20093-91-8

Upstream product

• 143-33-9 sodium cyanide 
• 19093-64-2 4'-Aminoflavone 
• 20093-73-6 terephthalic acid-(2-acetyl-phenyl ester)-methyl ester 
• 7377-26-6 4-Methoxycarbonylbenzoyl chloride 
• 20093-79-2 4-[3-(2-hydroxy-phenyl)-3-oxo-propionyl]-benzoic acid methyl ester 
• 55737-06-9 4-[3-(2-hydroxyphenyl)-3-oxopropenyl]benzoic acid 
• 619-66-9 4-Carboxybenzaldehyde 
• 118-93-4 o-hydroxyacetophenone 
• 7153-22-2 ethyl 4-cyanobenzoate 
• 20093-85-0 methyl 4-(4-oxo-4H-chromen-2-yl)benzoate 
• 55736-88-4 4-(4-oxo-4H-chromen-2-yl)benzonitrile 

Downstream Products

• 109697-00-9 4-(4-oxo-4H-chromen-2-yl)-benzoic acid ethyl ester 
• 20093-85-0 methyl 4-(4-oxo-4H-chromen-2-yl)benzoate 

Relevant academic research and scientific papers

Flavone-based hydrazones as new tyrosinase inhibitors: Synthetic imines with emerging biological potential, SAR, molecular docking and drug-likeness studies

Targeting tyrosinase (TYR), a key enzyme responsible for melanogenesis disorders, is a well-known approach utilized for the development of melanogenesis inhibitor. A variety of dermatological disorders and microbial skin infections can cause hyperpigmentation. Hence, exploring new scaffolds for the treatment of melanogenesis disease is an inspiring goal. In this context, a series of varyingly substituted flavone-based hydrazones have been designed, synthesized and characterized successfully. The present study describes the discovery of novel mushroom tyrosinase inhibitors (TIs) for treating hyperpigmentation. In due course, flavone scaffold has been incorporated into the novel chemotypes that exhibit in vitro inhibitory effects against mushroom tyrosinase for the purpose of discovering anti‐melanogenic agents. Biological investigations of prepared analogs herein demonstrated moderate to excellent activity against most of the fungal-bacterial strains and their activity is comparable to those of commercially available antibiotics i.e., Ciprofloxacin and Ketoconazole. Based on in vitro tyrosinase inhibitory assay, some compounds exhibited potent inhibition particularly, 3g (IC50 = 1.40 ± 0.16 μM), 3j (IC50 = 0.95 ± 0.07 μM), 3o (IC50 = 1.13 ± 0.11 μM), and 3q (IC50 = 1.01 ± 0.1 μM) showed best inhibition i.e., 0.7, 0.5, 0.6 and 0.5 folds, respectively, than kojic acid (IC50 = 1.79 ± 0.6 μM). Lineweaver-Burk plots demonstrated that the most potential derivative 3j tyrosinase inhibition proceeds via non-competitive pathway and the Michaelis-Menton constant (Km) value is 0.0265. Molecular modeling was performed for all tested analogs (3a–3q) using a model of mushroom tyrosinase to find crucial binding modes liable for inhibitory activity. The SARs were preliminarily examined, and the docking study revealed that analogs 3j, 3o and 3p had a strong binding association to tyrosinase (2Y9X). Furthermore, a drug-likeness study was employed and confirmed the favorable activity of the new analogs as a new anti-tyrosinase agent.

Synthesis of chromen-4-one-oxadiazole substituted analogs as potent β-glucuronidase inhibitors

Chromen-4-one substituted oxadiazole analogs 1–19 have been synthesized, characterized and evaluated for β-glucuronidase inhibition. All analogs exhibited a variable degree of β-glucuronidase inhibitory activity with IC50 values ranging in betw

Synthesis of novel flavone hydrazones: In-vitro evaluation of α-glucosidase inhibition, QSAR analysis and docking studies

Thirty derivatives of flavone hydrazone (5e34) had been synthesized through a five-step reaction and screened for their a-glucosidase inhibition activity. Chalcone 1 was synthesized through aldol condensation then subjected through oxidative cyclization,

Retinobenzoic Acids. Structure-Activity Relationships of Chalcone-4-carboxylic Acids and Flavone-4'-carboxylic Acids

The structure-activity relationships of (E)-chalcone-4-carboxylic acids, which are retinoidal benzoic acids represented by R-Ph-X-Ph-COOH (4, X=-COCH=CH-), are discussed on the basis of differentiation-inducing activity on human promyelocytic leukemia cells HL-60.The activity was increased by the substitution of a bulky alkyl group(s) (R), and among such compounds, (E)-4-benzoic acid (Ch55) and (E)-4-benzoic acid (Ch80) are several times more active than retinoic acid.Though the stable conformer of chalcone derivatives is linear (s-cis form), the conformationally restricted analogue 4-(6,7,8,9-tetrahydro-6,6,9,9-tetramethyl-4H-4-oxonaphthopyran-2-yl)benzoic acid (Fv80) is more active than Ch80.While the effect of introduction of an oxygen atom varied, 4-benzoic acid (Re80), regarded as a derivative of Ch80 with two additional hydroxyl groups, has very strong activity.