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琥珀酰胺

琥珀酰胺结构式
琥珀酰胺结构式
品牌特惠专场
常用名 琥珀酰胺 英文名 Butanediamide
CAS号 110-14-5 分子量 116.11900
密度 1.207 g/cm3 沸点 494ºC at 760 mmHg
分子式 C4H8N2O2 熔点 260-265 °C (dec.)(lit.)
MSDS 中文版 美版 闪点 252.6ºC
符号 GHS07
GHS07
信号词 Warning

Effects of structural analogues of the substrate and allosteric regulator of the human mitochondrial NAD(P)+-dependent malic enzyme.

Bioorg. Med. Chem. 17 , 5414-9, (2009)

Fumarate, a four-carbon trans dicarboxylic acid, is the allosteric activator of the human mitochondrial NAD(P)(+)-dependent malic enzyme (m-NAD(P)-ME). In this paper, we discuss the effects of the structural analogues of fumarate on human m-NAD(P)-ME. Succina...

Synthesis of novel melanocortin 4 receptor agonists and antagonists containing a succinamide core.

Bioorg. Med. Chem. Lett. 14 , 377, (2004)

A novel series of piperazines appended to a succinamide backbone were synthesized and found to have a high affinity for the melanocortin-4 receptor (IC(50)s ranging from <0.1 to 200 nM). Both agonists and antagonists of MC4R were prepared by modifying the gro...

A disubstituted succinamide is a potent sodium channel blocker with efficacy in a rat pain model.

Biochemistry 43(30) , 9866-76, (2004)

Sodium channel blockers are used clinically to treat a number of neuropathic pain conditions, but more potent and selective agents should improve on the therapeutic index of currently used drugs. In a high-throughput functional assay, a novel sodium channel (...

Structure analysis reveals the flexibility of the ADAMTS-5 active site.

Protein Sci. 20(4) , 735-44, (2011)

A ((1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl) succinamide derivative (here referred to as Compound 12) shows significant activity toward many matrix metalloproteinases (MMPs), including MMP-2, MMP-8, MMP-9, and MMP-13. Modeling studies had predicted that th...

Adaptable synthesis of C-glycosidic multivalent carbohydrates and succinamide-linked derivatization.

Org. Lett. 12(22) , 5262-5, (2010)

A modular approach to the synthesis of trivalent C-glycosidic carbohydrates is described. The approach is illustrated employing carboxylate-terminated C-glycosidic d-mannose, d-glucose, and d-galactose derivatives with different length C1-linked spacer units ...

Synthesis of novel succinamide derivatives having the 5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one skeleton as potent and selective M2 muscarinic receptor antagonists. I.

Chem. Pharm. Bull. 45(6) , 996-1007, (1997)

A series of 5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one derivatives containing the succinamide skeleton has been synthesized and evaluated for M1, M2 and M3 muscarinic receptor binding affinities (in vitro) and M2 and M3 muscarinic receptor antagoni...

Synthesis of novel succinamide derivatives having a 5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one skeleton as potent and selective M2 muscarinic receptor antagonists. II.

Chem. Pharm. Bull. 45(9) , 1458-69, (1997)

A series of succinamide derivatives containing the 5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one skeleton (6a-z) was prepared and evaluated for binding affinity to muscarinic receptors in vitro and for antagonism of bradycardia and salivation in vivo ...

Discovery of selective metal-binding peptoids using 19F encoded combinatorial libraries.

Bioorg. Med. Chem. Lett. 10(18) , 2115-8, (2000)

A method for encoding solid-phase split/mix combinatorial libraries using the chemical shift of synthetic fluoroarenes ('F-codes') has been developed. They have wide chemical shift dispersion and are detectable at the sub-micromol level. 19F NMR is used for d...

Novel P2-P4 macrocyclic inhibitors of HCV NS3/4A protease by P3 succinamide fragment depeptidization strategy.

Bioorg. Med. Chem. Lett. 20(1) , 168-74, (2010)

Hepatitis C represents a serious worldwide health-care problem. Recently, we have disclosed a novel class of P2-P4 macrocyclic inhibitors of NS3/4A protease containing a carbamate functionality as capping group at the P3 N-terminus. Herein we report our work ...

Synthesis and SAR of succinamide peptidomimetic inhibitors of cathepsin S.

Bioorg. Med. Chem. Lett. 17(10) , 2899-903, (2007)

Peptidic, non-covalent inhibitors of lysosomal cysteine protease cathepsin S (1 and 2) were investigated due to low oral bioavailability, leading to an improved series of peptidomimetic inhibitors. Utilizing phenyl succinamides as the P2 residue increased the...