:  Biochem Pharmacol       Date:  1979-06-15       Impact factor: 5.858

Review 5.  Pentamidine for the treatment of Pneumocystis carinii pneumonia and other protozoal diseases.

Authors:  R D Pearson; E L Hewlett
Journal:  Ann Intern Med       Date:  1985-11       Impact factor: 25.391

6.  Activity of inosine analogs against Pneumocystis carinii in culture.

Authors:  M S Bartlett; J J Marr; S F Queener; R S Klein; J W Smith
Journal:  Antimicrob Agents Chemother       Date:  1986-07       Impact factor: 5.191

7.  Management of opportunistic infections complicating the acquired immunodeficiency syndrome.

Authors:  L S Young
Journal:  Med Clin North Am       Date:  1986-05       Impact factor: 5.456

8.  Dapsone-trimethoprim for Pneumocystis carinii pneumonia in the acquired immunodeficiency syndrome.

Authors:  G S Leoung; J Mills; P C Hopewell; W Hughes; C Wofsy
Journal:  Ann Intern Med       Date:  1986-07       Impact factor: 25.391

9.  Phase I studies with trimetrexate: clinical pharmacology, analytical methodology, and pharmacokinetics.

Authors:  J T Lin; A R Cashmore; M Baker; R N Dreyer; M Ernstoff; J C Marsh; J R Bertino; L R Whitfield; R Delap; A Grillo-Lopez
Journal:  Cancer Res       Date:  1987-01-15       Impact factor: 12.701

10.  Activity of antifolates against Pneumocystis carinii dihydrofolate reductase and identification of a potent new agent.

Authors:  C J Allegra; J A Kovacs; J C Drake; J C Swan; B A Chabner; H Masur
Journal:  J Exp Med       Date:  1987-03-01       Impact factor: 14.307

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  26 in total

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Authors:  S C Pegg; J J Haresco; I D Kuntz
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2.  Opportunistic infections in HIV-infected patients.

Authors:  S D Shafran
Journal:  Can J Infect Dis       Date:  1992-03

3.  Models for evaluating compounds for activity against Pneumocystis carinii.

Authors:  M S Bartlett
Journal:  Eur J Clin Microbiol Infect Dis       Date:  1991-03       Impact factor: 3.267

Review 4.  Pneumocystis carinii, an opportunist in immunocompromised patients.

Authors:  M S Bartlett; J W Smith
Journal:  Clin Microbiol Rev       Date:  1991-04       Impact factor: 26.132

5.  In vitro and in vivo immunomodulatory effects of anti-Pneumocystis carinii drugs.

Authors:  M Viora; A De Luca; A D'Ambrosio; A Antinori; E Ortona
Journal:  Antimicrob Agents Chemother       Date:  1996-05       Impact factor: 5.191

6.  Activity of clindamycin with primaquine against Pneumocystis carinii in vitro and in vivo.

Authors:  S F Queener; M S Bartlett; J D Richardson; M M Durkin; M A Jay; J W Smith
Journal:  Antimicrob Agents Chemother       Date:  1988-06       Impact factor: 5.191

7.  New rat model of Pneumocystis carinii infection.

Authors:  M S Bartlett; J A Fishman; S F Queener; M M Durkin; M A Jay; J W Smith
Journal:  J Clin Microbiol       Date:  1988-06       Impact factor: 5.948

8.  Close association of Pneumocystis carinii from infected rat lung with culture cells as shown by light and electron microscopy.

Authors:  M S Bartlett; M P Goheen; C H Lee; M M Shaw; M M Durkin; J W Smith
Journal:  Parasitol Res       Date:  1994       Impact factor: 2.289

9.  Pneumocystis carinii dihydrofolate reductase used to screen potential antipneumocystis drugs.

Authors:  M C Broughton; S F Queener
Journal:  Antimicrob Agents Chemother       Date:  1991-07       Impact factor: 5.191

10.  Structure-activity and structure-selectivity studies on diaminoquinazolines and other inhibitors of Pneumocystis carinii and Toxoplasma gondii dihydrofolate reductase.

Authors:  A Rosowsky; J B Hynes; S F Queener
Journal:  Antimicrob Agents Chemother       Date:  1995-01       Impact factor: 5.191

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