scholarly journals Synthesis, Characterization and Study of Antimicrobial Activities of Mannich Bases Incorporating 1,2,4-Triazole Nucleus

2021 ◽  
Vol 2 (01) ◽  
pp. 19-27
Author(s):  
Rhambus Rawat ◽  
Prem Shankar Deo ◽  
Bhushan Shakya
Keyword(s):  
Schiff Base ◽  
Heterocyclic Compounds ◽  
Environmental Science ◽  
Biological Activities ◽  
Antimicrobial Activities ◽  
Mannich Bases ◽  
New Drugs ◽  
Spectroscopic Techniques ◽  
Antibacterial And Antifungal Activities ◽  
Antibacterial And Antifungal

Heterocyclic compounds containing triazole moiety have great importance in the field of medicine, pharmaceuticals, biochemistry, biology, therapeutics, environmental science, and industry. Triazoles and their derivatives have been extensively used in the development of new drugs. Biological activities of Schiff bases are highly investigated, but Mannich bases are on the verge of their development, and they are being synthesized in large number nowadays. In this work, Mannich bases are synthesized by incorporation 1,2,4-triazole moiety through Schiff base using different amines. Mannich bases are found to exhibit highly effective antibacterial and antifungal activities. The formation of synthesized compounds - 1,2,4-triazole-5-thione, Schiff base (4) and Mannich bases (5a and 5b) - are confirmed and characterized by spectroscopic techniques like UV, FTIR 1H-NMR and 13C-NMR. The activity of the synthesized compounds was tested against bacterial and fungal strain.

Synthesis and investigation of 3,5-bis-linear and macrocyclic tripeptidopyridine candidates by using l-valine, N,N′-(3,5-pyridinediyldicarbonyl)bis-dimethyl ester as synthon

2019 ◽  
Vol 74 (6) ◽  
pp. 473-478 ◽  
Author(s):  
Abd El-Galil E. Amr ◽  
Ahmed M. Naglah ◽  
Nermien M. Sabry ◽  
Alhussein A. Ibrahim ◽  
Elsayed A. Elsayed ◽  
...  
Keyword(s):  
Staphylococcus Aureus ◽  
Candida Albicans ◽  
Organic Molecules ◽  
Biological Activities ◽  
Dimethyl Ester ◽  
Antimicrobial Activities ◽  
Current Work ◽  
Antifungal Activities ◽  
Antibacterial And Antifungal Activities ◽  
Antibacterial And Antifungal

AbstractInterest in the synthesis of heterocyclic organic molecules with peptide moieties has gained attention due to their potential biological activities. The current work aimed at synthesizing new macrocyclic tripeptide imides and evaluating their possible antimicrobial activities. A series of 11 derivatives were prepared from dimethyl 3,5-pyridinevalinyl ester either by NaOH or NH2NH2 treatment, followed by cyclization and further reaction with NaOH or NH2NH2. The majority of synthesized derivatives showed promising antibacterial and antifungal activities in comparison to standard known antibiotics. Compounds 5a and 7b showed the most potential antibacterial against Staphylococcus aureus and antifungal activities against Candida albicans, respectively.

scholarly journals FACILE SYNTHESIS, SPECTRAL STUDIES, DFT CALCULATIONS AND BIOLOGICAL ACTIVITIES OF NOVEL NI (II), CU (II), AND PD (II) COMPLEXES OF THIADIAZOLE ANALOGS

2017 ◽  
Vol 9 (4) ◽  
pp. 185
Author(s):  
Priyanka Bhatt ◽  
S. Deepthi ◽  
Ch. Ravi Shankar Kumar ◽  
Anjali Jha
Keyword(s):  
Conventional Method ◽  
Biological Activities ◽  
Antimicrobial Activities ◽  
Diffusion Method ◽  
Spectral Studies ◽  
Spectroscopic Techniques ◽  
Anticancer Activities ◽  
Facile Synthesis ◽  
Spectral Techniques ◽  
Antibacterial And Antifungal Activities

Objective: A facile synthesis of some novel Schiff base derivatives of 2-substituted-5-amino-thiadiazoles along with their Ni (II), Cu (II), and Pd (II) complexes were achieved by sonication and the conventional method. In addition to establish the structure by DFT studies and to explore antimicrobial and anticancer activities of these novel compounds.Methods: The precursor 2-substituted-5-amino-thiadiazoles (T1-T3), target ligands and their metal complexes were synthesized by ultra-sonication and conventional means. The isolated products were thoroughly characterized by physical and spectroscopic techniques including 1H-NMR, [13]C-NMR and IR spectroscopy. All characterized compounds were screened for antimicrobial activities using well diffusion method, and MTT assay was performed for cytotoxicity.Results: All novel compounds were synthesized by a green route i.e. ultra sonication and a noticeable improvement in yield with shorter reaction time than the conventional method were observed. The octahedral geometry was proposed for Ni (II)/Cu (II) complexes whereas square planar for Pd (II) complexes on the basis of the spectral techniques which were supported by DFT analysis by Gaussian03. On the analysis of antimicrobial activities, the compound T7 and T10 showed maximum antibacterial and antifungal activities respectively. However, compounds T25, T37, T31 found to be a potential cytotoxic compound with IC50 value 0.469, 0.865 and 1.131 μM respectively.Conclusion: Analysis of synthetic protocol, it could be concluded that ultra-sonication is the better method to synthesize these potential biological active moiety. On the whole Cu (II) and Ni (II) complexes showed promising activity towards all microorganisms while Pd (II) complex emerged an excellent moiety in carcinoma cell line.

