MICROWAVE ASSISTED SYNTHESIS OF BIPHENYL BASED SCHIFF’S BASES AND THEIR ANTIMICROBIAL EVALUATION

INDIAN DRUGS ◽  
2018 ◽  
Vol 55 (03) ◽  
pp. 13-18
Author(s):  
R. Somani ◽  
◽  
P. Dubey ◽  
S. Zine

Schiff’s base constitutes a significant class of compounds for new drug development. They are widely used for industrial purposes and also exhibit a broad range of biological activities. The search for Schiff’s base containing compounds with more selective activity and lower side effects continues to be an active area of argument examination in medicinal chemistry. The biphenyl molecule consists of two connected phenyl rings. Biphenyl ring scaffolds are fairly non-reactive in nature. They enhance the log-P values; increase the tropical polar surface area (TPSA) of the molecule, act as hydrophobic carrier across biological membrane, thus, increasing the bioavailability of compounds. In the present work, a series of Schiff’s bases of biphenyl-4-carboxylic acid have been synthesized. These derivatives were characterized by elemental analysis, IR, and 1H NMR spectral data and have been explored for anti-bacterial, anti-fungal and anti-tubercular activities. The synthesized compounds have shown excellent anti-fungal potential, making them good candidates for future studies in antifungal research.

Author(s):  
N.N. Kansagara ◽  
V.R. Dangar ◽  
V.R. Shah

Schiff’s bases are obtained on heating an aldehydes with aromatic amine in presence of glacial acetic acid. These are the compounds containing characteristic –HC=N– group. Aryl amino methyl derivatives of heterocyclic compounds to synthesize by selective reduction of schiff’s bases (imine group) with sodiumborohydride in controlled experimental condition. Schiff’s base of N-Aryl-1-[6-methyl-2-(4-methylphenyl)imidazo[1,2-a]pyridin-3-yl]methanimines & Aryl amines of N-Aryl-1-[6-methyl-2-(4-methylphenyl)imidazo[1,2-a]pyridin-3-yl]methanamines were prepared. Their chemical structures were confirmed by means of IR, NMR, Mass data and by elemental analysis. All of the synthesized compounds were tested for their antibacterial and antifungal activity.


Author(s):  
Mousumi Chakraborty ◽  
Sanjay Baweja ◽  
Sunita Bhagat ◽  
TejpalSingh Chundawat

Abstract In the present study Schiff’s bases are synthesized by the conventional as well as by microwave irradiation. Excellent yield within short reaction time is obtained using microwave irradiation along with other advantages like mild reaction condition, non-hazardous and safer environmental conditions. The effects of temperature, reactant molar ratio, and microwave power variation on yield are observed. Mathematical model has been developed using matlab software to obtain the yield as a function of microwave power. Kinetic study of the reaction has also been attempted. Schiff’s bases structures are confirmed by IR, 1HNMR, Mass Spectra and elemental analysis.


2021 ◽  
Vol 43 (2) ◽  
pp. 227-227
Author(s):  
Muhammad Anwar Saeed Muhammad Anwar Saeed ◽  
Hizbullah Khan Hizbullah Khan ◽  
Muhammad Sirajuddin Muhammad Sirajuddin ◽  
Syed Muhammad Salman Syed Muhammad Salman

The manuscript describes the binding of DNA as well as biological studies of some mixed ligand dithiocarbamate Palladium (II) complexes (1-5). The observed compounds are of general formulae [PdCl(DT)(PR3)]. The dithiocarbamate “DT” and “PR3” groups are varied among the studied complexes as DT = bis[(2-methoxyethyl) dithiocarbamate)] (1 and 2), dibutyl dithiocarbamate (4 and 5), bis[(2-ethyl) hexyl dithiocarbamate)] (3); PR3 = triphenyl phosphine (1), benzy diphenyl phosphine (2), diphenyl-tert-butyl phpsphine (3), diphenyl-p-tolyl phosphine (4) and diphenyl-2-methoxy phenyl phosphine (5). The synthesized complexes were screened for DNA binding study via (UV Visible spectrophotometry and Viscometery) and biological activities such as anti-bacterial and anti-fungal, Molinspiration calculations and antioxidant potencies stimulated by hydrogen peroxide in human blood lymphocytes. In case of drug DNA interaction, complexes showed some sort of interaction with DNA solution. Almost all the complexes exhibited moderate antifungal and antibacterial behavior (against Gram positive and negative bacterial strains). The Molinspiration calculation study revealed that the said Pd (II) mixed complexes are biologically significant drugs having adequate molecular properties regarding drug likeness, except the log P values of complexes 3-5 because some structural adjustments must be done for enhancement of their bioavailability and hydrophilic nature. Regarding the antioxidant potential of complexes 1, 2 and 4, the H2O2 treatment of complexes violently decreased the action of antioxidant enzymes, superoxide dismutase and catalase and enhanced the level of thiobarbituric acid-reacting substances. Under experimental conditions, we conclude that all complexes act as anti-mutagens as they significantly suppress H2O2-induced oxidative damage at non-genotoxic concentrations.


2009 ◽  
Vol 2009 (4) ◽  
pp. 208-211 ◽  
Author(s):  
Jing Zhang ◽  
Lixue Zhang ◽  
Xinxiang Lei ◽  
Changfeng Zhou ◽  
Xiaodan Fu ◽  
...  

