83490-20-4Relevant academic research and scientific papers
MRGPRX2 ANTAGONISTS FOR THE TREATMENT OF INFLAMMATORY DISORDERS
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Paragraph 00115; 00224, (2021/05/15)
The present disclosure is directed to use of MrgprX2 antagonists in the treatment of inflammatory disorders, e.g., inflammatory disorders of the skin. This invention is also directed to pharmaceutical compositions comprising a MrgprX2 antagonist and a pha
Investigations on substituted (2-aminothiazol-5-yl)(imidazo[1,2-a]pyridin-3-yl)methanones for the treatment of Alzheimer's disease
Sagar, Sneha R.,Singh, Devendra Pratap,Das, Rajesh D.,Panchal, Nirupa B.,Sudarsanam, Vasudevan,Nivsarkar, Manish,Vasu, Kamala K.
, (2021/03/06)
Alzheimer's disease (AD) is a neurodegenerative disease majorly affecting old age populations. Various factors that affect the progression of the disease include, amyloid plaque formation, neurofibrillary tangles, inflammation, oxidative stress, etc. Here
Pharmacological investigation of quinoxaline-bisthiazoles as multitarget-directed ligands for the treatment of Alzheimer's disease
Sagar, Sneha R.,Singh, Devendra Pratap,Das, Rajesh D.,Panchal, Nirupa B.,Sudarsanam, Vasudevan,Nivsarkar, Manish,Vasu, Kamala K.
, (2019/06/08)
Alzheimer's disease (AD) is the most prevalent disease of old age leading to dementia. Complex AD pathogenesis involves multiple factors viz. amyloid plaque formation, neurofibrillary tangles and inflammation. Herein we report of a new series of quinoxaline-bisthiazoles as multitarget-directed ligands (MTDLs) targeting BACE-1 and inflammation concurrently. Virtual screening of a library of novel quinoxaline-bisthiazoles was performed by docking studies. The most active molecules from the docking library were taken up for synthesis and characterized by spectral data. Compounds 8a-8n showed BACE-1 inhibition in micro molar range. One of the compounds, 8n showed BACE-1 inhibition at IC50 of 3 ± 0.07 μM. Rat paw edema inhibition in acute and chronic models of inflammation were obtained at 69 ± 0.45% and 55 ± 0.7%, respectively. Compound 8n also showed noteworthy results in AlCl3 induced AD model. The treated rats exhibited excellent antiamnesic, antiamyloid, antioxidant, and neuroprotective properties. Behavioural parameters suggested improved cognitive functions which further validates the testimony of present study. Moreover, compound 8n was found to have inherent gastrointestinal safety. This new string of quinoxaline-bisthiazoles were identified as effective lead for the generation of potent MTDLs and compound 8n was found to showcase qualities to tackle AD pathogenesis.
Oxazole-based drug molecule for hospital sterilization, and preparation method thereof
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Paragraph 0033; 0034; 0035; 0036; 0037; 0038; 0038, (2019/10/01)
The invention discloses an oxazole-based drug molecule for hospital sterilization, and a preparation method thereof, and belongs to the technical field of synthesis of antibacterial drugs. According to the technical scheme, the oxazole-based drug molecule
Discovery, Development, and SAR of Aminothiazoles as LIMK Inhibitors with Cellular Anti-Invasive Properties
Charles, Mark D.,Brookfield, Joanna L.,Ekwuru, Tennyson C.,Stockley, Martin,Dunn, John,Riddick, Michelle,Hammonds, Tim,Trivier, Elisabeth,Greenland, Gavin,Wong, Ai Ching,Cheasty, Anne,Boyd, Susan,Crighton, Diane,Olson, Michael F.
supporting information, p. 8309 - 8313 (2015/11/09)
As part of a program to develop a small molecule inhibitor of LIMK, a series of aminothiazole inhibitors were discovered by high throughput screening. Scaffold hopping and subsequent SAR directed development led to a series of low nanomolar inhibitors of LIMK1 and LIMK2 that also inhibited the direct biomarker p-cofilin in cells and inhibited the invasion of MDA MB-231-luc cells in a matrigel inverse invasion assay.
