52182-26-0Relevant academic research and scientific papers
Design, synthesis: Via a one-pot approach and molecular docking studies of novel pyrrolo[2,1- a] isoquinoline derivatives
Borra, Satheesh,Boruah, Dhruba Jyoti,Kathirvelan, Devarajan,Maurya, Ram Awatar,Yuvaraj, Panneerselvam
supporting information, p. 792 - 797 (2022/01/22)
This new investigation describes an efficient three-component approach for the stereoselective synthesis of pyrrolo[2,1-a]isoquinolines from readily available isatins, chalcones and 1,2,3,4-tetrahydroisoquinoline without using a metal catalyst or additive
Synthesis and Evaluation of Indatraline-Based Inhibitors for Trypanothione Reductase
Walton, Jeffrey G. A.,Jones, Deuan C.,Kiuru, Paula,Durie, Alastair J.,Westwood, Nicholas J.,Fairlamb, Alan H.
experimental part, p. 321 - 328 (2012/01/12)
The search for novel compounds of relevance to the treatment of diseases caused by trypanosomatid protozoan parasites continues. Screening of a large library of known bioactive compounds has led to several drug-like starting points for further optimisation. In this study, novel analogues of the monoamine uptake inhibitor indatraline were prepared and assessed both as inhibitors of trypanothione reductase (TryR) and against the parasite Trypanosoma brucei. Although it proved difficult to significantly increase the potency of the original compound as an inhibitor of TryR, some insight into the preferred substituent on the amine group and in the two aromatic rings of the parent indatraline was deduced. In addition, detailed mode of action studies indicated that two of the inhibitors exhibit a mixed mode of inhibition. Give these inhibitors a TryR: Indatraline is a CNS-active inhibitor of trypanothione reductase (TryR) revealed in a previous high-throughput screen. For this study we prepared analogues of indatraline and tested their capacity to inhibit TryR and the proliferation of Trypanosoma brucei cells. Inhibitors of micromolar potency with a mixed mode of inhibition were identified.
