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

doi:10.1016/S0960-894X(01)00315-8

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

School of Medicine

Research output: Contribution to journal › Article › peer-review

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 language	English (US)
Pages (from-to)	1613-1617
Number of pages	5
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	11
Issue number	12
DOIs	https://doi.org/10.1016/S0960-894X(01)00315-8
State	Published - Jun 18 2001

ASJC Scopus subject areas

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

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

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@article{559d19cdf2894cecaaaedadb3e290754,

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.}",

note = "Funding Information: These studies were supported by National Institutes of Health Grants CA63552 (P.M.W.), CA85509 (P.M.W.), and AI 41398 (L.M.W., C.J.B.). Additional support was provided by a grant from the UNDP/World Health Organization, Tropical Disease Research Grant #960644 (P.M.W.), and a Pace University Scholarly Research Award (C.J.B.). The expert technical assistance of Mr. Benjamin Wei is gratefully acknowledged. ",

year = "2001",

month = jun,

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",

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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.

N1 - Funding Information: These studies were supported by National Institutes of Health Grants CA63552 (P.M.W.), CA85509 (P.M.W.), and AI 41398 (L.M.W., C.J.B.). Additional support was provided by a grant from the UNDP/World Health Organization, Tropical Disease Research Grant #960644 (P.M.W.), and a Pace University Scholarly Research Award (C.J.B.). The expert technical assistance of Mr. Benjamin Wei is gratefully acknowledged.

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.

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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

SN - 0960-894X

VL - 11

SP - 1613

EP - 1617

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 12

ER -

Novel alkylpolyamine analogues that possess both antitrypanosomal and antimicrosporidial activity

Abstract

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