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Literature DB >> 11412992

Novel alkylpolyamine analogues that possess both antitrypanosomal and antimicrosporidial activity.

Y Zou¹, Z Wu, N Sirisoma, P M Woster, R A Casero, L M Weiss, D Rattendi, S Lane, C J Bacchi.

Abstract

A novel series of alkyl- or aralkyl-substituted polyamine analogues was synthesized containing a 3-7-3 polyamine backbone. These analogues were evaluated in vitro, and in one case in vivo, for activity as antitrypanosomal agents, and for activity against opportunistic infection caused by Microsporidia. Compound 21 inhibits trypanosomal growth with an IC(50) as low as 31nM, while compound 24 shows promising activity in vitro against trypanosomes, and against Microsporidia in vitro and in vivo.

Entities: Chemical Disease

Mesh：

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Year: 2001 PMID： 11412992 PMCID： PMC3109676 DOI： 10.1016/s0960-894x(01)00315-8

Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823

13 in total

Review 1. Terminally alkylated polyamine analogues as chemotherapeutic agents.

Authors: R A Casero; P M Woster
Journal: J Med Chem Date: 2001-01-04 Impact factor: 7.446

2. CD8+ CTLs are essential for protective immunity against Encephalitozoon cuniculi infection.

Authors: I A Khan; J D Schwartzman; L H Kasper; M Moretto
Journal: J Immunol Date: 1999-05-15 Impact factor: 5.422

Review 3. Parasite polyamine metabolism: targets for chemotherapy.

Authors: N Yarlett; C J Bacchi
Journal: Biochem Soc Trans Date: 1994-11 Impact factor: 5.407

4. TNP-470 is an effective antimicrosporidial agent.

Authors: C Coyle; M Kent; H B Tanowitz; M Wittner; L M Weiss
Journal: J Infect Dis Date: 1998-02 Impact factor: 5.226

5. Polyamine synthesis and interconversion by the Microsporidian Encephalitozoon cuniculi.

Authors: C J Bacchi; S Lane; L M Weiss; N Yarlett; P Takvorian; A Cali; M Wittner
Journal: J Eukaryot Microbiol Date: 2001 May-Jun Impact factor: 3.346

6. Polyamines with N-(3-phenylpropyl) substituents are effective competitive inhibitors of trypanothione reductase and trypanocidal agents.

Authors: Z Li; M W Fennie; B Ganem; M T Hancock; M Kobaslija; D Rattendi; C J Bacchi; M C O'Sullivan
Journal: Bioorg Med Chem Lett Date: 2001-01-22 Impact factor: 2.823

7. S-(5'-deoxy-5'-adenosyl)-1-aminoxy-4-(methylsulfonio)-2-cyclopentene (AdoMao): an irreversible inhibitor of S-adenosylmethionine decarboxylase with potent in vitro antitrypanosomal activity.

Authors: J Guo; Y Q Wu; D Rattendi; C J Bacchi; P M Woster
Journal: J Med Chem Date: 1995-05-12 Impact factor: 7.446

8. Preparation of the pure diastereomeric forms of S-(5'-deoxy-5'-adenosyl)-1-ammonio-4-methylsulfonio-2-cyclopentene and their evaluation as irreversible inhibitors of S-adenosylmethionine decarboxylase from Escherichia coli.

Authors: Y Q Wu; P M Woster
Journal: Bioorg Med Chem Date: 1993-11 Impact factor: 3.641

9. Experimental microsporidiosis in immunocompetent and immunodeficient mice and monkeys.

Authors: E S Didier; P W Varner; P J Didier; A M Aldras; N J Millichamp; M Murphey-Corb; R Bohm; J A Shadduck
Journal: Folia Parasitol (Praha) Date: 1994 Impact factor: 2.122

10. Antimalarial polyamine analogues.

Authors: M L Edwards; D M Stemerick; A J Bitonti; J A Dumont; P P McCann; P Bey; A Sjoerdsma
Journal: J Med Chem Date: 1991-02 Impact factor: 7.446

15 in total

Review 1. Recent advances in the development of polyamine analogues as antitumor agents.

Authors: Robert A Casero; Patrick M Woster
Journal: J Med Chem Date: 2009-08-13 Impact factor: 7.446

2. Antiprotozoal activity of 1-phenethyl-4-aminopiperidine derivatives.

Authors: Christophe Dardonville; Cristina Fernández-Fernández; Sarah-Louise Gibbons; Nadine Jagerovic; Lidia Nieto; Gary Ryan; Marcel Kaiser; Reto Brun
Journal: Antimicrob Agents Chemother Date: 2009-06-29 Impact factor: 5.191

Review 3. Current status of the polyamine research field.

Authors: Anthony E Pegg; Robert A Casero
Journal: Methods Mol Biol Date: 2011

4. Discovery of novel alkylated (bis)urea and (bis)thiourea polyamine analogues with potent antimalarial activities.

Authors: Bianca K Verlinden; Jandeli Niemand; Janette Snyman; Shiv K Sharma; Ross J Beattie; Patrick M Woster; Lyn-Marie Birkholtz
Journal: J Med Chem Date: 2011-09-14 Impact factor: 7.446

5. Polyamine-dependent activation of Rac1 is stimulated by focal adhesion-mediated Tiam1 activation.

Authors: Bertha C Elias; Sujoy Bhattacharya; Ramesh M Ray; Leonard R Johnson
Journal: Cell Adh Migr Date: 2010-07-14 Impact factor: 3.405

6. Interrogating alkyl and arylalkylpolyamino (bis)urea and (bis)thiourea isosteres as potent antimalarial chemotypes against multiple lifecycle forms of Plasmodium falciparum parasites.

Authors: Bianca K Verlinden; Marna de Beer; Boobalan Pachaiyappan; Ethan Besaans; Warren A Andayi; Janette Reader; Jandeli Niemand; Riette van Biljon; Kiplin Guy; Timothy Egan; Patrick M Woster; Lyn-Marie Birkholtz
Journal: Bioorg Med Chem Date: 2015-01-28 Impact factor: 3.641

10. Analysis of the beta-tubulin gene and morphological changes of the microsporidium Anncaliia algerae both suggest albendazole sensitivity.

Authors: Marianita Santiana; Cyrilla Pau; Peter M Takvorian; Ann Cali
Journal: J Eukaryot Microbiol Date: 2014-09-15 Impact factor: 3.346