- Bioactivity of azomethines derived mechanochemically from 2-amino pyridine and studies on the effect of substituents on the reaction
-
Azomethines with pyridine framework serve as excellent pharmacophore. A number of azomethine derivatives were synthesised from 2-aminopyridine and differently substituted aromatic aldehydes in excellent to almost quantitative yields through green, mechanochemical protocol. Influence of the substituents in the nuclei of aromatic aldehydes on the rate of the reaction was investigated. Presence of ortho hydroxy groups in the nucleus of aromatic aldehydes led to the completion of the reactions in almost no time with nearly quantitative yields. 2,2'-diphenyl-1-picrylhydrazyl (DPPH) radical was used to evaluate the in vitro antioxidant activity of the prepared azomethines and the results were compared with standard natural antioxidant L-ascorbic acid. Most of the derivatives showed fairly strong antioxidant property. Antibacterial activity of the prepared azomethines were examined against Bacillus subtilis (Gram-positive) and Escherichia coli (Gram-negative) strains by using agar well diffusion method. Some of the azomethines exhibited encouraging antibacterial activities.
- Sarma, Madhushree Das,Ghosh, Subhojit
-
p. 1295 - 1303
(2020/12/04)
-
- Synthesis, antimicrobial screening, homology modeling, and molecular docking studies of a new series of Schiff base derivatives as prospective fungal inhibitor candidates
-
Twelve new Schiff base derivatives have been prepared by the condensation reaction of different amino substituted compounds (aniline, pyridin-2-amine, o-toluidine, 2-nitrobenzenamine, 4-aminophenol, and 3-aminopropanol) and substituted aldehydes such as n
- Toubi, Yahya,Abrigach, Farid,Radi, Smaail,Souna, Faiza,Hakkou, Abdelkader,Alsayari, Abdulrhman,Muhsinah, Abdullatif Bin,Mabkhot, Yahia N.
-
-
- A novel approach towards design, synthesis and evaluation of some Schiff base analogues of 2-aminopyridine and 2-aminobezothiazole against hepatocellular carcinoma
-
Hepatocellular carcinoma is the most common primary malignancy of the liver with poor prognosis. In this study novel, Schiff's bases of 2-aminopyridine (SSSC-26 to 31) and 2-aminobenzothiazole (SSSC-32 to 37) were designed, synthesised and evaluated for antioxidant potential using DPPH method, and anti-hepatocellular carcinoma property using diethylnitrosamine (DEN) induced hepatocellular carcinoma rat model. The in-silico pharmacokinetic, rule of five and toxicity studies reveals that all the leads have an excellent intrinsic quality and sufficient structural features necessary for an oral activity. Molecular docking studies of all compounds into the ligand binding pocket of checkpoint kinase1 and vascular endothelial growth factor receptor-2 was also performed using Schrodinger software suite v8.5, and which have shown good Glide scores. Further compounds were synthesised based on the docking score and ADMET profile. The 1,1-diphenyl-2-picrylhydrazil (DPPH) scavenging study was carried out, and results showed that SSSC-29 (IC50-63.60) and SSSC-33 (IC50-60.32) were having good anti-oxidant potential in comparison with ascorbic acid (IC50-55.27). SSSC-33 further evaluated for anti-cancer potential against diethylnitrosamine (200 mg/kg bw) induced hepatocellular carcinoma in rats. The biochemical, histopathological and morphological data showed that SSSC-33 can reverse the changes occurred in the cancerous liver significantly. All these findings suggested that SSSC-33-((benzo[d]thiazol-2-ylimino) methyl)phenol) could be a potential compound in combating the oxidative damage of hepatic cells occurred due to the development of hepatocellular carcinoma induced by a chemical carcinogen, DEN.
- Chacko, Shinu,Samanta, Subir
-
p. 162 - 176
(2017/02/26)
-
- Regioselective synthesis of 2 H-indazoles using a mild, one-pot condensation-cadogan reductive cyclization
-
An operationally simple and efficient one-pot synthesis of 2H-indazoles from commercially available reagents is reported. Ortho-imino-nitrobenzene substrates, generated via condensation, undergo reductive cyclization promoted by tri-n-butylphosophine to afford substituted 2H-indazoles under mild reaction conditions. A variety of electronically diverse ortho-nitrobenzaldehydes and anilines were examined. To further extend the scope of the transformation, aliphatic amines were also employed to form N2-alkyl indazoles selectively under the optimized reaction conditions.
- Genung, Nathan E.,Wei, Liuqing,Aspnes, Gary E.
-
supporting information
p. 3114 - 3117
(2014/06/23)
-
- Ultrasonics promoted synthesis of thiazolidinones from 2-aminopyridine and 2-picolilamine
-
The efficient multicomponent synthesis of thiazolidinones from the reaction of arenealdehydes, mercaptoacetic acid and 2-picolilamine or 2-aminopyridine under ultrasound irradiation are reported. The reaction with 2-aminopyridine needs a Lewis acid cataly
- Gouvêa, Daniela P.,Bare?o, Valéria D.O.,Bosenbecker, Juliano,Drawanz, Bruna B.,Neuenfeldt, Patrícia D.,Siqueira, Geonir M.,Cunico, Wilson
-
experimental part
p. 1127 - 1131
(2012/08/08)
-
- Simple and efficient one-pot synthesis of imidazo[1,2-a]pyridines catalyzed by magnetic nano-Fe3O4-KHSO4·SiO 2
-
The present report highlights a magnetic nano-Fe3O 4-KHSO4·SiO2 catalyzed synthesis of imidazo[1,2-a]pyridines. The synthetic strategy adopted is expedient, versatile, and offers good to excellent yields from readily available starting materials.
- Guntreddi, Tirumaleswararao,Allam, Bharat Kumar,Singh, Krishna Nand
-
p. 2635 - 2638,4
(2012/12/12)
-
- An approach to fused pyrimidine derivatives via Schiff bases of aromatic ortho-nitrocarbaldehydes. An investigation of substituent effects on the reaction course
-
The synthesis of fused pyrimidines from the Schiff bases of aromatic ortho-nitrocarbaldehydes is reported. The Schiff bases after selective reduction of the nitro group on 10% Pd/C, followed by condensation of the amines formed with orthoesters, are transformed to the corresponding imidates. Heating of the latter in a sealed tube with an excess of ammonia (or with ammonia in ethanol) gives fused pyrimidines. The influence of various substituents in the aromatic ring of the imine moiety of the Schiff bases on the overall yield of fused pyrimidine derivatives has been investigated. Moderate electron-withdrawing groups gave the best results.
- Ostrowski,Wolniewicz
-
p. 705 - 713
(2007/10/03)
-