358656-96-9Relevant academic research and scientific papers
Synthesis, characterization, and anti-amoebic activity of N-(pyrimidin-2-yl)benzenesulfonamide derivatives
Roouf Bhat, Abdul,Arshad, Mohammad,Ju Lee, Eun,Pokharel, Smritee,Choi, Inho,Athar, Fareeda
, p. 2267 - 2277 (2013)
A new series of N-(pyrimidin-2-yl)benzenesulfonamide derivatives, 3a-3i and 4a-4i, was synthesized from pyrimidin-2-amines, 2a-2i, with the aim to explore their effects on in vitro growth of Entamoeba histolytica. The chemical structures of the compounds
Rapid abnormal [3+2]-cycloaddition of isatinN,N′-cyclic azomethine imine 1,3-dipoles with chalcones
Yue, Guizhou,Dou, Zhengjie,Zhou, Zexi,Zhang, Li,Feng, Juhua,Chen, Huabao,Yin, Zhongqiong,Song, Xu,Liang, Xiaoxia,Wang, Xianxiang,Rao, Hanbing,Lu, Cuifen
supporting information, p. 8813 - 8817 (2020/06/08)
The rapid synthesis of novel dicyclic spiropyrrolidine was reported, using [3+2]-cycloaddition of isatinN,N′-cyclic azomethine imine 1,3-dipoles, generated from the condensation of substituted isatins and pyrazolidones, with chalcones in 2-5 min. The dicy
Synthesis, cyclooxygenase inhibition and anti-inflammatory evaluation of new 1,3,5-triaryl-4,5-dihydro-1H-pyrazole derivatives possessing methanesulphonyl pharmacophore
Abdellatif, Khaled R. A.,Elsaady, Mohammed T.,Abdel-Aziz, Salah A.,Abusabaa, Ahmed H. A.
, p. 1545 - 1555 (2016/10/09)
A new series of 1,3,5-triaryl-4,5-dihydro-1H-pyrazole derivatives 13a–p were synthesized via aldol condensation of 3/4-nitroacetophenones with appropriately substituted aldehydes followed by cyclization of the formed chalcones with 4-methanesulfonylphenylhydrazine hydrochloride. All the synthesized compounds were evaluated for their cyclooxygenase (COX) inhibition, anti-inflammatory activity and ulcerogenic liability. All compounds were more potent inhibitors for COX-2 than COX-1. While most compounds showed good anti-inflammatory activity, compounds 13d, 13f, 13k and 13o were the most potent derivatives (ED50 = 66.5, 73.4, 79.8 and 70.5 μmol/kg, respectively) in comparison with celecoxib (ED50 = 68.1 μmol/kg). Compounds 13d, 13f, 13k and 13o (ulcer index = 3.89, 4.86, 4.96 and 3.92, respectively) were 4–6 folds less ulcerogenic than aspirin (ulcer index = 22.75) and showed approximately ulceration effect similar to celecoxib (ulcer index = 3.35). In addition, molecular docking studies were performed for compounds 13d, 13f, 13k and 13o inside COX-2 active site which showed acceptable binding interactions (affinity in kcal/mol ?2.1774, ?6.9498) in comparison with celecoxib (affinity in kcal/mol ?6.5330).
Design, Synthesis, Antibacterial Activity, and Molecular Docking Studies of Novel Hybrid 1,3-Thiazine-1,3,5-Triazine Derivatives as Potential Bacterial Translation Inhibitor
Singh, Udaya P.,Pathak, Manish,Dubey, Vaibhav,Bhat, Hans R.,Gahtori, Prashant,Singh, Ramendra K.
, p. 572 - 583,12 (2020/07/31)
Some novel hybrid 1,3-thiazine-1,3,5-triazine derivatives were synthesized and tested for antibacterial activity. Compounds 8c and 8f were found active against Gram positive and Gram negative microorganisms. Molecular docking studies have been performed o
Synthesis and antimicrobial activity of some pyrazoline derivatives
Ahirwar,Gautam,Shrivastava
experimental part, p. 5297 - 5302 (2012/07/28)
The objective of present study is to synthesize and screening of antimicrobial activity of some derivatives of pyrazoline. 1H-[4-nitro phenyl-5-(substituted phenyl)]pyrazoline has been used as a precursor to synthesize some biologically active heterocycles. Reaction of 1-(4-nitrophenyl)-3-(substituted phenyl) prop-2-en-1-one with hydrazine hydrate gave 1H-(3-nitrophenyl-5-(substituted phenyl) pyrazoline which on reaction with benzoyl chloride in pyridine gave 1-benzoyl-(4-nitrophenyl)-5-(substituted phenyl) prazoline and on reaction with acetic acid yields 1-acetyl-(4- nitrophenyl)-5-(substituted phenyl) pyrazoline derivatives. Several derivatives have been synthesized and screened for their antimicrobial efficacy against Bacillus subtilis, Escherichia coli, Staphylococcus aureus and Klebsiella pneumoniae. Antifungal activity against, Aspergillus flavus, Fusarium oxisporum, Aspergillus niger and Trichoderma viridae.
