Novel alkylpolyamine analogues that possess both antitrypanosomal and antimicrosporidial activity

Yu Zou, Zhiqian Wu, Nilantha Sirisoma, Patrick M. Woster, Robert A. Casero, Louis M. Weiss, Donna Rattendi, Schennella Lane, Cyrus J. Bacchi

Research output: Contribution to journalArticle

34 Scopus citations

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 IC50 as low as 31 nM, while compound 24 shows promising activity in vitro against trypanosomes, and against Microsporidia in vitro and in vivo.

Original languageEnglish (US)
Pages (from-to)1613-1617
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume11
Issue number12
DOIs
StatePublished - Jun 18 2001

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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    Zou, Y., Wu, Z., Sirisoma, N., Woster, P. M., Casero, R. A., Weiss, L. M., Rattendi, D., Lane, S., & Bacchi, C. J. (2001). Novel alkylpolyamine analogues that possess both antitrypanosomal and antimicrosporidial activity. Bioorganic and Medicinal Chemistry Letters, 11(12), 1613-1617. https://doi.org/10.1016/S0960-894X(01)00315-8