Sixteen novel Schiff's bases have been synthesised in high yields from 4-amino-3-(3-hydroxybutyl)-1 H-1, 2, 4-triazole-5-thione. All the newly synthesised compounds have been characterised by elemental analysis, IR, 1H NMR, 13C NMR and MS. Plant growth-regulating activity tests showed that most compounds have remarkable effects on the growth of wheat and radish at a mass concentration of 50μg mL−1.


2020 ◽  
Vol 11 (SPL4) ◽  
pp. 1006-1011
Author(s):  
Khudheyer Jawad Kadem

In this work, three novel Schiff's bases subsidiaries were set up from Ethylene Diamine Tetra Acetic corrosive Derivatives(K1, K2 and K3); (K1) which was blend from response of EDTA with 4-hydroxybenzaldehyde and 2,4-dintrophenyl hydrazine. (K2) which was union from response of EDTA with vinilline and 2,4-dintrophenyl hydrazine. (K3) which was amalgamation from response of EDTA with 4-aminoacetophenone and 2,4-dintrophenyl hydrazine after that combination three novel hetrocyclic compound Containing Sulfur molecule; Derivative with compounds containing carbonyl group (aldehyde or ketone) the carbonyl group of aldehyde or ketone react with primary amine to produce mine compounds (Schiff bases), Reaction of produced Schiff base compounds with mercaptoacetic acid (thioglycolic acid) to synthesized new heterocyclic compounds Compounds with heterogeneous ring are characterized by having many biological activities Which attracts the attention of researchers, and accordingly various derivatives containing sulfur were prepared for heterocyclic compounds, these prepared compounds can have inhibitory activity for some bacteria, fungi, and viruses. (M1,M2 and M3)which were union from response of (K1,K2 and K3) individually with marcaptoacetic acid. All of the Schiff’s bases derivatives and hetrocyclic compound Containing Sulphur atom were characterized and identified by spectroscopic methods ( FT-IR and 1H-NMR) spectroscopies.


Author(s):  
D.T. Biradar ◽  

Objective: Many methods can be found in literature for the synthesis a Oxazines and Thiazines. Few are reported for one-pot multi component cyclo-condensation of an alkayane urea / Thiourea and Aldehyde to 2- amino-4H-1, 3-Oxazines or Thiazines. Different catalysts are reported like Trifluoro-acetic acid, glacial acetic acid under reflux condition Mandal and Co-workers have utilized perchloric acid (HClO4) supported on silica gel as catalyst under solvent free condition ytterbium trifluorate [Yb(OTF)3] plays role of Lewis acid. It is also used in several Diel’s-Alder cyclo-addition reactions. Inspired these observations, development of simple effective synthetic strategy for the synthesis of 2-amino-4H-1, 3-Oxazium & Thiazines was attempted. Material and Methods: One pot multi-component synthesis of Schiff’s base as new ligand an their complexes with Ni, Fe, Co and Cu and developed using 2-amino-4H-1,3 Oxazines /Thiazines and substituted Aldehydes, different catalyst are used to synthesize of 2-amino 4H-1,3 Oxazines. Its characterization is confirmed by taking IR, NMR spectra. The Schiff’s base act as ligand is bidentate, when it is treated to metal complexes in 1:1 ratio (metal: ligand) complexes are formed. Result: By using the bioactive molecules like 2-amino-4H-1, 3 Oxazine / Thiazines, Schiff’s Bases can be synthesized by using different aldehydes. These Schiff’s Bases has antitumor, antipyretic, anti-inflammatory property. And these Schiff’s bases treated with bioactive metals like Co, Fe, Cu, Zn which enhances their bio-activity. Conclusion: All these synthesized Schiff’ Bases and their metal complexes having bioactive properties.


2021 ◽  
Vol 37 (1) ◽  
pp. 187-193
Author(s):  
D. G. Anuse ◽  
V. J. Desale ◽  
B. R. Thorat ◽  
D. D. Anuse ◽  
S. G. Jagadhani ◽  
...  

The substituted 2-Aminobenzothiazole and ethyl 2-(4-formyl-3-hydroxyphenyl)-4-methylthiazole-5-carboxylate in methanol mix together and heat the reaction mixture for overnight, It gives Schiff’s bases (derivatives of substituted aminobenzothiazole) 3. This compound 3 when treated with Zinc Chloride it gives Zinc metal complex of Schiff’s bases 4 and if compound 3 was treated with Lanthanum chloride gives Lanthanum metal complex of Schiff’s bases 5, which shows marked biological activities.


2021 ◽  
Vol 10 (4) ◽  
pp. 151-155
Author(s):  
Amir Hassan ◽  
Nawaz Khan

A series of novel acyl hydrazone derivatives of benzimidazole-2-thiol were synthesized. The acylhydrazide was condensed with a series of aromatic substituted aldehydes to yield the tetra decylhydrazone Schiff”s bases of benzimidazole-2-thiol. The acylhydrazide was taken in methanol in round bottom flask added 2-3 drops acetic acid and refluxed on hotplate the reaction mixture was monitored with TLC. After completion of reaction the product was precipitated in ice cool water, washed and dried. The synthesized compounds were screened for different biological activities such as antimicrobial, antihistamine, neutropic, analgesic, antiprotozoal, antimalarial, antiallergic, antioxidant, anticonvulsant, anti-tubercular and have shown a good results.


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