scholarly journals Green Route for Efficient Synthesis of Novel Amino Acid Schiff Bases as Potent Antibacterial and Antifungal Agents and Evaluation of Cytotoxic Effects

2014 ◽  
Vol 2014 ◽  
pp. 1-12 ◽  
Author(s):  
Harshita Sachdeva ◽  
Rekha Saroj ◽  
Sarita Khaturia ◽  
Diksha Dwivedi ◽  
Om Prakash Chauhan

Green chemical one-pot multicomponent condensation reaction of substituted 1H-indole-2,3-diones (1), various amino acids (2), and thiosemicarbazide (3) is found to be catalyzed by lemon juice as natural acid using water as a green solvent to give the corresponding Schiff bases (4) in good to excellent yields. This method is experimentally simple, clean, high yielding, and green, with reduced reaction times. The product is purified by simple filtration followed by washing with water and drying process. The synthesized compounds are characterized by FT-IR,13CNMR, and1HNMR spectroscopy and are screened for their antifungal activity againstAspergillus niger,Penicillium notatum,Fusarium oxysporum,Alternaria brassicicola,Chaetomium orium, andLycopodium sp.and antibacterial activity against Gram-positive bacteria,Bacillus licheniformis,Staphylococcus aureus, andMicrococcus luteus,and Gram-negative bacteria,Pseudomonas aeruginosaandEscherichia coli. Compounds have also been evaluated for cytotoxic effects against human colon cancer cell line Colo205.

2013 ◽  
Vol 2013 ◽  
pp. 1-8 ◽  
Author(s):  
Kavitha Kankanala ◽  
Vangala Ranga Reddy ◽  
Yumnam Priyadarshini Devi ◽  
Lakshmi Narasu Mangamoori ◽  
Khagga Mukkanti ◽  
...  

The nimesulide based novel glycolamide esters were designed and synthesized for the first timeviaa three-step method starting from nimesulide. Structures of the synthesized compounds were confirmed by spectroscopic analysis. All the synthesized compounds were examined for their cytotoxic effectsin vitro,some of which showed significant cytotoxic activities against HCT-15 human colon cancer cell line.


ChemInform ◽  
2011 ◽  
Vol 42 (32) ◽  
pp. no-no
Author(s):  
Ping Wu ◽  
Xi-Mei Cai ◽  
Qi-Fang Wang ◽  
Chao-Guo Yan

2015 ◽  
Vol 93 (11) ◽  
pp. 1245-1248 ◽  
Author(s):  
Ahmad Reza Moosavi-Zare ◽  
Mohammad Ali Zolfigol ◽  
Fateme Derakhshan-Panah ◽  
Masoume Daraei

A one-pot, multicomponent condensation reaction of phenols, aromatic aldehydes, and amides in the presence of catalytic amount of trityl chloride as a homogeneous organocatalyst under solvent-free condition to prepare amidoalkyl phenols has been reported. It is interesting that trityl chloride by in situ generation of trityl carbocation with inherent instability catalyzes the reaction.


2020 ◽  
Vol 7 (4) ◽  
pp. 215-226
Author(s):  
Muhammad Rizwan Khan ◽  
Mohsin Abbas Khan ◽  
Khalil Ahmad ◽  
Asad Hamad ◽  
Muhammad Sajid-ur-Rehman ◽  
...  

Objective: Nowadays antibacterial drugs resistance is major problem in the world. To overcome this problem, some novel derivates of doxycycline were synthesized by single step condensation reaction with ten different types of aromatic and aliphatic aldehydes and ketones in ethanol as solvent and acetic acid as catalyst. In these reactions, deprotonation of primary amine occurs that results in formation of imine.  Methods: All the derivatives physically characterized and confirmed by analytical techniques i.e. FTIR and 1H NMR and 13C NMR. The derived compounds have exhibited significantly more active against both gram positive as well as gram negative bacterial strains as compared to parent drug. Results: Derived Schiff bases RDC2, RDC4 and RDC10 showed zone of inhibition against Bacillus subtilis as compared to doxycycline and derived Schiff bases RDC1, RDC2, RDC5, RDC6, RDC7 and RDC8 showed more zone of inhibition against Micrococcus luteus as compared to doxycycline. Yield (75%), m.p. 180-185°C, Mol. Wt. 1063, Elemental Analysis: (Calculated) for C58H54N4O16: iC, 65.53; H, 5.12; N, 5.27; (Found): C, 65.49; H, 5.18; N, 5.37; FTIR (ν, cm‐1): 3066 (=C-H), 1665(C=N), 1585, 1490(C=C, phenyl), 3650(OH), 1692 (C=O); 1H NMR (DMSO−d6, δ, ppm), 6.02-6.03 d, 6.91-6.92 d, (=CH-); 6.88-6.89 t (=CH), 2.89-2.90 d, (-CH); 1.07-1.08 q, (-CH3), 3.38-3.39 d; 3.17-3.18 d, (CH), 1.47-1.48 t (CH), 1.48 s, (CH3), 6.96-6.97d, 7.577-7.588 d, (-CH=) 15.21 s (OH); 4.62 s (OH); 1.46-1.47 s (OH); 13C NMR (DMSO−d6, δ, ppm). Conclusion: Doxycycline is among broad-spectrum tetracycline. The Schiff bases derived from doxycycline show significantly highly active against gram negative bacteria as compared to doxycycline. In future further study on these derived compounds will help in market new derivative of doxycycline, which will have more broad-spectrum activity than doxycycline.


RSC Advances ◽  
2016 ◽  
Vol 6 (73) ◽  
pp. 68788-68797 ◽  
Author(s):  
Lingala Suresh ◽  
P. Sagar Vijay Kumar ◽  
T. Vinodkumar ◽  
G. V. P. Chandramouli

A ceria nanocatalyst was used for the one-pot, multicomponent condensation reaction of benzoylacetonitrile, aromatic aldehydes and 5-amino-triazole/tetrazole proceeding via C–C and C–N bond formation to deliver triazolo/tetrazolo[1,5-a]pyrimidines.


2020 ◽  
Vol 44 (9-10) ◽  
pp. 576-579 ◽  
Author(s):  
Hongmei Wang ◽  
XiuLian Zhu ◽  
Shouheng Deng ◽  
Qinhua Chen ◽  
Xiaohua Zeng

Seven ( E)-2-aroyl-4-(4-fluorobenzylidene)-5-oxopyrrolidines were synthesized via a tandem Ugi 4CC/SN cyclization sequence starting from a Baylis-Hillman-derived acid, primary amines, arylglyoxals, and isocyanides in one pot. In addition, the cytotoxicity of these compounds on the cervical cancer cell line HeLa was studied by MTT assay. The results showed that most of the compounds could inhibit the proliferation of HeLa cells significantly.


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