Efficient synthesis of new tetradentate ligands with potential applications for 64Cu PET-imaging
Bodio, Ewen,Julienne, Karine,Gouin, Sébastien G.,Faivre-Chauvet, Alain,Deniaud, David
body text, p. 924 - 927 (2011/03/20)
We wish to report the synthesis of new tetradentate ligands in less than 3 h in good to excellent yields from a commercially available compound using microwave-assisted technology. First tests of complexation showed a high ability of these ligands to chel
Utilization of a nitrogen-sulfur nonbonding interaction in the design of new 2-aminothiazol-5-yl-pyrimidines as p38α MAP kinase inhibitors
Lin, Shuqun,Wrobleski, Stephen T.,Hynes Jr., John,Pitt, Sidney,Zhang, Rosemary,Fan, Yi,Doweyko, Arthur M.,Kish, Kevin F.,Sack, John S.,Malley, Mary F.,Kiefer, Susan E.,Newitt, John A.,McKinnon, Murray,Trzaskos, James,Barrish, Joel C.,Dodd, John H.,Schieven, Gary L.,Leftheris, Katerina
scheme or table, p. 5864 - 5868 (2010/11/18)
The design, synthesis, and structure-activity relationships (SAR) of a series of 2-aminothiazol-5-yl-pyrimidines as novel p38α MAP kinase inhibitors are described. These efforts led to the identification of 41 as a potent p38α inhibitor that utilizes a un
Synthesis of nitrogen bicyclic scaffolds: Pyrimido[1,2-a]pyrimidine-2,6- diones
Grosjean, Sylvain,Triki, Smail,Meslin, Jean-Claude,Julienne, Karine,Deniaud, David
scheme or table, p. 9912 - 9924 (2011/02/22)
The multi-step synthesis of 1,3,7-trisubstituted pyrimido[1,2-a] pyrimidinediones starting from isothiocyanates is described. These nitrogen bicycles were prepared by an iterative sequence of functionalization/ cyclocondensation reactions. [4+2] Cycloaddition reactions took place between diazadienic chains and various acyl chlorides providing sophisticated heterobicycles.
A convenient synthesis of di- and trisubstituted 2-aminoimidazoles from 1-amidino-3-trityl-thioureas
Kaila, Jitendra C.,Baraiya, Arshi B.,Pandya, Amit N.,Jalani, Hitesh B.,Vasu, Kamala K.,Sudarsanam
scheme or table, p. 3955 - 3958 (2009/10/11)
Convenient synthesis of 2-amino-1,5-disubstituted and 2-amino-1,4,5-trisubstituted imidazoles has been reported using readily available starting materials and simple reagents under mild conditions. Guanylation of 1-amidino-3-trityl-thioureas 1 and 7 using
A novel, simple cyclocondensation reaction towards glycosyl triazines
Kikelj, Vincent,Julienne, Karine,Janvier, Pascal,Meslin, Jean-Claude,Deniaud, David
experimental part, p. 3453 - 3460 (2009/05/26)
Sugars bearing an isothiocyanate moiety at C-1 react with diazadienium iodide to afford glycosyl triazines that represent, through an easy cyclocondensation reaction step, a flexible entry to different nucleoside analogues. We herein demonstrate that this [4+2] cycloaddition reaction occurs with total regiocontrol and good yields. Subsequent transformation of the thiocarbonyl into a carbonyl, and nucleophilic substitution of the methylsulfanyl group by ammonia, yields the 5-azacytidine analogues. All compounds were fully characterised by IR, HRMS, and 13C and 1H NMR (COSY, HMBC and HMQC). Georg Thieme Verlag.
