Antileishmanial structure-activity relationships of synthetic phospholipids: In vitro and in vivo activities of selected derivatives

被引:13
|
作者
Seifert, Karin
Lemke, Andreas
Croft, Simon L.
Kayser, Oliver
机构
[1] Univ London London Sch Hyg & Trop Med, Dept Infect & Trop Dis, London WC1E 7HT, England
[2] Univ Groningen, Groningen, Netherlands
关键词
D O I
10.1128/AAC.00465-07
中图分类号
Q93 [微生物学];
学科分类号
071005 ; 100705 ;
摘要
Antileishmanial activities of 91 synthetic phospholipids against Leishmania donovani were evaluated in vitro and cytotoxicity assessed against two mammalian cell lines. Promising compounds were tested further in vivo. In vitro structure-activity relationships showed a positive contribution of head groups bearing ring systems (N-methylpiperidino and N-methylmorpholino) to antileishmanial activity.
引用
收藏
页码:4525 / 4528
页数:4
相关论文
共 50 条
  • [1] In vivo and in vitro activities of new L-Valine derivatives:: Structure-activity relationships
    Tsekova, Daniela
    Makakova, Emilia
    Alov, Petko
    Gorneva, Galina
    Pajeva, Ilza
    Tancheva, Lyubka
    Petkov, Vesselin
    [J]. JOURNAL OF PEPTIDE SCIENCE, 2008, 14 (08) : 82 - 82
  • [2] Antitrypanosomal and antileishmanial activities of flavonoids and their analogues:: In vitro, in vivo, structure-activity relationship, and quantitative structure-activity relationship studies
    Tasdemir, D
    Kaiser, M
    Brun, R
    Yardley, V
    Schmidt, TJ
    Tosun, F
    Rüedi, P
    [J]. ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, 2006, 50 (04) : 1352 - 1364
  • [3] Synthesis, antiepileptic effects, and structure-activity relationships of α-asarone derivatives: In vitro and in vivo neuroprotective effect of selected derivatives
    Zhang, Jian
    Mu, Keman
    Yang, Peng
    Feng, Xinqian
    Zhang, Di
    Fan, Xiangyu
    Wang, Qiantao
    Mao, Shengjun
    [J]. BIOORGANIC CHEMISTRY, 2021, 115
  • [4] 3D-Quantitative structure-activity relationships of synthetic antileishmanial ring-substituted ether phospholipids
    Kapou, Agnes
    Benetis, Nikolas P.
    Avlonitis, Nikos
    Calogeropoulou, Theodora
    Koufaki, Maria
    Scoulica, Efi
    Nikolaropoulos, Sotiris S.
    Mavromoustakos, Thomas
    [J]. BIOORGANIC & MEDICINAL CHEMISTRY, 2007, 15 (03) : 1252 - 1265
  • [5] Structure-Activity Relationships of Fish Oil Derivatives with Antiallergic Activity in Vitro and in Vivo
    Kim, In-Hae
    Kanayama, Yoshiki
    Nishiwaki, Hisashi
    Sugahara, Takuya
    Nishi, Kosuke
    [J]. JOURNAL OF MEDICINAL CHEMISTRY, 2019, 62 (21) : 9576 - 9592
  • [6] Antileishmanial Anthracene Endoperoxides: Efficacy In Vitro, Mechanisms and Structure-Activity Relationships
    Machin, Laura
    Piontek, Martin
    Todhe, Sara
    Staniek, Katrin
    Monzote, Lianet
    Fudickar, Werner
    Linker, Torsten
    Gille, Lars
    [J]. MOLECULES, 2022, 27 (20):
  • [7] Structure-activity relationships for In vitro and In vivo toxicity
    Blagg, Julian
    [J]. ANNUAL REPORTS IN MEDICINAL CHEMISTRY, VOL 41, 2006, 41 : 353 - 368
  • [8] Structure-activity relationships of antileishmanial and antimalarial chalcones
    Liu, M
    Wilairat, P
    Croft, SL
    Tan, ALC
    Go, ML
    [J]. BIOORGANIC & MEDICINAL CHEMISTRY, 2003, 11 (13) : 2729 - 2738
  • [9] Structure-activity relationships for the antileishmanial and antitrypanosomal activities of 1'-substituted 9-anilinoacridines
    Gamage, SA
    Figgitt, DP
    Wojcik, SJ
    Ralph, RK
    Ransijn, A
    Mauel, J
    Yardley, V
    Snowdon, D
    Croft, SL
    Denny, WA
    [J]. JOURNAL OF MEDICINAL CHEMISTRY, 1997, 40 (16) : 2634 - 2642
  • [10] Synthetic 2-Methoxyestradiol Derivatives: Structure-Activity Relationships
    Peyrat, Jean-Francois
    Brion, Jean-Daniel
    Alami, Mouad
    [J]. CURRENT MEDICINAL CHEMISTRY, 2012, 19 (24) : 4142 - 4156