scholarly journals Quinoline Functionalized Schiff Base Silver (I) Complexes: Interactions with Biomolecules and In Vitro Cytotoxicity, Antioxidant and Antimicrobial Activities

Molecules ◽  
2021 ◽  
Vol 26 (5) ◽  
pp. 1205
Author(s):  
Adesola A. Adeleke ◽  
Sizwe J. Zamisa ◽  
Md. Shahidul Islam ◽  
Kolawole Olofinsan ◽  
Veronica F. Salau ◽  
...  
Keyword(s):  
Schiff Base ◽  
Antioxidant Activities ◽  
Biological Activities ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Antimicrobial Activities ◽  
In Vitro Cytotoxicity ◽  
Spectroscopic Techniques ◽  
Antioxidant Power

A series of fifteen silver (I) quinoline complexes Q1–Q15 have been synthesized and studied for their biological activities. Q1–Q15 were synthesized from the reactions of quinolinyl Schiff base derivatives L1–L5 (obtained by condensing 2-quinolinecarboxaldehyde with various aniline derivatives) with AgNO3, AgClO4 and AgCF3SO3. Q1–Q15 were characterized by various spectroscopic techniques and the structures of [Ag(L1)2]NO3Q1, [Ag(L1)2]ClO4Q6, [Ag(L2)2]ClO4Q7, [Ag(L2)2]CF3SO3Q12 and [Ag(L4)2]CF3SO3Q14 were unequivocally determined by single crystal X-ray diffraction analysis. In vitro antimicrobial tests against Gram-positive and Gram-negative bacteria revealed the influence of structure and anion on the complexes′ moderate to excellent antibacterial activity. In vitro antioxidant activities of the complexes showed their good radical scavenging activity in ferric reducing antioxidant power (FRAP). Complexes with the fluorine substituent or the thiophene or benzothiazole moieties are more potent with IC50 between 0.95 and 2.22 mg/mL than the standard used, ascorbic acid (2.68 mg/mL). The compounds showed a strong binding affinity with calf thymus-DNA via an intercalation mode and protein through a static quenching mechanism. Cytotoxicity activity was examined against three carcinoma cell lines (HELA, MDA-MB231, and SHSY5Y). [Ag(L2)2]ClO4Q7 with a benzothiazole moiety and [Ag(L4)2]ClO4Q9 with a methyl substituent had excellent cytotoxicity against HELA cells.

scholarly journals Synthesis of disulphide-Schiff base derivatives and investigations of in vitro antimicrobial activities against some human pathogens

2017 ◽  
Vol 1 (3) ◽  
pp. 230-234 ◽  
Author(s):  
Sefa Durmuş ◽  
Aslıhan Dalmaz ◽  
Görkem Dülger ◽  
Duygu Bircan Kadıoğlu
Keyword(s):  
Schiff Base ◽  
Schiff Bases ◽  
Antimicrobial Activities ◽  
Diffusion Method ◽  
Control Group ◽  
Human Pathogens ◽  
Antibacterial And Antifungal Activities ◽  
Schiff Base Derivatives ◽  
Antibacterial And Antifungal

Abstract Thio-Schiff bases are becoming increasingly widespread in various branches such as the preparation of certain medicines, cosmetic products, and polymer production. In particular, the presence of antibacterial, antifungal, antiviral, antitumor and antimalarial properties of Schiff bases containing sulfur in the structure has made these compounds attractive in different disciplines. In this study, different derivatives of dimeric disulfide-Schiff bases have been synthesized. The antibacterial and antifungal activities of the synthesized these compounds were investigated in vitro against some human pathogens (Acinetobacter baumannii, Escherichia coli, Klebsiella pneumoniae, Staphylococcus aureus and Candida albicans, C. tropicalis, C. guilliermondii and C. glabrata). Test microorganisms were isolated from the patients appyling to Medical Faculty Hospital of Duzce University were used. Diffusion method was used to determine the antimicrobial activities of the compounds.standard antibacterial (Cefotaxime, Amoxicillin/clavulanicacid) and antifungal (Posaconazole) antibiotics were used as the control group and the results were compared. The result indicated that antimicrobial activity of Disulphide-Schiff Base Derivatives exhibited less activity against bacteria as compared to AMC30 (Amoxicillin/clavulanicacid), but highly effective against bacteria as compared to CTX30 (Cefotaxime). In addition, the compounds exhibited less activity against yeast.

