20161-52-8Relevant articles and documents
β-Selective Aroylation of Activated Alkenes by Photoredox Catalysis
Lei, Zhen,Banerjee, Arghya,Kusevska, Elena,Rizzo, Eric,Liu, Peng,Ngai, Ming-Yu
supporting information, p. 7318 - 7323 (2019/04/30)
Late-stage synthesis of α,β-unsaturated aryl ketones remains an unmet challenge in organic synthesis. Reported herein is a photocatalytic non-chain-radical aroyl chlorination of alkenes by a 1,3-chlorine atom shift to form β-chloroketones as masked enones
Steric hindrance effect on the thermo- and photo-responsive properties of pyrene-based polymers
Liao, Junqiu,Liu, Shenglan,Yuan, Yongjie,Zhang, Hailiang
, p. 5698 - 5708 (2018/04/23)
In this work, the influence of the steric hindrance effect between a polymeric backbone and the side groups on the lower critical solution temperature (LCST)-type behavior and photodegradation behavior, respectively, has been carefully studied. A series o
PROPANE-1,3-DIONE DERIVATIVE OR ITS SALT
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Page/Page column 21, (2008/06/13)
Compounds useful as GnRH receptor antagonists are provided. The present inventors have further examined propane-1,3-dione derivatives and confirmed as a result that a propane-1,3-dione having 2-(1,3-dihydro-2H-benzimidazol-2-ylidene), or a compound which
ORGANIC COMPOUNDS
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Page/Page column 74-75, (2008/06/13)
Compounds of the formula (I) are inhibitors of protein tyrosine phosphatases (PTPases) and, thus, may be employed for the treatment of conditions mediated by PTPase activity. The compounds of the present invention may also be employed as inhibitors of other enzymes characterized with a phosphotyrosine binding region such as the SH2 domain. Accordingly, the compounds of formula (I) may be employed for prevention and/or treatment of insulin resistance associated with obesity, glucose intolerance, diabetes mellitus, hypertension and ischemic diseases of the large and small blood vessels, conditions that accompany type-2 diabetes, including hyperlipidemia, hypertriglyceridemia, atherosclerosis, vascular restenosis, irritable bowel syndrome, pancreatitis, adipose cell tumors and carcinomas such as liposarcoma, dyslipidemia, and other disorders where insulin resistance is indicated. In addition, the compounds of the present invention may be employed to treat and/or prevent cancer, osteoporosis, musculoskeletal, neurodegenerative and infectious diseases, and diseases involving inflammation and the immune system.
1,2-Dibenzamidobenzene inhibitors of human factor Xa
Herron, David K.,Goodson Jr., Theodore,Wiley, Michael R.,Weir, Leonard C.,Kyle, Jeffrey A.,Yee, Ying K.,Tebbe, Ann Louise,Tinsley, Jennifer M.,Mendel, David,Masters, John J.,Franciskovich, Jeffry B.,Sawyer, J. Scott,Beight, Douglas W.,Ratz, Andrew M.,Milot, Guy,Hall, Steven E.,Klimkowski, Valentine J.,Wikel, James H.,Eastwood, Brian J.,Towner, Richard D.,Gifford-Moore, Donetta S.,Craft, Trelia J.,Smith, Gerald F.
, p. 859 - 872 (2007/10/03)
High-throughput screening of a combinatorial library of diamidophenols yielded lead compounds with the ability to inhibit human factor Xa (fXa) at micromolar concentrations (e.g. compound 4, fXa apparent K(ass) = 0.64 x 106 L/mol). SAR studies in this novel structural series of fXa inhibitors showed that the phenolic hydroxyl group was not essential for activity. The best activity was found in substituted 1,2-dibenzamidobenzenes in which the phenyl group of one benzoyl group (A-ring) was substituted in the 4-position with relatively small lipophilic or polarizable groups such as methoxy, vinyl, or chloro and the phenyl group of the other benzoyl group (B-ring) was substituted in the 4-position with larger lipophilic groups such as tertbutyl or dimethylamino. The central phenyl ring (C-ring) tolerated a wide variety of substituents, but methoxy, methanesulfonamido, hydroxyl, and carboxyl substitution produced slightly higher levels of activity than other substituents when present in combination with favorable B-ring substitution. Methylation of the amide nitrogen atoms was found to greatly decrease activity. Compound 12 is the highest affinity fXa inhibitor in this group of compounds, having fXa apparent K(ass) = 25.5 x 106 L/mol, about 40x more active than the original lead. This lead series does not show potent inhibition of human thrombin. A model for the binding of these ligands to the fXa active site is proposed. The model is consistent with the observed SAR and can serve to guide future SAR studies.
