Synthesis, characterization, and biological evaluation of some novel Schiff bases as potential metabolic enzyme inhibitors

2022 ◽  
Author(s):  
Reşit Çakmak ◽  
Eyüp Başaran ◽  
Murat Şentürk
Keyword(s):  
Schiff Bases ◽  
Enzyme Inhibitors ◽  
Biological Evaluation ◽  
Metabolic Enzyme

SYNTHESIS, CHARACTERIZATION AND BIOLOGICAL EVALUATION OF 3-FORMYL INDOLE BASED SCHIFF BASES

2018 ◽  
Vol 7 (6) ◽  
Author(s):  
Singh Gurvinder ◽  
Singh Prabhsimran ◽  
Dhawan R. K.
Keyword(s):  
Antimicrobial Activity ◽  
Spectral Analysis ◽  
Schiff Bases ◽  
Antimicrobial Agents ◽  
Biological Evaluation ◽  
Fungal Strain ◽  
Bacterial Strains ◽  
Standard Drug ◽  
Gram Negative ◽  
E Coli

In order to develop new antimicrobial agents, a series of 3-formyl indole based Schiff bases were synthesized by reacting 3-formyl indole(indole-3-carboxaldehyde) with substituted aniline taking ethanol as solvent. The reaction was carried in the presence of small amount of p-toluene sulphonic acid as catalyst.All the synthesized compounds were characterized by IR, 1H-NMR spectral analysis. All the synthesized compounds were evaluated for antimicrobial activity against two gram positive bacterial strains (B. subtilisand S. aureus) and two gram negative bacterial strains (P. aeruginosaand E. coli) and one fungal strain (C. albicans). All the synthesized compounds were found to have moderate to good antimicrobial activity. The  standard drug amoxicillin, fluconazole were used for antimicrobial activity. Among the synthesized compounds, the maximum antimicrobial activity was shown by compounds GS04, GS07, GS08 and GS10.

Nalidixic Acid Schiff bases: Synthesis and Biological Evaluation

2017 ◽  
Vol 14 ◽  
Author(s):  
Asif Husain ◽  
Munendra Mohan Varshney ◽  
Versha Parcha ◽  
Aftab Ahmad ◽  
Shahalam Khan
Keyword(s):  
Nalidixic Acid ◽  
Schiff Bases ◽  
Biological Evaluation ◽  
Synthesis And Biological Evaluation

Novel C-9, 9'-O-acyl Esters of (-)-Carinol as Free-radical Scavengers and Xanthine Oxidase Enzyme Inhibitors: Synthesis and Biological Evaluation

2013 ◽  
Vol 9 (1) ◽  
pp. 100-103 ◽  
Author(s):  
Praveen Kumar Suryadevara ◽  
Hari Babu Tatipaka ◽  
Rama Subba Rao Vidadala ◽  
Ashok k Tiwari ◽  
Janaswamy Madhusudana Rao ◽  
...  
Keyword(s):  
Free Radical ◽  
Xanthine Oxidase ◽  
Enzyme Inhibitors ◽  
Biological Evaluation ◽  
Free Radical Scavengers ◽  
Radical Scavengers ◽  
Oxidase Enzyme ◽  
Synthesis And Biological Evaluation

Catechol‐ and Phenol‐Containing Thio‐Schiff Bases: Synthesis, Electrochemical Properties and Biological Evaluation

2021 ◽  
Vol 6 (39) ◽  
pp. 10609-10618
Author(s):  
Ivan V. Smolyaninov ◽  
Daria A. Burmistrova ◽  
Maxim V. Arsenyev ◽  
Nailya R. Almyasheva ◽  
Ekaterina S. Ivanova ◽  
...  
Keyword(s):  
Electrochemical Properties ◽  
Schiff Bases ◽  
Biological Evaluation

Physiological assessment of non–target site restistance in multiple-resistant junglerice (Echinochloa colona)

Weed Science ◽  
2019 ◽  
Vol 67 (6) ◽  
pp. 622-632 ◽  
Author(s):  
Christopher E. Rouse ◽  
Nilda Roma-Burgos ◽  
Bianca Assis Barbosa Martins
Keyword(s):  
Management Practices ◽  
Enzyme Inhibitors ◽  
Treatment Resistance ◽  
Target Site ◽  
Metabolic Enzyme ◽  
Herbicide Resistant ◽  
Whole Plant ◽  
Detoxification Mechanism ◽  
Target Site Resistance ◽  
Resistance To Herbicides

