Authors Mpitimpiti, AN; Petzer, JP; Petzer, A; Jordaan, JHL; Lourens, ACU in SPRINGER published article about PARKINSONS-DISEASE; IMMUNOSTIMULATORY ACTIVITY; COUMARIN DERIVATIVES; HIGH-POTENCY; 3-FORMYL-4-HYDROXYCOUMARIN; CONSTITUENTS; SAFINAMIDE; SCAFFOLD in [Mpitimpiti, Annah N.; Petzer, Jacobus P.; Petzer, Anel; Lourens, Anna C. U.] North West Univ, Ctr Excellence Pharmaceut Sci, Private Bag X6001, ZA-2520 Potchefstroom, South Africa; [Petzer, Jacobus P.; Petzer, Anel; Lourens, Anna C. U.] North West Univ, Sch Pharm, Pharmaceut Chem, Private Bag X6001, ZA-2520 Potchefstroom, South Africa; [Jordaan, Johannes H. L.] North West Univ, Res Focus Area Chem Resource Beneficiat, Private Bag X6001, ZA-2520 Potchefstroom, South Africa in 2019.0, Cited 57.0. Recommanded Product: Benzyl Alcohol. The Name is Benzyl Alcohol. Through research, I have a further understanding and discovery of 100-51-6
Based on reports that chromone compounds are good potency inhibitors of monoamine oxidase (MAO), the present study evaluates the effect of substitution with flexible side chains on the 3 position on MAO inhibition potency. Fifteen chromone derivatives were synthesised by reacting aromatic and aliphatic amines and alcohols with chromone 3-carboxylic acid in the presence of carbonyldiimidazole (CDI). This yielded chromane-2,4-dione and ester chromone derivatives. Generally, the esters exhibited weak MAO inhibition, while the chromane-2,4-dione derivatives showed promise as selective MAO-B inhibitors with IC50 values in the micromolar range. Compound 14b, 3-[(benzylamino)methylidene]-3,4-dihydro-2H-1-benzopyran-2,4-dione, was the most potent MAO-B inhibitor with an IC50 value of 638 mu M. This compound was shown to be a reversible and competitive MAO-B inhibitor with a K-i of 94 mu M. In conclusion, the effect of chain elongation and introduction of flexible substituents on position 3 of chromone were explored and the results showed that aminomethylidene substitution is preferable over ester substitution. Good potency MAO-B inhibitors may act as leads for the design and development of therapy for Parkinson’s disease where these agents reduce the central metabolism of dopamine. [GRAPHICS] .
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,Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles