70909-46-5

Upstream product

• 95-92-1 oxalic acid diethyl ester 
• 1131-62-0 1-(3,4-dimethoxyphenyl)ethanone 

Downstream Products

• 1105191-08-9 C₁₂H₁₃NO₄ 
• 1018662-99-1 C₁₂H₁₁NO₄ 
• 371157-17-4 ethyl 5-(3,4-dimethoxyphenyl)-isoxazole-3-carboxylate 
• 79183-93-0 4-(3,4-dimethoxy-phenyl)-2,4-dioxo-butyric acid 

Relevant academic research and scientific papers

Synthesis and Biological Screening of Novel 5-(5-Aryl-1-phenyl-1H-pyrazol-3-yl)-3-aryl-1,2,4-oxadiazole Derivatives

A new series of 5-(5-aryl-1-phenyl-1H-pyrazol-3-yl)-3-aryl-1,2,4-oxadiazole (6a-o) have been synthesized by a cyclocondensation reaction of ethyl 5-(4-chlorophenyl)-1-phenyl-1H-pyrazole-3-carboxylate (3a-c) with aryl imidoxime (5a-e). The newly synthesize

Novel N-benzylpiperidine derivatives of 5-arylisoxazole-3-carboxamides as anti-Alzheimer's agents

The complex pathophysiology of Alzheimer's disease (AD) has prompted researchers to develop multitarget-directed molecules to find an effective therapy against the disease. In this context, a novel series of N-(1-benzylpiperidin-4-yl)-5-arylisoxazole-3-ca

Design and synthesis of novel 5-arylisoxazole-1,3,4-thiadiazole hybrids as α-glucosidase inhibitors

Background: α-Glucosidase inhibitors have occupied a significant position in the treatment of type 2 diabetes. In this respect, the development of novel and efficient non-sugar-based inhibitors is in high demand. Objective: Design and synthesis of new 5-arylisoxazole-1,3,4-thiadiazole hybrids possessing α-glucosidase inhibitory activity were developed. Methods: Different derivatives were synthesized by the reaction of various 5-arylisoxazole-3-carboxylic acids and ethyl 2-((5-amino-1,3,4-thiadiazol-2-yl)thio)acetate. Finally, they were evalu-ated for their α-glucosidase inhibitory activity. Results: It was found that ethyl 2-((5-(5-(2-chlorophenyl)isoxazole-3-carboxamido)-1,3,4-thiadiazol-2-yl)thio)acetate (5j) was the most potent compound (IC50 = 180.1 μM) compared with acarbose as the reference drug (IC50 = 750.0 μM). Also, the kinetic study of 5j revealed a competitive inhibition and docking study results indicated desired interactions of that compound with amino acid residues located close to the active site of α-glucosidase. Conclusion: Good α-glucosidase inhibitory activity obtained by the title compounds introduced them as an efficient scaffold, which merits to be considered in anti-diabetic drug discovery developments.

THIADIAZINE DERIVATIVES

The invention relates to thiadiazine derivatives, or pharmaceutically acceptable salts, biologically active metabolites, pro-drugs, racemates, enantiomers, diastereomers, solvates and hydrates thereof, as well as to pharmaceutical compositions containing

Design and Synthesis of Novel Arylisoxazole-Chromenone Carboxamides: Investigation of Biological Activities Associated with Alzheimer's Disease

A novel series of hybrid arylisoxazole-chromenone carboxamides were designed, synthesized, and evaluated for their cholinesterase (ChE) inhibitory activity based on the modified Ellman's method. Among synthesized compounds, 5-(3-nitrophenyl)-N-{4-[(2-oxo-

Green and efficient synthesis of new pyrido[2,3-d]pyrimidine derivatives using Pd/SBA-15 as a nanocatalyst

N-Fused heterocycles have received significant attention over the years as valuable compounds due to their biological and pharmaceutical activities. Heterogeneous catalysts such as periodic mesoporous materials have played an important role in the synthes

The First Example of Azole-Fused Cyclic Anhydride Reacting in the Castagnoli-Cushman Way

Pyrazole-fused cyclic anhydrides have been employed for the first time as the Castagnoli-Cushman reaction partners to produce hitherto unknown 4-oxo-4,5,6,7-tetrahydropyrazolo[1,5- a ]pyrazine-7-carboxylates in remarkably convenient and speedy fashion. At

Novel hybrid molecules of isoxazole chalcone derivatives: Synthesis and study of In Vitro cytotoxic activities

Background: Now-a-days, the model of “hybrid drugs” has acquired recognition in medicine due to their significant role in the treatment of different health problems. Methods: We have synthesized new series of isoxazole-chalcone conjugates (14a-m) by the C

Synthesis, Characterization and biological applications of pyrazole-benzothiazolamine conjugates

Present paper describes the synthesis of some new pyrazole-benzothiazolamine conjugates by molecular conjunction by adopting appropriate synthetic routes. Purification of intermediates and final compounds has been done by recrystallization and chromatographic techniques. Characterization of all the newly synthesized pyrazole-benzothiazolamine derivatives was done by physical and spectral data. The experimental procedure for the preparation of seventeen pyrazole-benzthiazolamine conjugates has been incorporated. Data of synthesized compounds like IR, 1H NMR and Mass spectra were neatly presented. All these compounds were evaluated for their activity against Gram-positive and Gram-negative bacteria and various fungal strains. Anticancer activity has been carried out for the synthesized compounds using HeLa, DU145 and A549 cell lines using MTT assay and we found that the pyrazole-benzothiazolamine conjugates were possess antimicrobial, antifungal and anticancer activities.

Synthesis of new arylisoxazole–oxindole conjugates as potent antiproliferative agents

A new series of arylisoxazole–oxindole derivatives (6a–r) were synthesized and evaluated for their antiproliferative activity against human cancer cell lines including non-small cell lung (A549), cervical (HeLa), breast (MCF-7), and prostate (DU-145) cancer cell lines. The synthesized compounds (6a–r) demonstrated excellent to moderate cytotoxicity with IC50 values ranging from 0.82 to 3.69?μm. Some new compounds (6m–r) exhibited profound cytotoxicity better or similar to positive control. More particularly, the compound 6q possesses donating substituent like methoxy group presented at 5-position on D ring exhibited remarkable antiproliferative activity against A-549 (lung cancer) with an IC50 value 0.82?μm. Further studies to determine the mechanistic aspects of these conjugates are under progress.