33165-46-7Relevant academic research and scientific papers
Investigation of antioxidant and anti-nociceptive potential of isoxazolone, pyrazolone derivatives, and their molecular docking studies
Anwar, Tayyaba,Nadeem, Humaira,Sarwar, Sadia,Naureen, Humaira,Ahmed, Safia,Khan, ArifUllah,Arif, Muazzam
, p. 893 - 903 (2020/07/15)
A series of new isoxazolone (3a–d) and pyrazolone (4a–d) derivatives were synthesized and assessed for their antioxidant and analgesic activity. Among synthesized compounds, 3b and 4b having nitro (NO2) group show high analgesic activity at a dose of 6 mg/kg. Analgesic activity was further proceeded to explore the contribution of opioidergic mechanisms in the mediation of analgesic effects. Animals were administered with naloxone, a nonselective opioid inverse agonist, at the dose of 0.5 mg/kg. The results obtained suggested that the analgesic effects of the synthesized compounds were not reversed by naloxone, specifying that the compounds 3b and 4b do not follow the opioidergic pathway in order to relieve pain in animal models. Further, the binding interactions of compounds 3b and 4b were analyzed by docking them against nonopioid receptors COX-1 (3N8X) and COX-2 (3LN1). The results demonstrate the analgesic potential of isoxazolone and pyrazolone derivatives, especially compounds 3b and 4b can be considered promising lead molecules for further investigation and development into potent analgesic drugs. In addition, the antioxidant potential of compounds was also found to be related to better analgesic activity, thus providing an insight into the role of oxidative stress in the mediation of analgesia.
Synthesis and Pharmacological Investigations of Novel Pyrazolyl and Hydrazonoyl Cyanide Benzimidazole Entities
Khalifa, Mohamed E.,Gobouri, Adil A.,Kabli, Fahad M.,Altalhi, Tariq A.,Almalki, Abdulraheem S. A.,Elemshaty, Amira M.
, p. 1426 - 1436 (2019/04/17)
Various novel benzimidazole entities linked to pyrazolyl and hydrazonoyl cyanide substrates carrying aryl and heteroaryl groups (8a–e to 10a–e) were synthesized using new route syntheses and were focused on their pharmacological evaluation as one of the m
Designing of a fluoride selective receptor through molecular orbital engineering
Mishra, Rakesh K.,Kumar, Virendra,Diwan, Uzra,Upadhyay,Roy Chowdhury
, p. 167 - 174 (2013/01/14)
The stepwise substitution of appropriate groups over the 3-[(2,4-dinitro-phenyl)-hydrazono]-butyric acid ethyl ester (R3) lead receptor R1 which showed selectivity towards fluoride in DMSO. The UV-vis and 1H NMR titration studies revealed the d
A facile and rapid synthesis of benzothiazines
Dabholkar, Vijay V.,Gavande, Rahul P.
, p. 365 - 368 (2013/09/24)
A series of 2H. 4H-2-[3-methyl-4-(substituted) phenyl azo pyrazolon-5-one-1-yl]-carbonyl methyl-3-oxo-1,4-benzothiazines have been synthesized by the reaction of 2H, 4H-2-hydrazino carbonyl methyl-3-oxo-1,4- benzothiazine with substituted acetoacetic ester derivatives using ultrasound and microwave irradiation. All the synthesized compounds were investigated for their antibacterial activities. The result indicated that the compounds showed convincing activities against Gram-positive bacteria (Bacillus subtilis and Streptococcus lactis) when compared with standard drug (ampicillin trihydrate). These compounds were also synthesized by conventional method and their structures have been elucidated on the basis of spectral analyses and chemical analysis.
Synthesis of 5-(substituted phenylazo)-6-hydroxy-4-methyl-3--cyano-2- pyridones from ethyl 3-oxo-2-(substituted phenylazo)butanoates
Dostanic, Jasmina,Valentic, Natasa,Uscumlic, Gordana,Mijin, Dusan
experimental part, p. 499 - 504 (2012/02/03)
A new procedure for the synthesis of known azo pyridone dyes is presented. A series of 5-(substituted arylazo)-6-hydroxy-4-methyl-3-cyano-2--pyridones were prepared from ethyl 3-oxo-2-(substituted phenylazo)butanoates and cyanoacetamide in acetone using potassium hydroxide as a catalyst by simple refluxing the reaction mixture. The structure of these dyes was confirmed by FT-IR, NMR and UV-Vis spectroscopy. Copyright 2011 (CC) SCS.
