Synthesis and antikinetoplastid activities of 3-substituted quinolinones derivatives

Davide Audisio; Samir Messaoudi; Sandrine Cojean; Jean François Peyrat; Jean Daniel Brion; Christian Bories; Françoise Huteau; Philippe M. Loiseau; Mouad Alami

doi:10.1016/j.ejmech.2012.03.003

Synthesis and antikinetoplastid activities of 3-substituted quinolinones derivatives

Davide Audisio
, Samir Messaoudi
, Sandrine Cojean
, Jean François Peyrat
, Jean Daniel Brion
, Christian Bories
, Françoise Huteau
, Philippe M. Loiseau
, Mouad Alami

CNRS
Université Paris-Saclay
Univ Paris-Sud

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

34 Citations (Scopus)

Abstract

A new family of quinolinone derivatives has been synthesized and evaluated for their antikinetoplastid activities against Leishmania donovani and Trypanosoma brucei brucei. Results from these structure-activity relationship studies enabled identification of compounds 3a and 4g as the most active compounds against L. donovani promastigotes and amastigotes parasites (IC ₅₀ values in a range of 2-11 μM). Additionally, compound 3b has emerged from this study as the most active compound in the series against T. b. brucei with a MEC value of 12 μM. These three compounds are worth of further in vivo evaluation.

Original language	English
Pages (from-to)	44-50
Number of pages	7
Journal	European Journal of Medicinal Chemistry
Volume	52
DOIs	https://doi.org/10.1016/j.ejmech.2012.03.003
Publication status	Published - 1 Jun 2012
Externally published	Yes

Keywords

Antiprotozoal
HSP90
Leishmania donovani
Quinolinone derivatives
Trypanosoma brucei brucei

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10.1016/j.ejmech.2012.03.003

Cite this

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title = "Synthesis and antikinetoplastid activities of 3-substituted quinolinones derivatives",

abstract = "A new family of quinolinone derivatives has been synthesized and evaluated for their antikinetoplastid activities against Leishmania donovani and Trypanosoma brucei brucei. Results from these structure-activity relationship studies enabled identification of compounds 3a and 4g as the most active compounds against L. donovani promastigotes and amastigotes parasites (IC 50 values in a range of 2-11 μM). Additionally, compound 3b has emerged from this study as the most active compound in the series against T. b. brucei with a MEC value of 12 μM. These three compounds are worth of further in vivo evaluation.",

keywords = "Antiprotozoal, HSP90, Leishmania donovani, Quinolinone derivatives, Trypanosoma brucei brucei",

author = "Davide Audisio and Samir Messaoudi and Sandrine Cojean and Peyrat, \{Jean Fran{\c c}ois\} and Brion, \{Jean Daniel\} and Christian Bories and Fran{\c c}oise Huteau and Loiseau, \{Philippe M.\} and Mouad Alami",

year = "2012",

month = jun,

day = "1",

doi = "10.1016/j.ejmech.2012.03.003",

language = "English",

volume = "52",

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journal = "European Journal of Medicinal Chemistry",

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publisher = "Elsevier Masson s.r.l.",

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TY - JOUR

T1 - Synthesis and antikinetoplastid activities of 3-substituted quinolinones derivatives

AU - Audisio, Davide

AU - Messaoudi, Samir

AU - Cojean, Sandrine

AU - Peyrat, Jean François

AU - Brion, Jean Daniel

AU - Bories, Christian

AU - Huteau, Françoise

AU - Loiseau, Philippe M.

AU - Alami, Mouad

PY - 2012/6/1

Y1 - 2012/6/1

N2 - A new family of quinolinone derivatives has been synthesized and evaluated for their antikinetoplastid activities against Leishmania donovani and Trypanosoma brucei brucei. Results from these structure-activity relationship studies enabled identification of compounds 3a and 4g as the most active compounds against L. donovani promastigotes and amastigotes parasites (IC 50 values in a range of 2-11 μM). Additionally, compound 3b has emerged from this study as the most active compound in the series against T. b. brucei with a MEC value of 12 μM. These three compounds are worth of further in vivo evaluation.

AB - A new family of quinolinone derivatives has been synthesized and evaluated for their antikinetoplastid activities against Leishmania donovani and Trypanosoma brucei brucei. Results from these structure-activity relationship studies enabled identification of compounds 3a and 4g as the most active compounds against L. donovani promastigotes and amastigotes parasites (IC 50 values in a range of 2-11 μM). Additionally, compound 3b has emerged from this study as the most active compound in the series against T. b. brucei with a MEC value of 12 μM. These three compounds are worth of further in vivo evaluation.

KW - Antiprotozoal

KW - HSP90

KW - Leishmania donovani

KW - Quinolinone derivatives

KW - Trypanosoma brucei brucei

U2 - 10.1016/j.ejmech.2012.03.003

DO - 10.1016/j.ejmech.2012.03.003

M3 - Article

C2 - 22472166

AN - SCOPUS:84860321069

SN - 0223-5234

VL - 52

SP - 44

EP - 50

JO - European Journal of Medicinal Chemistry

JF - European Journal of Medicinal Chemistry

ER -

Synthesis and antikinetoplastid activities of 3-substituted quinolinones derivatives

Abstract

Keywords

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