Literature DB >> 9714224

Dicationic furans inhibit development of Cryptosporidium parvum in HSD/ICR suckling Swiss mice.

B L Blagburn1, K L Drain, T M Land, P H Moore, R G Kinard, D S Lindsay, A Kumar, J Shi, D W Boykin, R R Tidwell.   

Abstract

The efficacy of dicationic diarylfurans was evaluated against Cryptosporidium parvum by a suckling murine model. Candidate drugs were solubilized or suspended in deionized water and administered orally at a constant dose rate on days 0-5 (treatment day 0) to suckling ICR Swiss mice experimentally inoculated with oocysts of C. parvum. Efficacy was based on numbers of oocysts recovered from the intestinal tracts of mice subjected to necropsy examination on day 6. Numerous candidate furans significantly reduced the numbers of oocysts recovered from treated mice compared with control mice. Compounds 1, 2, 4, and 9 demonstrated superior efficacies (10% of controls or better) against C. parvum. Compounds 3, 5, 6, 7, 8, 11, 17, 18, and 19 also significantly reduced the numbers of oocysts recovered from treated mice but demonstrated efficacies ranging from 17 to 65% of controls. Compound 4 was particularly efficacious against C. parvum at a dosage as low as 8.5 mg/kg of body weight. Compound 4 is identified as a lead compound for additional studies in other animal models.

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Year:  1998        PMID: 9714224

Source DB:  PubMed          Journal:  J Parasitol        ISSN: 0022-3395            Impact factor:   1.276


  8 in total

1.  Antileishmanial activities of several classes of aromatic dications.

Authors:  James J Brendle; Abram Outlaw; Arvind Kumar; David W Boykin; Donald A Patrick; Richard R Tidwell; Karl A Werbovetz
Journal:  Antimicrob Agents Chemother       Date:  2002-03       Impact factor: 5.191

2.  Dicyclic and tricyclic diaminopyrimidine derivatives as potent inhibitors of Cryptosporidium parvum dihydrofolate reductase: structure-activity and structure-selectivity correlations.

Authors:  R G Nelson; A Rosowsky
Journal:  Antimicrob Agents Chemother       Date:  2001-12       Impact factor: 5.191

3.  Efficacy of clofazimine and nitazoxanide combination in treating intestinal cryptosporidiosis and enhancing intestinal cellular regeneration in immunocompromised mice.

Authors:  Marwa Esmat; Amany A Abdel-Aal; Maisa A Shalaby; Manal Badawi; Hala Elaskary; Ahmed Badawi Yousif; Mennat-Elrahman A Fahmy
Journal:  Food Waterborne Parasitol       Date:  2022-05-04

4.  Comparative efficacy evaluation of dicationic carbazole compounds, nitazoxanide, and paromomycin against Cryptosporidium parvum infections in a neonatal mouse model.

Authors:  B L Blagburn; K L Drain; T M Land; R G Kinard; P H Moore; D S Lindsay; D A Patrick; D W Boykin; R R Tidwell
Journal:  Antimicrob Agents Chemother       Date:  1998-11       Impact factor: 5.191

5.  Host cells participate in the in vitro effects of novel diamidine analogues against tachyzoites of the intracellular apicomplexan parasites Neospora caninum and Toxoplasma gondii.

Authors:  Angela Leepin; Angela Stüdli; Reto Brun; Chad E Stephens; David W Boykin; Andrew Hemphill
Journal:  Antimicrob Agents Chemother       Date:  2008-03-24       Impact factor: 5.191

Review 6.  Novel amidines and analogues as promising agents against intracellular parasites: a systematic review.

Authors:  M N C Soeiro; K Werbovetz; D W Boykin; W D Wilson; M Z Wang; A Hemphill
Journal:  Parasitology       Date:  2013-04-08       Impact factor: 3.234

7.  In vitro antifungal activities of a series of dication-substituted carbazoles, furans, and benzimidazoles.

Authors:  M Del Poeta; W A Schell; C C Dykstra; S K Jones; R R Tidwell; A Kumar; D W Boykin; J R Perfect
Journal:  Antimicrob Agents Chemother       Date:  1998-10       Impact factor: 5.191

8.  Direct inhibition of the DNA-binding activity of POU transcription factors Pit-1 and Brn-3 by selective binding of a phenyl-furan-benzimidazole dication.

Authors:  Paul Peixoto; Yang Liu; Sabine Depauw; Marie-Paule Hildebrand; David W Boykin; Christian Bailly; W David Wilson; Marie-Hélène David-Cordonnier
Journal:  Nucleic Acids Res       Date:  2008-04-25       Impact factor: 16.971

  8 in total

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