Unprecedented Biological Evaluation of Zn(II) Complexes supported by “Self-adjustable” Acyclic Diiminodipyrromethane Schiff’s Bases: DFT, Molecular Docking; Biological activity studies

2021 ◽  
pp. 108936
Author(s):  
Shiva Krishna Loke ◽  
Eswar Pagadala ◽  
Venkatesan Srinivasadesikan ◽  
Rex Jeya Rajkumar Samdavid Thanapaul ◽  
T. Pooventhiran ◽  
...  
Keyword(s):  
Biological Activity ◽  
Molecular Docking ◽  
Biological Evaluation ◽  
Schiff’S Bases ◽  
Schiff's Bases

Synthesis of Some Formazan Derivatives from Schiff’s Bases and Studying of Biological Activity

2017 ◽  
Vol 13 (4) ◽  
pp. 97-112
Author(s):  
Shima Ibraheem Chyad Al-khazraji ◽  
◽  
Hussein Abbood Idham
Keyword(s):  
Biological Activity ◽  
Schiff’S Bases ◽  
Schiff's Bases

Synthesis and Biological Evaluation of Chalconyl Incorporated Schiff’s Bases of Sulphonamides

2017 ◽  
Vol 8 (03) ◽  
Author(s):  
Neeraj Kumar ◽  
Dhruti Bhatt ◽  
Chandra Shekhar Sharma ◽  
Hamendra Pratap Singh ◽  
Harshda Pandiya ◽  
...  
Keyword(s):  
Antibacterial Activity ◽  
Antifungal Activity ◽  
Biological Evaluation ◽  
Antibacterial And Antifungal Activity ◽  
Schiff’S Bases ◽  
E Coli ◽  
Schiff's Bases ◽  
Microbial Strains ◽  
Antibacterial And Antifungal ◽  
Synthesis And Biological Evaluation

A series of of Chalconyl Incorporated Schiff’s Bases of Sulphonamides was synthesized by reacting substituted chalcone derivatives with Sulphacetamide sodium in methanol. All the title compounds synthesized (2a-2d) were tested for antibacterial and antifungal activity using E. coli, P. aeruginosa, S. aureus, S. pyogenus and C. albicans, A. niger and A. clavatus respectively as microbial strains and Sulphacetamide sodium as standard. The compound 2d showed significant antibacterial activity and 2a showed moderate antifungal activity as compared with Sulphacetamide Sodium.

Synthesis, Biological Evaluation and Molecular Modeling Studies of Novel C (7) Modified Analogues of Chrysin

2020 ◽  
Vol 17 (7) ◽  
pp. 873-883
Author(s):  
Pulabala Ramesh ◽  
Vankadari Srinivasa Rao ◽  
Puchakayala Muralidhar Reddy ◽  
Katragadda Suresh Babu ◽  
Mutheneni Srinivasa Rao
Keyword(s):  
Natural Products ◽  
Biological Activity ◽  
Molecular Docking ◽  
Biological Activities ◽  
Antimicrobial Activities ◽  
Docking Studies ◽  
Biological Evaluation ◽  
Molecular Docking Studies ◽  
Fungal Strains

Background:: Most of the currently available pharmaceutical drugs are either natural products or analogues of natural products. Flavonoids are plant based natural polyphenolic compounds which exhibit a wide range of biological activities. Chrysin, a natural flavone, exhibits several biological activities like antiallergic, anti-inflammatory and anticancer. Many efforts were made to enhance the biological activity of chrysin. In continuation of our work on synthetic modifications of chrysin, amino-alcohol containing heterocyclic moiety is linked to chrysin at C (7) position to enhance its biological activity. Methods:: A series of new C (7) modified analogues of chrysin (3a-k) have been designed and synthesized in two steps. Chrysin, on reacting with epichlorohydrin in the presence of K2CO3 in DMF gave epoxide (2) which was made to react with cyclic secondary amines in the presence of LiBr to form the designed products (3a-k). All the synthesized compounds (3a-k) were well characterized by 1H NMR, 13C NMR and mass spectral data. The synthesized analogues (3a-k) were screened for their in vitro biological activities against a panel of bacterial and fungal strains. Molecular docking studies were also performed on these compounds with E. coli FabH (1HNJ) and S. cerevisiae (5EQB) enzymes, to support the observed biological activities. Results:: A series of new 2-hydroxy 3-amino chrysin derivatives (3a-k) were synthesized in two steps, starting with chrysin and their structures were characterized by spectral analysis. In vitro biological activities of these analogues against a panel of bacterial and fungal strains indicated that some of the derivatives manifested significant activities compared to standard drugs. Molecular docking and binding energy values were also correlated with experimental antimicrobial screening results. Lipinski’s “rule of five” is also obeyed by these analogues (3a-k) and exhibit drug-likeness. Conclusion:: In the present study, a series of new C (7) modified chrysin analogues (3a-k) were synthesized and tested for their in vitro antimicrobial activities. These biological studies indicated that some of the derivatives exhibited moderate to good antimicrobial activities compared to standard drugs. Molecular docking studies performed on these compounds correlated with the experimental antimicrobial activities. The results obtained in the study will be useful in establishing new drug entities to control the pathogenic epidemics.

scholarly journals Synthesis, characterization and biological evaluation of Schiff’s bases derivatives as potent antibacterial agents