scholarly journals Synthesis, characterization, electrochemical behavior and antibacterial/antifungal activities of [Cd(l)X2] complexes with a Schiff base ligand

2014 ◽  
Vol 79 (7) ◽  
pp. 793-804 ◽  
Author(s):  
Morteza Montazerozohori ◽  
Sahar Yadegari ◽  
Asghar Naghiha
Keyword(s):  
Schiff Base ◽  
Schiff Base Ligand ◽  
Electrochemical Behavior ◽  
Antimicrobial Properties ◽  
Antimicrobial Activities ◽  
Molar Conductance ◽  
Salmonella Spp ◽  
Antifungal Activities ◽  
Antibacterial And Antifungal Activities ◽  
Antibacterial And Antifungal

A new symmetrical bidentate Schiff base ligand (L) was applied for the synthesis of some new cadmium coordination compounds with general formula of [Cd(L)X2] in which X is halide and pseudo-halide. The ligand and all cadmium complexes were characterized by some techniques such as elemental analysis, FT-IR, 1H, 13C NMR, UV-Visible and molar conductance. Electrochemical behavior of ligand and Cd(II) complexes were investigated by cyclic voltammetry method. Morphology and shape of [Cd(L)Cl2] particles were depicted by SEM. Antimicrobial properties such as antibacterial and antifungal activities of the complexes as compared with ligand were checked against three Gram-negative bacteria; Escherichia coli (ATCC 25922), Pseudomunase aeroginosa (ATCC 9027) and Salmonella Spp. and two Gram-positive bacteria; Staphylococcus aureus (ATCC 6538) and Corynebacterium renale and three fungal strains including Aspergillus Niger, Penicillium chrysogenum and Candida albicans. The results revealed appropriate antibacterial and antifungal activities for all compounds, and it was also found that the coordination of ligand to Cd (II) lead to an increase in the antimicrobial activities in most of cases.

scholarly journals Synthesis, Characterization and Antimicrobial Studies of Schiff Base Ligand-Derived from Amoxicillin and Benzaldehyde

2016 ◽  
Vol 19 (2) ◽  
pp. 211-214
Author(s):  
Asif Iqbal ◽  
Farhana Hoque
Keyword(s):  
Schiff Base ◽  
Pharmaceutical Journal ◽  
Spectroscopic Techniques ◽  
Disc Diffusion ◽  
Melting Point Determination ◽  
Antibacterial And Antifungal Activities ◽  
Antimicrobial Studies ◽  
Point Determination ◽  
Antibacterial And Antifungal

Advanced research into synthetic chemistry has pointed out several organic compounds with antimicrobial potential. Schiff bases are one of such compounds. This research aims at the synthesis of a Schiff base out of a fairly common antibiotic amoxicillin and benzaldehyde. The synthesized compound was characterized by different spectroscopic techniques. It was also subjected to melting point determination, TLC and solubility tests. The Schiff base was screened for antibacterial and antifungal activities in-vitro by disc diffusion method.Bangladesh Pharmaceutical Journal 19(2): 211-214, 2016

scholarly journals Synthesis and Evaluation of Antimicrobial Activities of Novel N-Substituted Indole Derivatives

2020 ◽  
Vol 2020 ◽  
pp. 1-9
Author(s):  
Tanveer MahamadAlli Shaikh ◽  
Habtamu Debebe
Keyword(s):  
Antimicrobial Activities ◽  
New Drugs ◽  
Diffusion Method ◽  
Indole Derivatives ◽  
Disc Diffusion ◽  
Disc Diffusion Method ◽  
Standard Drug ◽  
Antibacterial And Antifungal Activities ◽  
Antibacterial And Antifungal

Indole motifs are one of the most significant scaffolds in the discovery of new drugs. We have described a synthesis of new N-substituted indole derivatives (1-3), and their in vitro antimicrobial activities were investigated. The synthesis of titled compounds has been demonstrated by utilizing commercially available starting materials. The antibacterial and antifungal activities were performed using new strains of bacteria Staphylococcus aureus, Escherichia coli, and Candida albicans using the disc diffusion method. Notably, the compound 4-(1-(2-(1H-indol-1-yl) ethoxy) pentyl)-N,N-dimethyl aniline (1) was found to be most potent than the other analogues (2 and 3), which has shown higher inhibition than the standard drug chloramphenicol.

scholarly journals Synthesis, Characterization and Antimicrobial Evaluation of Mannich Bases of 4-(Furan-2-yl-methyleneamino)-3-(2-hydroxyphenyl)-1H-1,2,4-triazole-5-thione

