Design, synthesis and evaluation of 3-amide-5-aryl benzoic acid derivatives as novel P2Y14R antagonists with potential high efficiency against acute gouty arthritis

2021 ◽  
pp. 113313
Author(s):  
Ran Lu ◽  
Yilin Wang ◽  
Chunxiao Liu ◽  
Zhenguo Zhang ◽  
Baiyang Li ◽  
...  
Keyword(s):  
Benzoic Acid ◽  
High Efficiency ◽  
Gouty Arthritis ◽  
Design Synthesis ◽  
Acute Gouty Arthritis ◽  
Benzoic Acid Derivatives

scholarly journals Hydrogenation of benzoic acid derivatives over Pt/TiO2 under mild conditions

2021 ◽  
Vol 4 (1) ◽  
Author(s):  
Miao Guo ◽  
Xiangtao Kong ◽  
Chunzhi Li ◽  
Qihua Yang
Keyword(s):  
Electron Transfer ◽  
Benzoic Acid ◽  
High Efficiency ◽  
Carboxyl Groups ◽  
Carboxyl Group ◽  
Benzoic Acids ◽  
Catalyst Poisoning ◽  
Benzoic Acid Derivatives ◽  
Mild Conditions ◽  
Transfer Direction

AbstractHydrogenation of benzoic acid (BA) to cyclohexanecarboxylic acid (CCA) has important industrial and academic significance, however, the electron deficient aromatic ring and catalyst poisoning by carboxyl groups make BA hydrogenation a challenging transformation. Herein, we report that Pt/TiO2 is very effective for BA hydrogenation with, to our knowledge, a record TOF of 4490 h−1 at 80 °C and 50 bar H2, one order higher than previously reported results. Pt/TiO2 catalysts with electron-deficient and electron-enriched Pt sites are obtained by modifying the electron transfer direction between Pt and TiO2. Electron-deficient Pt sites interact with BA more strongly than electron-rich Pt sites, helping the dissociated H of the carboxyl group to participate in BA hydrogenation, thus enhancing its activity. The wide substrate scope, including bi- and tri-benzoic acids, further demonstrates the high efficiency of Pt/TiO2 for hydrogenation of BA derivatives.

Design, synthesis and biological activity of novel substituted 3-benzoic acid derivatives as MtDHFR inhibitors

2020 ◽  
Vol 28 (15) ◽  
pp. 115600
Author(s):  
Thales Kronenberger ◽  
Glaucio Monteiro Ferreira ◽  
Alfredo Danilo Ferreira de Souza ◽  
Soraya da Silva Santos ◽  
Antti Poso ◽  
...  
Keyword(s):  
Biological Activity ◽  
Benzoic Acid ◽  
Design Synthesis ◽  
Benzoic Acid Derivatives

scholarly journals Therapy with canakinumab for gout

2019 ◽  
Vol 56 ◽  
pp. 41-48 ◽  
Author(s):  
M. S. Eliseev ◽  
E. L. Nasonov
Keyword(s):  
High Efficiency ◽  
Interleukin 1 ◽  
Gouty Arthritis ◽  
Favorable Effect ◽  
Tophaceous Gout ◽  
Acute Gouty Arthritis ◽  
Acute Arthritis ◽  
Inflammatory Drugs ◽  
Anti Inflammatory ◽  
Inflammatory Action

A significant part of patients with gout has contraindications to taking nonsteroidal anti-inflammatory drugs, colchicine and glucocorticoids. Such therapy is often ineffective, particularly in patients with the severe tophaceous gout what hampers treatment of acute arthritis attack assuming the need for other methods of therapy. During the last years several medications have been introduced the mechanism of anti-inflammatory action of which is associated with inhibition of interleukin 1 (IL1) playing a key role in the development of acute gouty arthritis. To date, the most well-studied and the only registered drug for relief of acute arthritis attack is canakinumab, recommended for use in situations where other therapy options are unacceptable. Despite these limitations, the use of IL1 inhibitors, in particular canakinumab, seems promising due to the high efficiency of the drug, the ability to use it in patients with comorbid diseases, as well as a favorable effect on the risk of cardiovascular disease.

Bjerkandera adusta as a source of benzoic acid derivatives targeting 26S proteasome and cathepsins B&L

2019 ◽  
Author(s):  
K Georgousaki ◽  
N Tsafantakis ◽  
S Gumeni ◽  
V González-Menéndez ◽  
G Lambrinidis ◽  
...  
Keyword(s):  
Benzoic Acid ◽  
26S Proteasome ◽  
Bjerkandera Adusta ◽  
Benzoic Acid Derivatives

2,4-Dichloro-5-[(N-aryl/alkyl)sulfamoyl]benzoic Acid Derivatives: In Vitro Antidiabetic Activity, Molecular Modeling and In silico ADMET Screening

2019 ◽  
Vol 15 (2) ◽  
pp. 186-195 ◽  
Author(s):  
Samridhi Thakral ◽  
Vikramjeet Singh
Keyword(s):  
Molecular Docking ◽  
Benzoic Acid ◽  
Inhibitory Activity ◽  
In Silico ◽  
Computational Study ◽  
Antidiabetic Activity ◽  
Standard Drug ◽  
Benzoic Acid Derivatives ◽  
In Silico Admet ◽  
Inhibitory Potential

Background: Postprandial hyperglycemia can be reduced by inhibiting major carbohydrate hydrolyzing enzymes, such as α-glucosidase and α-amylase which is an effective approach in both preventing and treating diabetes. Objective: The aim of this study was to synthesize a series of 2,4-dichloro-5-[(N-aryl/alkyl)sulfamoyl] benzoic acid derivatives and evaluate α-glucosidase and α-amylase inhibitory activity along with molecular docking and in silico ADMET property analysis. Method: Chlorosulfonation of 2,4-dichloro benzoic acid followed by reaction with corresponding anilines/amines yielded 2,4-dichloro-5-[(N-aryl/alkyl)sulfamoyl]benzoic acid derivatives. For evaluating their antidiabetic potential α-glucosidase and α-amylase inhibitory assays were carried out. In silico molecular docking studies of these compounds were performed with respect to these enzymes and a computational study was also carried out to predict the drug-likeness and ADMET properties of the title compounds. Results: Compound 3c (2,4-dichloro-5-[(2-nitrophenyl)sulfamoyl]benzoic acid) was found to be highly active having 3 fold inhibitory potential against α-amylase and 5 times inhibitory activity against α-glucosidase in comparison to standard drug acarbose. Conclusion: Most of the synthesized compounds were highly potent or equipotent to standard drug acarbose for inhibitory potential against α-glucosidase and α-amylase enzyme and hence this may indicate their antidiabetic activity. The docking study revealed that these compounds interact with active site of enzyme through hydrogen bonding and different pi interactions.

Sign in / Sign up

Export Citation Format

Share Document