Synthesis and pharmacological evaluation of bis-3-(3,4-dichlorophenyl)acrylamide derivatives as glycogen phosphorylase inhibitors
-
Add time:07/16/2019 Source:sciencedirect.com
During our research using a high-throughput screening system for discovery of a new class of human liver glycogen phosphorylase a (hLGPa) inhibitors, a series of 3-(3,4-dichlorophenyl)acrylamide derivatives were synthesized, and their inhibitory activities toward hLGPa were evaluated. Among the derivatives, (2E,2′E)-N,N′-pentane-1,5-diylbis[3-(3,4-dichlorophenyl)acrylamide] (6c) inhibited hLGPa with an IC50 value of 0.023 μM. An X-ray crystallographic study of the enzyme–6c complex showed that the inhibitor is bound at the dimer interface site, where the 3,4-dichlorophenyl moiety interacts hydrophobically with the enzyme.
We also recommend Trading Suppliers and Manufacturers of 5-(3,4-DICHLOROPHENYL)-1H-PYRAZOLE-3-CARBOXYLIC ACID (cas 276684-04-9). Pls Click Website Link as below: cas 276684-04-9 suppliers
Prev:Pyrazinyl ureas revisited: 1-(3-(Benzyloxy)pyrazin-2-yl)-3-(3,4-dichlorophenyl)urea, a new blocker of Aβ-induced mPTP opening for Alzheimer's disease
Next:Pharmacokinetics and metabolism of 3,4-dichlorophenyl-propenoyl-sec.-butylamine in rats by high performance liquid chromatography–ion trap mass spectrometry) - 【Back】【Close 】【Print】【Add to favorite 】
- Related Information
- 1-Heteroaryl-6-(3,4-dichlorophenyl)-3-azabicyclo[4.1.0]heptane: Further insights into a class of triple re-uptake inhibitors07/21/2019
- Synthesis and characterisation a series of N-(3,4-dichlorophenyl)-N′-(2,3 and 4-methylbenzoyl)thiourea derivatives07/19/2019
- The antiviral compound 5-(3,4-dichlorophenyl) methylhydantoin inhibits the post-synthetic cleavages and the assembly of poliovirus in a cell-free system07/18/2019
- Pharmacokinetics and metabolism of 3,4-dichlorophenyl-propenoyl-sec.-butylamine in rats by high performance liquid chromatography–ion trap mass spectrometry07/17/2019
- Pyrazinyl ureas revisited: 1-(3-(Benzyloxy)pyrazin-2-yl)-3-(3,4-dichlorophenyl)urea, a new blocker of Aβ-induced mPTP opening for Alzheimer's disease07/15/2019
- Synthesis, crystal structures, molecular docking, and in vitro biological activities evaluation of transition metal complexes with 4-(3,4-dichlorophenyl) piperazine-1-carboxylic acid07/14/2019
- Synthesis and insect antifeedant activities of some substituted styryl 3,4-dichlorophenyl ketones07/13/2019
- Preparation of (S)-4-(1-(3,4-dichlorophenyl)-2-methoxyethyl)piperidine07/12/2019
- Interaction between 3,4‑dichlorophenyl‑propenoyl‑sec.‑butylamine (3,4‑DCPB), an antiepileptic drug, and cytochrome P450 in rat liver microsomes and recombinant human enzymes in vitro07/11/2019