2021 ◽  
Vol 42 (1) ◽  
pp. 6-15
Author(s):  
Prem Shankar Deo ◽  
Rhambus Rawat ◽  
Bhushan Shakya
Keyword(s):  
Schiff Base ◽  
Bioactive Compounds ◽  
Biological Activities ◽  
Antimicrobial Activities ◽  
Mannich Bases ◽  
Spectral Techniques ◽  
Fungal Strains ◽  
Antimicrobial Evaluation ◽  
Ft Ir ◽  
Pharmacological Application

Triazole nucleus has drawn much attention since the last decade because of its various potent biological activities. The pharmacological application of triazoles has been widely recognized and well documented. Schiff and Mannich bases are both considered as bioactive compounds, however, there are not much of documentation about the Mannich bases as their study has begun lately. The main aim of this study was to synthesize new Mannich bases from Schiff base bearing 1,2,4-triazole nucleus to access their antimicrobial activities. The newly synthesized compounds 1,2,4-triazole-5-thione, Schiff base (4) and Mannich bases (5a & 5b) were characterized by spectral techniques like UV, FT-IR, and NMR. Mannich bases were tested against various bacterial (gm +ve and gm –ve) as well as fungal strains. The synthesized Mannich bases showed good to moderate activities against the tested bacterial and fungal strains.

scholarly journals Synthesis, characterization and antimicrobial activities of schiff base derived from thiourea and anisaldehyde and its Mn(II), Fe (II) and Co(II) complexes

2018 ◽  
Vol 11 (1) ◽  
pp. 20-24
Author(s):  
I.T. Siraj ◽  
B.U. Sambo
Keyword(s):  
Escherichia Coli ◽  
Schiff Base ◽  
Metal Ion ◽  
Condensation Reaction ◽  
Antimicrobial Activities ◽  
Spectral Studies ◽  
Tetradentate Ligand ◽  
Antibacterial And Antifungal Activities ◽  
Antibacterial And Antifungal ◽  
Metal Ligand

Complexes of Mn(II), Fe(II) and Co(II) with a Schiff base derived from condensation reaction of thiourea and o-anisaldehyde has been synthesized and characterized analytically and spectroscopically. Melting point of the Schiff base was found to be 160°C and the complexes decomposed within a temperature range of 215 to 275°C. Molarconductances of the complexes were found to be within 1.1 to 3.5W–1 cm2 mol–1 range. Magnetic moment indicated the complexes to be paramagnetic (4.03 to 5.71BM). Infrared spectrum of the Schiff base showed the azomethine peak at 1601cm–1 which shifted up to1687cm–1 in the complexes. The analytical and spectral studies revealed that all the metal(II) complexes are in 1:3 metal ligand ratio, with the Schiff base acting as tetradentate ligand towards the metal ion via azomethine – N, and methoxy –O and two chlorine atoms were further coordinated to the metal(II) ion. The synthesized ligand and its respective metal (II) complexes were screened for their antibacterial activity against Staphylococcus aureus and Escherichia coli strains and antifungal activity against Aspergillus flavus and Mucorindicus. The results revealed that, the Schiff base and the metal (II) complexes showed significant antibacterial and antifungal activities at high concentration.Keywords: Metal complexes, thiourea, anisaldehyde, characterization, antimicrobial

Synthesis, characterization and biological activities of 1,3,4-oxadiazole derivatives of nalidixic acid and their copper complexes

2019 ◽  
Author(s):  
Chem Int
Keyword(s):  
Nalidixic Acid ◽  
Copper Complexes ◽  
Biological Activities ◽  
Bidentate Coordination ◽  
Antibacterial And Antifungal Activities ◽  
Elemental Analyses ◽  
Oxadiazole Derivatives ◽  
Antibacterial And Antifungal ◽  
Derivatives Of ◽  
Substituted 1

A series of novel 1, 3, 4-oxadiazole analogues was synthesized from cyclization of hydrazones of substituted 1-ethyl-1,4-dihydro-7-methyl-4-oxo-1,8-naphthyridine-3-carbohydrazides were prepared from nalidixic acid. The structures of synthesized oxadiazole derivatives and their copper complexes were elucidated on the basis of FTIR, elemental analyses, 1H-NMR and atomic absorption spectral analysis. It was observed from spectral data that metal ligand ratio was 1:1 in all copper complexes and they were bidentate, coordination was found to be done through oxygen of 4-oxo group and nitrogen of oxadiazole ring. The synthesized compounds were further evaluated with biological activities and compared with parent hydrazones. Copper complexes possess antibacterial and antifungal activities better than the oxadiazoles while they have better antioxidant activity then copper complexes. Parent hydrazones were better in all biological activities than synthesized oxadiazoles.

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