14396-89-5Relevant articles and documents
An Enzymatic Platform for Primary Amination of 1-Aryl-2-alkyl Alkynes
Liu, Zhen,Qin, Zi-Yang,Zhu, Ledong,Athavale, Soumitra V.,Sengupta, Arkajyoti,Jia, Zhi-Jun,Garcia-Borràs, Marc,Houk,Arnold, Frances H.
supporting information, p. 80 - 85 (2022/01/08)
Propargyl amines are versatile synthetic intermediates with numerous applications in the pharmaceutical industry. An attractive strategy for efficient preparation of these compounds is nitrene propargylic C(sp3)-H insertion. However, achieving this reacti
KCNT1 INHIBITORS AND METHODS OF USE
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Page/Page column 65-66, (2021/10/02)
The present invention is directed to, in part, compounds and compositions useful for preventing and/or treating a neurological disease or disorder, a disease or condition relating to excessive neuronal excitability, and/or a gain-of-function mutation in a gene (e.g., KCNT1). Methods of treating a neurological disease or disorder, a disease or condition relating to excessive neuronal excitability, and/or a gain-of-function mutation in a gene such as KCNT1 are also provided herein.
1-((1H-PYRAZOL-4-YL)METHYL)-3-(PHENYL)-1,3-DIHYDRO-2H-IMIDAZOL-2-ONE DERIVATIVES AND RELATED COMPOUNDS AS GPR139 ANTAGONISTS FOR THE TREATMENT OF E.G. DEPRESSION
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Paragraph 000414-000415, (2021/11/26)
The present invention refers to compounds of formula (I). The present invention also relates to compounds of formula (I) for use as G Protein coupled Receptor 139 (GPR139) antagonists in methods of medical treatment of e.g. depression, Alzheimer's disease
Synthesis and bioactivities of novel N-(4-(2-Aryloxythiazol-5-yl)but-3-yn- 2-yl)benzamides
Zhu, Youquan,Liu, Pei,Wang, Danyang,Zhang, Jin,Cheng, Jie,Ma, Yuan,Zou, Xiaomao,Yang, Huazheng
, p. 173 - 181 (2013/08/24)
A series of novel N-(4-(2-aryloxythiazol-5-yl)but-3-yn-2-yl)benzamide derivatives were designed and synthesized. Their structures were identified by 1H NMR and elemental analyses. Preliminary bioassays indicated that some title compounds provided >80% control of Sclerotinia sclerotiorum at 50 μg/mL and >70% herbicidal activities against B. campestris at 100 μg/mL. Their structure-activities relationships were also discussed. A series of novel N-(4-(2-aryloxythiazol-5-yl)but-3-yn-2-yl)benzamide derivatives were designed and synthesized. Some of them provided >80% control of Sclerotinia sclerotiorum at 50 μg/mL and >70% herbicidal activities against B. campestris at 100 μg/mL. Copyright
Kinetic resolution of propargylamines via a highly enantioselective non-enzymatic N-acylation process
Kolleth, Amandine,Christoph, Sarah,Arseniyadis, Stellios,Cossy, Janine
supporting information, p. 10511 - 10513,3 (2020/09/02)
The non-enzymatic kinetic resolution of diversely substituted primary propargylic amines is reported featuring a highly selective acetyl transfer using (1S,2S)-1 in conjunction with AliquatTM 336, affording the corresponding enantio-enriched N-
NOVEL ACETYL-COA CARBOXYLASE (ACC) INHIBITORS AND THEIR USE IN DIABETES, OBESITY AND METABOLIC SYNDROME
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Page/Page column 29, (2008/06/13)
The present invention relates to compounds of formula (I), which inhibit acetyl-CoA carboxylase (ACC) and are useful for the prevention or treatment of metabolic syndrome, type II diabetes, obesity, atherosclerosis and cardiovascular diseases in humans.
Synthesis and structure-activity relationships of N-{3-[2-(4-alkoxyphenoxy) thiazol-5-yl]-1-methylprop-2-ynyl}carboxy derivatives as selective acetyl-CoA carboxylase 2 inhibitors
Gu, Yu Gui,Weitzberg, Moshe,Clark, Richard F.,Xu, Xiangdong,Li, Qun,Zhang, Tianyuan,Hansen, T. Matthew,Liu, Gang,Xin, Zhili,Wang, Xiaojun,Wang, Rongqi,McNally, Teresa,Camp, Heidi,Beutel, Bruce A.,Sham, Hing L.
, p. 3770 - 3773 (2007/10/03)
A structurally novel acetyl-CoA carboxylase (ACC) inhibitor is identified from high-throughput screening. A preliminary structure-activity relationship study led to the discovery of potent dual ACC1/ACC2 and ACC2 selective inhibitors against human recombinant ACC1 and ACC2. Selective ACC2 inhibitors exhibited IC50 1000-fold selectivity against ACC1. (S)-Enantiomer 9p exhibited high ACC2 activity and lowered muscle malonyl-CoA dose-dependently in acute rodent studies, whereas (R)-enantiomer 9o was weak and had no effect on the malonyl-CoA level.
Synthesis of substituted Se-phenyl selenocarboxylates from terminal alkynes
Tiecco, Marcello,Testaferri, Lorenzo,Temperini, Andrea,Bagnoli, Luana,Marini, Francesca,Santi, Claudio,Terlizzi, Raffaella
, p. 3447 - 3458 (2007/10/03)
Se-Phenyl selenocarboxylates have been conveniently prepared from (phenylseleno)acetylenes by treatment with p-toluenesulfonic acid monohydrate in dichloromethane. This easy conversion is compatible with a broad range of oxygen- and nitrogen-containing functional groups. The Se-phenyl selenocarboxylates were easily converted into the corresponding esters and amides. Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2004.
Psychoactive propargylamine derivatives used in the treatment of anxiety, psychotic states or aggression
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, (2008/06/13)
Propargylamine derivatives having the general formula: STR1 wherein R is a hydrogen atom, an unsubstituted phenyl group or a phenyl group substituted with halogen, trifluoromethyl, loweralkoxy, nitro, cyano, amido or N,N-diloweralkylamido, R1,
