Synthesis and evaluation of phenoxymethylbenzamide analogues as anti-trypanosomal agents

被引：7
|
作者：
Manos-Turvey, Alexandra [1 ]
Watson, Emma E. [1 ]
Sykes, Melissa L. [2 ]
Jones, Amy J. [2 ]
Baell, Jonathan B. [3 ]
Kaiser, Marcel [4 ,5 ]
Avery, Vicky M. [2 ]
Payne, Richard J. [1 ]
机构：
[1] Univ Sydney, Sch Chem, Sydney, NSW 2006, Australia
[2] Griffith Univ, Eskitis Inst Drug Discovery, Discovery Biol, Nathan, Qld 4111, Australia
[3] Monash Univ, Monash Inst Pharmaceut Sci, Fac Pharm & Pharmaceut Sci, Dept Med Chem, Parkville, Vic, Australia
[4] Swiss Trop & Publ Hlth Inst, Basel, Switzerland
[5] Univ Basel, Basel, Switzerland
来源：
MEDCHEMCOMM | 2015年 / 6卷 / 03期
关键词：
HUMAN AFRICAN TRYPANOSOMIASIS; ORNITHINE-DECARBOXYLASE; STRAIN; 427; BRUCEI; DISCOVERY; TARGET; ENZYME; ASSAY; HTS;
D O I：
10.1039/c4md00406j
中图分类号：
Q5 [生物化学]; Q7 [分子生物学];
学科分类号：
071010 ; 081704 ;
摘要：
The synthesis and anti-trypanosomal activity of a compound library based on a phenoxymethylbenzamide hit discovered in a high throughput screen is described. Several of the analogues exhibited potent activity against Trypanosoma brucei rhodesiense, a human infective strain of the trypanosome parasite, that serve as lead compounds for further optimisation.
引用
收藏
页码：403 / 406
页数：4
相关论文
共 50 条
  • [1] Synthesis of cyclohexapeptides as antimalarial and anti-trypanosomal agents
    Pena, S.
    Fagundez, C.
    Medeiros, A.
    Comini, M.
    Scarone, L.
    Sellanes, D.
    Manta, E.
    Tulla-Puche, J.
    Albericio, F.
    Stewart, L.
    Yardleyh, V.
    Serra, G.
    MEDCHEMCOMM, 2014, 5 (09) : 1309 - 1316
  • [2] Analogues of thiolactomycin as potential anti-malarial and anti-trypanosomal agents
    Jones, SM
    Urch, JE
    Brun, R
    Harwood, JL
    Berry, C
    Gilbert, IH
    BIOORGANIC & MEDICINAL CHEMISTRY, 2004, 12 (04) : 683 - 692
  • [3] Generation of Anti-trypanosomal Agents through Concise Synthesis and Structural Diversification of Sesquiterpene Analogues
    Oguri, Hiroki
    Hiruma, Takahisa
    Yamagishi, Yutaka
    Oikawa, Hideaki
    Ishiyama, Aki
    Otoguro, Kazuhiko
    Yamada, Haruki
    Omura, Satoshi
    JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, 2011, 133 (18) : 7096 - 7105
  • [4] Synthesis and biological evaluation of selective tubulin inhibitors as anti-trypanosomal agents
    Bobba, Viharika
    Nanavaty, Vishal
    Idippily, Nethrie D.
    Zhao, Anran
    Li, Bibo
    Su, Bin
    BIOORGANIC & MEDICINAL CHEMISTRY, 2017, 25 (12) : 3215 - 3222
  • [5] Synthesis and biological evaluation of selective tubulin inhibitors as anti-trypanosomal agents
    Bobba, Viharika
    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2019, 257
  • [6] Synthesis and biological evaluation of imidamide analogs as selective anti-trypanosomal agents
    Bobba, Viharika
    Li, Yaxin
    Afrin, Marjia
    Dano, Raina
    Zhang, Wenjing
    Li, Bibo
    Su, Bin
    BIOORGANIC & MEDICINAL CHEMISTRY, 2022, 61
  • [7] Synthesis of precursors and macrocycle analogs of aerucyclamides as anti-trypanosomal agents
    Pena, Stella
    Scarone, Laura
    Medeiros, Andrea
    Manta, Eduardo
    Comini, Marcelo
    Serra, Gloria
    MEDCHEMCOMM, 2012, 3 (11) : 1443 - 1448
  • [8] Design, synthesis, and evaluation of novel anti-trypanosomal compounds
    Lepovitz, Lance T.
    Meis, Alan R.
    Thomas, Sarah M.
    Wiedeman, Justin
    Pham, Alexandra
    Mensa-Wilmot, Kojo
    Martin, Stephen F.
    TETRAHEDRON, 2020, 76 (16)
  • [9] Piperamides and their derivatives as potential anti-trypanosomal agents
    Fernando Cotinguiba
    Luis Octávio Regasini
    Vanderlan da Silva Bolzani
    Hosana Maria Debonsi
    Gabriela Duó Passerini
    Regina Maria Barretto Cicarelli
    Massuo Jorge Kato
    Maysa Furlan
    Medicinal Chemistry Research, 2009, 18 : 703 - 711
  • [10] Identification of indirubin derivatives as anti-trypanosomal agents
    Vougogiannopoulou, K.
    Gaboriaud-Kolar, N.
    Efstathiou, A.
    Soteriadou, K.
    Smirlis, D.
    Skaltsounis, L.
    PLANTA MEDICA, 2014, 80 (16) : 1437 - 1437
12345