2017 ◽  
Vol 4 (5) ◽  
pp. 216
Author(s):  
Versha Parcha ◽  
Ankit Kumar ◽  
Babita Mahajan ◽  
Jaswinder Kaur
Keyword(s):  
Antibacterial Effect ◽  
Biological Evaluation ◽  
Spectral Studies ◽  
Schiff’S Bases ◽  
Zone Of Inhibition ◽  
Schiff's Bases ◽  
Almost All ◽  
Derivatives Of ◽  
Antibacterial Potential ◽  
Schiffs Bases

Objective: To design, synthesize and screen biologically newer Substituted Schiff bases by condensing substituted acid hydrazides with various benzaldehydes and explore their antimicrobial potential.Methods: Present study synthesis of various derivatives of Schiffs bases was carried out by: firstly converting substituted acids to acid hydrazides and then to Schiff's bases after condensation with substituted benzaldehyde. Synthesized compounds were characterised on the basis of spectral studies (like UV, IR, and NMR). All the synthesized derivatives were screened further for their antibacterial effect against Salmonella typhimurium, Shigella sonnei, Staphylococcus aureus& Bacillus cereus.Results: From this study it could be observed that schiff’s bases 2-[( aminophenylhydrazinyldene o,m,dinitrobenzoyl] aniline (H) and compound 2-[( aminophenylzinyldene) p amino benzoyl] aniline (I) showed very good zone of inhibition against almost all strains tested for.Conclusions: So further attempts could be made to extend the series and explore their antibacterial potential to achieve hopeful goal.

scholarly journals Synthesis and biological evaluation of new aryl substituted Schiff’s bases

2017 ◽  
Vol 4 (6) ◽  
pp. 252
Author(s):  
Versha Parcha ◽  
Jaswinder Kaur
Keyword(s):  
Antimicrobial Agents ◽  
Acid Hydrazide ◽  
Structure Activity Relationship ◽  
Biological Evaluation ◽  
Activity Relationship ◽  
Spectral Studies ◽  
Schiff’S Bases ◽  
Structure Activity ◽  
Schiff's Bases ◽  
Good Potential

Objective: Chemical substances employed to treat various infections caused by various types of microorganism are termed as antimicrobials and natural chemical compounds produced by specific types of bacteria are termed as antibiotics. Unlimited use of antibiotics in humans and animals and in areas other than the treatment and prophylaxis of disease have resulted in a serious problem of drug resistance. Various attempts have been adopted to cope with the resistance problem and enhance the activity, or broaden the spectrum of drugs. Based on structure-activity relationship synthesis of new compounds has been one of the best approaches for better results. It has been demonstrated that Schiff base of some leading molecules and antibiotics possess good potential as more effective and safe drugs. Encouraged by reports on potential of Schiff’s bases as antimicrobial agents and to cope up with the current requirements of developing newer, safer and broad spectrum agents attempts were made to synthesize new Schiff’s bases.Methods: Our earlier in which structure activity relationship studies revealed that substitution by nitro and amino gp in Schiff’s base moiety resulted in the enhancement of activity. So further attempts were made to extend the series with incorporation of nitro and amino moiety by condensing o,m dinitro substituted acid hydrazide with various nitro/amino substituted benzaldehydes for increasing their antimicrobial potential.Results: Synthesized compounds were characterized on the basis of spectral studies (like UV, IR, and NMR). All the synthesized derivatives were screened further for their antibacterial effect. All the synthesized derivatives were screened further for their antibacterial effect.Conclusions: Highest activity was observed in the derivative with nitro substitution in both the aryl rings.

scholarly journals Overview on Nitrogen containing compounds and their assessment based on ‘International Regulatory Standards’

2018 ◽  
Vol 8 (6-s) ◽  
pp. 424-428 ◽  
Author(s):  
Ansar R. Shaikh ◽  
Mazahar Farooqui ◽  
R.H. Satpute ◽  
Syed Abed
Keyword(s):  
Biological Activity ◽  
Heterocyclic Compounds ◽  
Schiff’S Bases ◽  
Schiff's Bases ◽  
Regulatory Standards ◽  
Class 1 ◽  
Structural Alerts ◽  
Regulatory Assessment ◽  
Novel Catalyst ◽  
Nitrogen Containing Compounds

Heterocyclic compounds have a role in most fields of sciences such as medicinal chemistry, biochemistry also another area of sciences. More than 90% of new drugscontain heterocycles and the interface between chemistry and biology, at which so much new scientific insight, discovery and application is taking place is crossed by heterocyclic compounds. Compounds derived from heterocyclic rings in pharmacy, medicine, agriculture, plastic, polymer and other fields.Most active heterocycles that have shown considerable biological actions as antifungal, anti-inflammatory, antibacterial, anticonvulsant, antiallergic, herbicidal, anticancer activity. There is always a strong need for new and efficient processes in synthesizing of new Heterocycles.Alum have been used as a novel catalyst in the synthesis of Schiff’s bases. Synthesized Schiff’s bases are free from use of ICH class 1 and Class 2 solvents and also free from structural alerts genotoxic impurities. This review highlights on various aspects of heterocyclic compounds with its biological activity & regulatory assessment based on the ‘International Regulatory Standards’. Keywords: Heterocycles. Nitrogen containing compounds Biological activity, History, Regulatory assessment, International Regulatory Standards

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