3382-80-7Relevant academic research and scientific papers
Novel 1,3,4-thiadiazole compounds as potential MAO-A inhibitors-design, synthesis, biological evaluation and molecular modelling
Kaplancikli, Zafer Asim,Levent, Serkan,Osmaniye, Derya,?zkay, Yusuf,Acar ?evik, Ulviye,Kaya ?avu?o?lu, Betül,Sa?lik, Begüm Nurpelin
, p. 1063 - 1074 (2020/10/06)
Monoamine oxidases (MAOs) are important drug targets for the management of neurological disorders. Herein, a series of new 1,3,4-thiadiazole derivatives bearing various alkyl/arylamine moieties as MAO inhibitors were designed and synthesized. All of the compounds were more selective against hMAO-A than hMAO-B. The half maximal inhibitory concentration (IC50) values of most of the compounds were lower than that of the common drug moclobemide (IC50 = 4.664 μM) and compound 6b was proven to be the most active compound (IC50 = 0.060 μM). Moreover, it was seen that compound 6b showed a similar inhibition profile to that of clorgyline (IC50 = 0.048 μM). The inhibition profile was found to be reversible and competitive for compound 6b with MAO-A selectivity. Molecular modelling studies aided in the understanding of the interaction modes between compound 6b and MAO-A. Furthermore, this compound was predicted to have a good pharmacokinetic profile and high BBB penetration. Therefore, such compounds are of interest towards developing new MAO inhibitors.
Synthesis of some novel 2-substituted benzothiazole derivatives containing benzylamine moiety as monoamine oxidase inhibitory agents
Kaya, Betül,Sa?l?k, Begüm Nurpelin,Levent, Serkan,?zkay, Yusuf,Kaplanc?kl?, Zafer As?m
, p. 1654 - 1661 (2016/10/09)
In the present work, 12 new 2-(5-substituted-benzothiazol-2-ylsulfanyl)-N-(substitutedbenzyl)-N-(4-substitutedphenyl) acetamide derivatives (4a–l) was designed and synthesized. The structures of the synthesized compounds were clarified using Fourier trans
Schiff bases as potential fungicides and nitrification inhibitors
Aggarwal, Nisha,Kumar, Rajesh,Dureja, Prem,Rawat, Diwan S.
experimental part, p. 8520 - 8525 (2010/08/03)
A number of substituted Schiff bases were synthesized and characterized by 1H NMR and mass spectrometry. These compounds were screened for antifungal activity In vitro against pathogenic fungi, namely, Sclerotium rolfsll and Rhizoctonia batatlcola, and fo
Imino Diels-Alder reactions: Efficient synthesis of 2-aryl-4-(2'- oxopyrrolidinyl-1')-1,2,3,4-tetrahydroquinolines catalyzed by Antimony(III) Sulfate
Srinivasa, Aswathanarayana,Mahadevan, Kittappa M.,Hulikal, Vijaykumar
experimental part, p. 255 - 259 (2009/05/26)
Antimony(III) sulfate is found to catalyze the imino Diels-Alder reaction of Schiff's bases with N-vinylpyrrolidin-2-one to afford 2-aryl-4-(2'- oxopyrrolidinyl-1')-1,2,3,4-tetrahydroquinolines. One-pot synthesis of 1,2,3,4-tetrahydroquinolines from 3-nit