AbstractHerbicide-resistant Echinochloa species are among the most problematic weeds in agricultural crops globally. Recurring herbicide selection pressure in the absence of diverse management practices has resulted in greater than 20% of sampled Echinochloa populations from rice (Oryza sativa L.) fields demonstrating multiple resistance to herbicides in Arkansas, USA. We assessed the resistance profile and potential mechanisms of resistance in a multiple herbicide–resistant junglerice [Echinochloa colona (L.) Link] (ECO-R) population. Whole-plant and laboratory bioassays were conducted to identify the potential mechanisms of non–target site resistance in this population. ECO-R was highly resistant to propanil (>37,800 g ha−1) and quinclorac (>17,920 g ha−1) and had elevated tolerance to cyhalofop (R/S = 1.9) and glufosinate (R/S = 1.2) compared to the susceptible standard. The addition of glufosinate (590 g ha−1) to cyhalofop (314 g ha−1), propanil (4,500 g ha−1), or quinclorac (560 g ha−1) controlled ECO-R 100%. However, cyhalofop applied with propanil (48% control) or quinclorac (15% control) was antagonistic. The application of the known metabolic enzyme inhibitors malathion, carbaryl, and piperonyl butoxide increased control of ECO-R with propanil (>75%) but not with other herbicides. Neither absorption nor translocation of [14C]cyhalofop or propanil was different between ECO-R and ECO-S. [14C]Quinclorac absorption was also similar between ECO-R and ECO-S; however, translocation of quinclorac into tissues above the treated leaf of ECO-R was >20% higher than that in ECO-S. The abundance of metabolites was higher (∼10%) in the treated leaves of ECO-R than in ECO-S beginning 48 h after treatment. The activity of β-cyanoalanine synthase, which detoxifies hydrogen cyanide, was not different between ECO-R and ECO-S following quinclorac treatment. Resistance to propanil was due to herbicide detoxification by metabolic enzymes. Resistance to quinclorac was due to a detoxification mechanism yet to be understood. The reduction in sensitivity to cyhalofop and glufosinate might be a secondary effect of the mechanisms conferring high resistance to propanil and quinclorac.

scholarly journals Discovery of New Schiff Bases Tethered Pyrazole Moiety: Design, Synthesis, Biological Evaluation, and Molecular Docking Study as Dual Targeting DHFR/DNA Gyrase Inhibitors with Immunomodulatory Activity

Molecules ◽  
2020 ◽  
Vol 25 (11) ◽  
pp. 2593 ◽  
Author(s):  
Ashraf S. Hassan ◽  
Ahmed A. Askar ◽  
Ahmed M. Naglah ◽  
Abdulrahman A. Almehizia ◽  
Ahmed Ragab
Keyword(s):  
Molecular Docking ◽  
Schiff Bases ◽  
Dihydrofolate Reductase ◽  
Enzyme Assay ◽  
Dna Gyrase ◽  
Docking Study ◽  
Biological Evaluation ◽  
Immunomodulatory Activity ◽  
Molecular Docking Study ◽  
Design Synthesis

A series of Bis-pyrazole Schiff bases (6a–d and 7a–d) and mono-pyrazole Schiff bases (8a–d and 9a–d) were designed and synthesized through the reaction of 5-aminopyrazoles 1a–d with aldehydes 2–5 using mild reaction condition with a good yield percentage. The chemical structure of newly formed Schiff bases tethered pyrazole core was confirmed based on spectral and experimental data. All the newly formed pyrazole Schiff bases were evaluated against eight pathogens (Gram-positive, Gram-negative, and fungi). The result exhibited that, most of them have good and broad activities. Among those, only six Schiff bases (6b, 7b, 7c, 8a, 8d, and 9b) displayed MIC values (0.97–62.5 µg/mL) compared to Tetracycline (15.62–62.5 µg/mL) and Amphotericin B (15.62–31.25 µg/mL), MBC values (1.94–87.5 µg/mL) and selectivity to tumor cell than normal cells. Immunomodulatory activities showed that the promising Schiff bases increase the immunomodulator effect of defense cell and the Schiff base 8a is the highest one by (Intra. killing activity = 136.5 ± 0.3%) having a pyrazole moiety as well as amide function (O=C-NH2) and piperidinyl core. Furthermore, the most potent one exhibited broad activity depending on both MIC and MBC values. Moreover, to study the mechanism of these pyrazole Schiff bases, two active Schiff bases 8a and 9b from six derivatives were introduced to study the enzyme assay as dihydrofolate reductase (DHFR) on E. coli organism and DNA gyrase with two different organisms, S. aureus and B. subtilis, to determine the inhibitory activities with lower values in the case of DNA gyrase (8a and 9b) or nearly as DHFR compound 9b, while pyrazole 8a showed excellent inhibitory against all enzyme assay. The molecular docking study against dihydrofolate reductase and DNA gyrase were performed to study the binding between active site in the pocket with the two Schiff bases (8a and 9b) that exhibited good binding affinity with different bond types as H-bonding, aren-aren, and arene-cation interaction as well as study the physicochemical and pharmacokinetic properties of the two active Schiff bases 8a and 9b.

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