Literature DB >> 18271517

Highly water-soluble prodrugs of anthelmintic benzimidazole carbamates: synthesis, pharmacodynamics, and pharmacokinetics.

C Chassaing1, M Berger, A Heckeroth, T Ilg, M Jaeger, C Kern, K Schmid, M Uphoff.   

Abstract

Highly water-soluble prodrugs 1a- g of anthelmintic benzimidazole carbamates 2a- g were synthesized. These prodrugs combine high aqueous solubility and stability with high lability in the presence of alkaline phosphatases. The veterinary utility of 1a was shown by a pharmacodynamic and pharmacokinetic study performed in swine. Comparable anthelmintic efficacy was observed with prodrug 1a or the parent fenbendazole 2a. The pharmacokinetic results showed that 2a is better absorbed when derived from 1a than when applied as such.

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Year:  2008        PMID： 18271517     DOI： 10.1021/jm701456r

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  10 in total

1.  Synthesis, characterization, DNA binding and cleavage studies of mixed-ligand Cu(II) complexes of 2,6-bis(benzimidazol-2-yl)pyridine.

Authors:  M Sunita; M Padmaja; B Anupama; C Gyana Kumari
Journal:  J Fluoresc       Date:  2012-05       Impact factor: 2.217

2.  Sorption of thiabendazole in sub-tropical Brazilian soils.

Authors:  Odilon França de Oliveira Neto; Alejandro Yopasa Arenas; Anne Hélène Fostier
Journal:  Environ Sci Pollut Res Int       Date:  2017-05-29       Impact factor: 4.223

3.  Discovery and Characterization of a Water-Soluble Prodrug of a Dual Inhibitor of Bacterial DNA Gyrase and Topoisomerase IV.

Authors:  Hardwin O'Dowd; Dean E Shannon; Kishan R Chandupatla; Vaishali Dixit; Juntyma J Engtrakul; Zhengqi Ye; Steven M Jones; Colleen F O'Brien; David P Nicolau; Pamela R Tessier; Jared L Crandon; Bin Song; Dainius Macikenas; Brian L Hanzelka; Arnaud Le Tiran; Youssef L Bennani; Paul S Charifson; Anne-Laure Grillot
Journal:  ACS Med Chem Lett       Date:  2015-06-22       Impact factor: 4.345

4.  Systematic structure modifications of multitarget prostate cancer drug candidate galeterone to produce novel androgen receptor down-regulating agents as an approach to treatment of advanced prostate cancer.

Authors:  Puranik Purushottamachar; Abhijit M Godbole; Lalji K Gediya; Marlena S Martin; Tadas S Vasaitis; Andrew K Kwegyir-Afful; Senthilmurugan Ramalingam; Zeynep Ates-Alagoz; Vincent C O Njar
Journal:  J Med Chem       Date:  2013-06-07       Impact factor: 7.446

5.  (2-{[2-(1H-Benzimidazol-2-yl-κN)phen-yl]imino-methyl-κN}-5-methyl-phenolato-κO)chloridozinc(II).

Authors:  Naser Eltaher Eltayeb; Siang Guan Teoh; Suchada Chantrapromma; Hoong-Kun Fun
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2011-08-02

6.  2-(5,6-Dihydro-benzimidazo[1,2-c]quinazolin-6-yl)-5-meth-oxy-phenol.

Authors:  Naser Eltaher Eltayeb; Siang Guan Teoh; Suchada Chantrapromma; Hoong-Kun Fun
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2011-08-27

7.  [2-(1H-Benzimidazol-2-yl-κN)aniline-κN]dichloridozinc.

Authors:  Naser Eltaher Eltayeb; Siang Guan Teoh; Suchada Chantrapromma; Hoong-Kun Fun
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2011-07-09

8.  Crystal structure of aqua-bis-[2-(1H-benzimidazol-2-yl-κN (3))aniline-κN]zinc dinitrate.

Authors:  Yongtae Kim; Sung Kwon Kang
Journal:  Acta Crystallogr E Crystallogr Commun       Date:  2015-03-14

9.  3-O-Carbamoyl-5,7,20-O-trimethylsilybins: Synthesis and Preliminary Antiproliferative Evaluation.

Authors:  Sitong Wu; Guanglin Chen; Qiang Zhang; Guangdi Wang; Qiao-Hong Chen
Journal:  Molecules       Date:  2021-10-24       Impact factor: 4.411

10.  Novel compound shows in vivo anthelmintic activity in gerbils and sheep infected by Haemonchus contortus.

Authors:  Elora Valderas-García; Nerea Escala; María Álvarez-Bardón; Verónica Castilla-Gómez de Agüero; Maria Cambra-Pellejà; Laura González Del Palacio; Raquel Vallejo García; Jennifer de la Vega; Arturo San Feliciano; Esther Del Olmo; María Martínez-Valladares; Rafael Balaña-Fouce
Journal:  Sci Rep       Date:  2022-07-29       Impact factor: 4.996
  10 in total

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