59775-49-4Relevant academic research and scientific papers
Synthesis and comparison of biological activities of azetidinone, thiazolidinone and related compounds
Govindarajan,Beena,Bhat
, p. 259 - 264 (2003)
Recent discoveries of non-classical β-lactam antibiotics such as nocardicines, monobactams and thienamycin have stimulated much interest. Besides this, the unique feature of these strained molecules is that these heterocycles are becoming powerful buildin
Ultrasound-promoted solvent-free synthesis of some new α-aminophosphonates as potential antioxidants
Basha, Meson Haji,Rao, Kammela Prasada,Subramanyam, Chennamasetty
, p. 147 - 153 (2020)
Ultrasonic irradiation has been adopted in order to achieve an efficient synthesis of some novel α-aminophosphonates by Pudovik reaction. Major benefits of this method are as follows: Eco-friendly, free of catalyst, high yielding, uncomplicated work-up pr
Development of 1,3-thiazole analogues of imidazopyridines as potent positive allosteric modulators of GABAA receptors
Tikhonova, Tatyana A.,Rassokhina, Irina V.,Kondrakhin, Eugeny A.,Fedosov, Mikhail A.,Bukanova, Julia V.,Rossokhin, Alexey V.,Sharonova, Irina N.,Kovalev, Georgy I.,Zavarzin, Igor V.,Volkova, Yulia A.
, (2019/11/28)
Structure–activity relationship studies were conducted in the search for 1,3-thiazole isosteric analogs of imidazopyridine drugs (Zolpidem, Alpidem). Three series of novel γ-aminobutyric acid receptor (GABAAR) ligands belonging to imidazo[2,1-b]thiazoles, imidazo[2,1-b][1,3,4]thiadiazoles, and benzo[d]imidazo[2,1-b]thiazoles were synthesized and characterized as active agents against GABAAR benzodiazepine-binding site. In each of these series, potent compounds were discovered using a radioligand competition binding assay. The functional properties of highest-affinity compounds 28 and 37 as GABAAR positive allosteric modulators (PAMs) were determined by electrophysiological measurements. In vivo studies on zebrafish demonstrated their potential for the further development of anxiolytics. Using the OECD “Fish, Acute Toxicity Test” active compounds were found safe and non-toxic. Structural bases for activity of benzo[d]imidazo[2,1-b]thiazoles were proposed using molecular docking studies. The isosteric replacement of the pyridine nuclei by 1,3-thiazole, 1,3,4-thiadiazole, or 1,3-benzothiazole in the ring-fused imidazole class of GABAAR PAMs was shown to be promising for the development of novel hypnotics, anxiolytics, anticonvulsants, and sedatives drug-candidates.
Access to Amide from Aldimine via Aerobic Oxidative Carbene Catalysis and LiCl as Cooperative Lewis Acid
Wang, Guanjie,Fu, Zhenqian,Huang, Wei
supporting information, p. 3362 - 3365 (2017/07/13)
Herein, an efficient route to amides from aldimines via aza-Breslow intermediates through aerobic oxidative carbene catalysis with LiCl as a cooperative Lewis acid is described. Many of the obtained N-heteroarylamides feature biological activity. Ambient
Synthesis of Imidazo[2,1-b]thiazoles via Copper-Catalyzed A3-Coupling in Batch and Continuous Flow
Rassokhina, Irina V.,Tikhonova, Tatyana A.,Kobylskoy, Sergey G.,Babkin, Igor Yu.,Shirinian, Valerii Z.,Gevorgyan, Vladimir,Zavarzin, Igor V.,Volkova, Yulia A.
, p. 9682 - 9692 (2017/09/23)
A straightforward method for the synthesis of functionalized imidazo[2,1-b]thiazoles starting from benzaldehydes, 2-aminothiazoles, and alkynes under copper(I,II) catalysis was developed. The protocol allows the construction of a variety of aryl-substituted imidazo[2,1-b]benzothiazoles, -[2,1-b]thiazoles, and -[2,1-b][1,3,4]thiadiazoles. The reactions were easy to perform affording most of the desired products in 33-93% yields. The intensification of the process in a continuous-flow reactor increases the products' yields up to quantitative.
Heteroaryl substituted bis-trifluoromethyl carbinols as malonyl-CoA decarboxylase inhibitors
Cheng, Jie-Fei,Mak, Chi Ching,Huang, Yujin,Penuliar, Richard,Nishimoto, Masahiro,Zhang, Lin,Chen, Mi,Wallace, David,Arrhenius, Thomas,Chu, Donald,Yang, Guang,Barbosa, Miguel,Barr, Rick,Dyck, Jason R.B.,Lopaschuk, Gary D.,Nadzan, Alex M.
, p. 3484 - 3488 (2007/10/03)
A series of heteroaryl-substituted bis-trifluoromethyl carbinols were prepared and evaluated as malonyl-CoA decarboxylase (MCD) inhibitors. Some thiazole-based derivatives showed potent in vitro MCD inhibitory activities and significantly increased glucos
Design of new cognition enhancers: From computer prediction to synthesis and biological evaluation
Geronikaki, Athina A.,Dearden, John C.,Filimonov, Dmitrii,Galaeva, Irina,Garibova, Taissia L.,Gloriozova, Tatiana,Krajneva, Valentina,Lagunin, Alexey,Macaev, Fliur Z.,Molodavkin, Guenadij,Poroikov, Vladimir V.,Pogrebnoi, Serghei I.,Shepeli, Felix,Voronina, Tatiana A.,Tsitlakidou, Maria,Vlad, Liudmila
, p. 2870 - 2876 (2007/10/03)
To discover new cognition enhancers, a set of virtually designed synthesizable compounds from different chemical series was investigated using two computer-aided approaches. One of the approaches is prediction of biological activity spectra for substances
Cycloaddition Reactions and other Reactions of 2-(Sulphinylamino)thiazole
Ahmed, G. A.
, p. 525 - 528 (2007/10/03)
2-(Sulphinylamino)thiozole (1) on reaction with some dienes under Diels-Alder condition gave the cycloaddition products (2a,b).Compound 1 also underwent reaction with nitrile oxide to form 3H-1,2,3,5-oxathiadiazole-2-oxide (3).The reactivity of 1 tow
