80393-38-0Relevant academic research and scientific papers
Synthesis of imidazo[1,2-: C] thiazoles through Pd-catalyzed bicyclization of tert-butyl isonitrile with thioamides
Peng, Xiangjun,Qin, Feng,Xu, Mengyue,Zhu, Shaojie,Pan, Yingming,Tang, Haitao,Meng, Xiujin,Wang, Hengshan
supporting information, p. 8403 - 8407 (2019/09/30)
Building new biological molecules is challenging. Herein, imidazo[1,2-c]thiazoles were synthesized as a new class of heterobicyclic analogs through Pd-catalyzed cascade bicyclization from isonitriles with thioamides. The bicyclic scaffolds were constructed by inserting three molecules of isonitrile into two molecules of thioamide and then cyclizing them in a one-pot procedure. In vitro antitumor studies of these new compounds were conducted by using the MTT assay, and compound 3c showed excellent inhibitory effects against HepG2 at 7.06 ± 0.68 μM.
H2S-Donating Doxorubicins May Overcome Cardiotoxicity and Multidrug Resistance
Chegaev, Konstantin,Rolando, Barbara,Cortese, Daniela,Gazzano, Elena,Buondonno, Ilaria,Lazzarato, Loretta,Fanelli, Marilù,Hattinger, Claudia M.,Serra, Massimo,Riganti, Chiara,Fruttero, Roberta,Ghigo, Dario,Gasco, Alberto
supporting information, p. 4881 - 4889 (2016/06/13)
Doxorubicin (DOXO) is one of the most effective antineoplastic agents in clinical practice. Its use is limited by acute and chronic side effects, in particular by its cardiotoxicity and by the rapid development of resistance to it. As part of a program ai
SUBSTITUTED BENZAMIDES AND THEIR USES
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Paragraph 0567, (2015/12/01)
Provided herein are Substituted Benzamides, compositions, and method of their manufacture and use.
SUBSTITUTED BENZAMIDES AND THEIR USES
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Page/Page column 108, (2013/11/05)
Provided herein are Substituted Benzamides, compositions, and method of their manufacture and use.
A mild and versatile synthesis of thioamides
Mahammed,Jayashankara,Premsai Rai,Mohana Raju,Arunachalam
experimental part, p. 2338 - 2340 (2009/12/08)
Aliphatic and aromatic nitriles react with thioacetic acid in the presence of calcium hydride to give the corresponding thioamides in good to excellent yields. The examples studied include haloaryl nitriles in which the halogen is facile towards SNAr reactions under other conditions. Georg Thieme Verlag Stuttgart.
Design, synthesis and evaluation of trifluoromethane sulfonamide derivatives as new potent and selective peroxisome proliferator-activated receptor α agonists
Faucher, Nicolas,Martres, Paul,Laroze, Alain,Pineau, Olivier,Potvain, Florent,Grillot, Didier
, p. 710 - 715 (2008/09/19)
Starting from the structure of 5, a two-step strategy was applied to identify a new generation of trifluoromethane sulfonamides as potent PPARα agonists. Synthesis, in vitro and in vivo evaluation of the most potent compound are reported.
Preparation of primary thioamides from nitriles using sodium hydrogen sulfide and diethylamine hydrochloride
Boys, Mark L.,Downs, Victoria L.
, p. 295 - 298 (2007/10/03)
Primary thioamides are prepared in moderate to excellent yields by treating nitriles with sodium hydrogen sulfide and diethylamine hydrochloride in an appropriate solvent with mild heating. Copyright Taylor & Francis LLC.
Synthesis of aromatic thioamide from nitrile without handling of gaseous hydrogen sulfide
Manaka, Akira,Sato, Masakazu
, p. 761 - 764 (2007/10/03)
A new method for synthesizing aromatic primary thioamides is described. Simple treatment of aromatic nitriles with sodium hydrogen sulfide and magnesium chloride in dimethylformamide (DMF) gave aromatic primary thioamides in yields of 80-99% without handling of hazardous hydrogen sulfide.
Synthesis and biological activities of 4-phenyl-5-pyridyl-1,3-thiazole derivatives as p38 MAP kinase inhibitors
Miwatashi, Seiji,Arikawa, Yasuyoshi,Naruo, Ken-Ichi,Igaki, Keiko,Watanabe, Yasumasa,Kimura, Hiroyuki,Kawamoto, Tomohiro,Ohkawa, Shigenori
, p. 410 - 418 (2007/10/03)
A novel series of 4-phenyl-5-pyridyl-1,3-thiazole analogues possessing potent in vitro inhibitory activity against p38 mitogen-activated protein kinase and the release of tumor necrosis factor-α (TNF-α) from human monocytic THP-1 cells stimulated by lipopolysaccharide has been identified. Subsequent structure-activity relationship (SAR) studies and optimization for absorption, distribution, metabolism, and elimination (ADME) profiles led to the identification of compounds 7g and 10b as orally active lead candidates that block the in vivo production of proinflammatory cytokine (TNF-α). In pharmacokinetic studies, compound 10b showed good oral administration in mice and demonstrated significant in vivo anti-inflammatory activity in an anti-collagen monoclonal antibody-induced arthritis mouse model (minimum effective dose (MED)=30 mg/kg). Further elucidation of this class of compounds may provide novel anti-inflammatory agents, such as anti-rheumatoid arthritis drugs.
ARYL DICARBOXAMIDES
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Page/Page column 46-47, (2010/02/10)
The present invention is related to aryl dicarboxamides of formula (I) and use thereof for the treatment and/or prevention of obesity and/or metabolic disorders mediated by insulin resistance or hyperglycernia, comprising diabetes type I and/or II, inadequate glucose tolerance, insulin resistance, hyperlipidemia, hypertriglyceridemia, hypercholes-terolemia, polycystic ovary syndrome (PCOS). In particular, the present invention is related to the use of aryl dicarboxamides of formula (I) to modulate, notably to inhibit the activity of PTPs. A is an airninocarbonyl moiety; Cy is an aryl, heteroaryl, aryl-heteroaryl, heteroaryl-aryl, aryl-aryl, cycloalkyl or heterocycle group; n is either 0 or 1; R1 and R2 are independently from each other is selected from the group consisting of hydrogen or C1-C6-alkyl; R4 and R5 are each independently from each other selected from the group consisting of H, hydroxy, C1-C6 alkyl, carboxy, C1-C6 alkoxy, C1-C3 alkyl carboxy, C2-C3 alkenyl carboxy, C2-C3 alkynyl carboxy, amino or R4 and R5 may form an unsaturated or saturated heterocyclic ring, whereby at least one of R4 or R5 is not a hydrogen or C1-C6 alkyl.
