Literature DB >> 22252809

In vitro and in vivo antimalarial activities of T-2307, a novel arylamidine.

Akiko Kimura1, Hiroshi Nishikawa, Nobuhiko Nomura, Junichi Mitsuyama, Shinya Fukumoto, Noboru Inoue, Shin-Ichiro Kawazu.   

Abstract

T-2307, a novel arylamidine, has been shown to exhibit broad-spectrum antifungal activities against clinically significant pathogens. Here, we evaluated the in vitro and in vivo antimalarial activity of T-2307. The 50% inhibitory concentrations (IC₅₀s) of T-2307 against Plasmodium falciparum FCR-3 and K-1 strains were 0.47 and 0.17 μM, respectively. T-2307 at 2.5 to 10 mg/kg of body weight/day exhibited activity against blood stage and liver stage parasites in rodent malaria models. In conclusion, T-2307 exhibited in vitro and in vivo antimalarial activity.

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Year:  2012        PMID: 22252809      PMCID: PMC3318391          DOI: 10.1128/AAC.05856-11

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


  15 in total

Review 1.  Drug discovery for malaria: a very challenging and timely endeavor.

Authors:  Michael H Gelb
Journal:  Curr Opin Chem Biol       Date:  2007-08       Impact factor: 8.822

2.  Diamidine compounds: selective uptake and targeting in Plasmodium falciparum.

Authors:  A M Stead; P G Bray; I G Edwards; H P DeKoning; B C Elford; P A Stocks; S A Ward
Journal:  Mol Pharmacol       Date:  2001-05       Impact factor: 4.436

3.  T-2307 shows efficacy in a murine model of Candida glabrata infection despite in vitro trailing growth phenomena.

Authors:  Eio Yamada; Hiroshi Nishikawa; Nobuhiko Nomura; Junichi Mitsuyama
Journal:  Antimicrob Agents Chemother       Date:  2010-06-14       Impact factor: 5.191

4.  Structure-activity relationships of analogs of pentamidine against Plasmodium falciparum and Leishmania mexicana amazonensis.

Authors:  C A Bell; J E Hall; D E Kyle; M Grogl; K A Ohemeng; M A Allen; R R Tidwell
Journal:  Antimicrob Agents Chemother       Date:  1990-07       Impact factor: 5.191

Review 5.  Malaria: progress, perils, and prospects for eradication.

Authors:  Brian M Greenwood; David A Fidock; Dennis E Kyle; Stefan H I Kappe; Pedro L Alonso; Frank H Collins; Patrick E Duffy
Journal:  J Clin Invest       Date:  2008-04       Impact factor: 14.808

Review 6.  Diamidines as antitrypanosomal, antileishmanial and antimalarial agents.

Authors:  Karl Werbovetz
Journal:  Curr Opin Investig Drugs       Date:  2006-02

7.  Disruption of the Plasmodium berghei 2-Cys peroxiredoxin TPx-1 gene hinders the sporozoite development in the vector mosquito.

Authors:  Kazuhiko Yano; Hitoshi Otsuki; Meiji Arai; Kanako Komaki-Yasuda; Takafumi Tsuboi; Motomi Torii; Shigeyuki Kano; Shin-Ichiro Kawazu
Journal:  Mol Biochem Parasitol       Date:  2008-03-13       Impact factor: 1.759

8.  Synchronization of Plasmodium falciparum erythrocytic stages in culture.

Authors:  C Lambros; J P Vanderberg
Journal:  J Parasitol       Date:  1979-06       Impact factor: 1.276

9.  In vitro and in vivo antifungal activities of T-2307, a novel arylamidine.

Authors:  Junichi Mitsuyama; Nobuhiko Nomura; Kyoko Hashimoto; Eio Yamada; Hiroshi Nishikawa; Makoto Kaeriyama; Akiko Kimura; Yozo Todo; Hirokazu Narita
Journal:  Antimicrob Agents Chemother       Date:  2008-01-28       Impact factor: 5.191

10.  A murine model of falciparum-malaria by in vivo selection of competent strains in non-myelodepleted mice engrafted with human erythrocytes.

Authors:  Iñigo Angulo-Barturen; María Belén Jiménez-Díaz; Teresa Mulet; Joaquín Rullas; Esperanza Herreros; Santiago Ferrer; Elena Jiménez; Alfonso Mendoza; Javier Regadera; Philip J Rosenthal; Ian Bathurst; David L Pompliano; Federico Gómez de las Heras; Domingo Gargallo-Viola
Journal:  PLoS One       Date:  2008-05-21       Impact factor: 3.240

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  1 in total

1.  Decarboxylative palladium(II)-catalyzed synthesis of aryl amidines from aryl carboxylic acids: development and mechanistic investigation.

Authors:  Jonas Rydfjord; Fredrik Svensson; Alejandro Trejos; Per J R Sjöberg; Christian Sköld; Jonas Sävmarker; Luke R Odell; Mats Larhed
Journal:  Chemistry       Date:  2013-08-28       Impact factor: 5.236

  1 in total

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