Synthesis and in vitro protozoocidal evaluation of novel diazabicyclic tropolone derivatives

Alexander Khrizman; Rachel D. Slack; Richard C. Remsing; Susan Little; Vanessa Yardley; Guillermo Moyna

doi:10.1002/ardp.200700143

Synthesis and in vitro protozoocidal evaluation of novel diazabicyclic tropolone derivatives

Alexander Khrizman, Rachel D. Slack, Richard C. Remsing, Susan Little, Vanessa Yardley, Guillermo Moyna

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

10 Scopus citations

Abstract

The synthesis and in vitro antiparasitic activity of twenty-seven novel diazabicycles based on tropolone ethers is presented. The compounds can be readily prepared by means of a high-yielding hetero Diels-Alder reaction using simple and readily available starting materials. Several of the new diazabicycles have in vitro activities against Trypanosoma cruzi, Leishmania donovani, Trypanosoma brucei rhodesiense, and chloroquine-resistant Plasmodium falciparum that are comparable or superior to those of currently employed protozoocidal agents.

Original language	English (US)
Pages (from-to)	569-576
Number of pages	8
Journal	Archiv der Pharmazie
Volume	340
Issue number	11
DOIs	https://doi.org/10.1002/ardp.200700143
State	Published - Nov 2007
Externally published	Yes

All Science Journal Classification (ASJC) codes

Pharmaceutical Science
Drug Discovery

Keywords

Hydrazynes
Parasitoses
Protozoocidal activity
Synthesis
Tropolone derivatives

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10.1002/ardp.200700143

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title = "Synthesis and in vitro protozoocidal evaluation of novel diazabicyclic tropolone derivatives",

abstract = "The synthesis and in vitro antiparasitic activity of twenty-seven novel diazabicycles based on tropolone ethers is presented. The compounds can be readily prepared by means of a high-yielding hetero Diels-Alder reaction using simple and readily available starting materials. Several of the new diazabicycles have in vitro activities against Trypanosoma cruzi, Leishmania donovani, Trypanosoma brucei rhodesiense, and chloroquine-resistant Plasmodium falciparum that are comparable or superior to those of currently employed protozoocidal agents.",

keywords = "Hydrazynes, Parasitoses, Protozoocidal activity, Synthesis, Tropolone derivatives",

author = "Alexander Khrizman and Slack, {Rachel D.} and Remsing, {Richard C.} and Susan Little and Vanessa Yardley and Guillermo Moyna",

year = "2007",

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doi = "10.1002/ardp.200700143",

language = "English (US)",

volume = "340",

pages = "569--576",

journal = "Archiv der Pharmazie",

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TY - JOUR

T1 - Synthesis and in vitro protozoocidal evaluation of novel diazabicyclic tropolone derivatives

AU - Khrizman, Alexander

AU - Slack, Rachel D.

AU - Remsing, Richard C.

AU - Little, Susan

AU - Yardley, Vanessa

AU - Moyna, Guillermo

PY - 2007/11

Y1 - 2007/11

N2 - The synthesis and in vitro antiparasitic activity of twenty-seven novel diazabicycles based on tropolone ethers is presented. The compounds can be readily prepared by means of a high-yielding hetero Diels-Alder reaction using simple and readily available starting materials. Several of the new diazabicycles have in vitro activities against Trypanosoma cruzi, Leishmania donovani, Trypanosoma brucei rhodesiense, and chloroquine-resistant Plasmodium falciparum that are comparable or superior to those of currently employed protozoocidal agents.

AB - The synthesis and in vitro antiparasitic activity of twenty-seven novel diazabicycles based on tropolone ethers is presented. The compounds can be readily prepared by means of a high-yielding hetero Diels-Alder reaction using simple and readily available starting materials. Several of the new diazabicycles have in vitro activities against Trypanosoma cruzi, Leishmania donovani, Trypanosoma brucei rhodesiense, and chloroquine-resistant Plasmodium falciparum that are comparable or superior to those of currently employed protozoocidal agents.

KW - Hydrazynes

KW - Parasitoses

KW - Protozoocidal activity

KW - Synthesis

KW - Tropolone derivatives

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DO - 10.1002/ardp.200700143

M3 - Article

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AN - SCOPUS:36549077336

SN - 0365-6233

VL - 340

SP - 569

EP - 576

JO - Archiv der Pharmazie

JF - Archiv der Pharmazie

IS - 11

ER -

Synthesis and in vitro protozoocidal evaluation of novel diazabicyclic tropolone derivatives

Abstract

All Science Journal Classification (ASJC) codes

Keywords

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