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 Citations (Scopus)

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

Fingerprint

Polyamines
Microsporidia
Trypanosomiasis
Opportunistic Infections
Inhibitory Concentration 50
Growth
In Vitro Techniques
N-dodecyl-L-lysine amide

ASJC Scopus subject areas

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

Cite this

Novel alkylpolyamine analogues that possess both antitrypanosomal and antimicrosporidial activity. / Zou, Yu; Wu, Zhiqian; Sirisoma, Nilantha; Woster, Patrick M.; Casero, Robert A.; Weiss, Louis M.; Rattendi, Donna; Lane, Schennella; Bacchi, Cyrus J.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 11, No. 12, 18.06.2001, p. 1613-1617.

Research output: Contribution to journalArticle

Zou, Y, Wu, Z, Sirisoma, N, Woster, PM, Casero, RA, Weiss, LM, Rattendi, D, Lane, S & Bacchi, CJ 2001, 'Novel alkylpolyamine analogues that possess both antitrypanosomal and antimicrosporidial activity', Bioorganic and Medicinal Chemistry Letters, vol. 11, no. 12, pp. 1613-1617. https://doi.org/10.1016/S0960-894X(01)00315-8
Zou, Yu ; Wu, Zhiqian ; Sirisoma, Nilantha ; Woster, Patrick M. ; Casero, Robert A. ; Weiss, Louis M. ; Rattendi, Donna ; Lane, Schennella ; Bacchi, Cyrus J. / Novel alkylpolyamine analogues that possess both antitrypanosomal and antimicrosporidial activity. In: Bioorganic and Medicinal Chemistry Letters. 2001 ; Vol. 11, No. 12. pp. 1613-1617.
@article{b7701c71148f454d9e07cc8d358bfc3d,
title = "Novel alkylpolyamine analogues that possess both antitrypanosomal and antimicrosporidial activity",
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.",
author = "Yu Zou and Zhiqian Wu and Nilantha Sirisoma and Woster, {Patrick M.} and Casero, {Robert A.} and Weiss, {Louis M.} and Donna Rattendi and Schennella Lane and Bacchi, {Cyrus J.}",
year = "2001",
month = "6",
day = "18",
doi = "10.1016/S0960-894X(01)00315-8",
language = "English (US)",
volume = "11",
pages = "1613--1617",
journal = "Bioorganic and Medicinal Chemistry Letters",
issn = "0960-894X",
publisher = "Elsevier Limited",
number = "12",

}

TY - JOUR

T1 - Novel alkylpolyamine analogues that possess both antitrypanosomal and antimicrosporidial activity

AU - Zou, Yu

AU - Wu, Zhiqian

AU - Sirisoma, Nilantha

AU - Woster, Patrick M.

AU - Casero, Robert A.

AU - Weiss, Louis M.

AU - Rattendi, Donna

AU - Lane, Schennella

AU - Bacchi, Cyrus J.

PY - 2001/6/18

Y1 - 2001/6/18

N2 - 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.

AB - 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.

UR - http://www.scopus.com/inward/record.url?scp=0035907476&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=0035907476&partnerID=8YFLogxK

U2 - 10.1016/S0960-894X(01)00315-8

DO - 10.1016/S0960-894X(01)00315-8

M3 - Article

C2 - 11412992

AN - SCOPUS:0035907476

VL - 11

SP - 1613

EP - 1617

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

SN - 0960-894X

IS - 12

ER -