An article C3 amino-substituted chalcone derivative with selective adenosine rA(1) receptor affinity in the micromolar range WOS:000590271200001 published article about ALPHA-KETO ACIDS; DRUG DISCOVERY; ANTIPROLIFERATIVE ACTIVITY; BIOLOGICAL-ACTIVITIES; INTERNATIONAL UNION; SCREENING LIBRARIES; ANTAGONIST; INHIBITORS; BRAIN; BINDING in [Janse van Rensburg, Helena D.; Legoabe, Lesetja J.; Terre’Blanche, Gisella] North West Univ, Ctr Excellence Pharmaceut Sci, Private Bag X6001, ZA-2520 Potchefstroom, South Africa; [Terre’Blanche, Gisella] Northwest Univ, Sch Pharm, Pharmaceut Chem, Private Bag X6001, ZA-2520 Potchefstroom, South Africa in 2021.0, Cited 124.0. Quality Control of 3-Hydroxybenzaldehyde. The Name is 3-Hydroxybenzaldehyde. Through research, I have a further understanding and discovery of 100-83-4
To identify novel adenosine receptor (AR) ligands based on the chalcone scaffold, herein the synthesis, characterization and in vitro and in silico evaluation of 33 chalcones (15-36 and 37-41) and structurally related compounds (42-47) are reported. These compounds were characterized by radioligand binding and GTP shift assays to determine the degree and type of binding affinity, respectively, against rat (r) A(1) and A(2A) ARs. The chalcone derivatives 24, 29, 37 and 38 possessed selective A(1) affinity below 10 mu M, and thus, are the most active compounds of the present series; compound 38 was the most potent selective A(1) AR antagonist (K-i (r) = 1.6 mu M). The structure-affinity relationships (SAR) revealed that the NH2-group at position C3 of ring A of the chalcone scaffold played a key role in affinity, and also, the Br-atom at position C3 ‘ on benzylidene ring B. Upon in vitro and in silico evaluation, the novel C3 amino-substituted chalcone derivative 38-that contains an alpha,ss-unsaturated carbonyl system and easily allows structural modification-may possibly be a synthon in future drug discovery. [GRAPHICS] .
Quality Control of 3-Hydroxybenzaldehyde. About 3-Hydroxybenzaldehyde, If you have any questions, you can contact van Rensburg, HDJ; Legoabe, LJ; Terre’Blanche, G or concate me.
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