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.

scholarly journals Spectral characterization, microbial activities and toxicity study of some newly synthesized hydrazone derivatives

2017 ◽  
Vol 5 (2) ◽  
pp. 54
Author(s):  
N. Kalaiarasi ◽  
S. Manivarman
Keyword(s):  
Biological Activities ◽  
Proton Nmr ◽  
Thiobarbituric Acid ◽  
Spectral Characterization ◽  
Toxicity Study ◽  
Microbial Activities ◽  
Phenyl Hydrazine ◽  
Antibacterial And Antifungal Activities ◽  
Antibacterial And Antifungal ◽  
Derivatives Of

Hydrazone derivatives of 2-Thioxodihyropyrimidine-2-dione were synthesized by addition of thiobarbituric acid with phenyl hydrazine, dinitrophenyl hydrazine, semicarbazide, thiosemicarbazide and benzohydrazide respectively. Structures of these synthesized compounds are characterized by means of UV, IR, Proton-NMR, Carbon- NMR. Finally the hydrazone derivatives synthesized are screened for biological activities namely antibacterial and antifungal activities. Also in addition the toxicity studies of the compounds are also performed.

Synthesis of a Series of Novel 2-Amino-5-Substituted 1,3,4-oxadiazole and 1,3,4-thiadiazole Derivatives as Potential Anticancer, Antifungal and Antibacterial Agents

2021 ◽  
Vol 17 ◽  
Author(s):  
Em Canh Pham ◽  
Tuyen Ngoc Truong ◽  
Nguyen Hanh Dong ◽  
Duy Duc Vo ◽  
Tuoi Thi Hong Do
Keyword(s):  
Cell Line ◽  
Biological Activities ◽  
Chemical Properties ◽  
Diffusion Method ◽  
Anticancer Activities ◽  
Molecular Docking Study ◽  
Antifungal Activities ◽  
Antibacterial And Antifungal Activities ◽  
Thiadiazole Derivatives ◽  
Antibacterial And Antifungal

Background: Many compounds containing a five-membered heterocyclic ring display exceptional chemical properties and versatile biological activities. Objective: The objective of the present study was the desire to prepare the 5-substituted 2-amino-1,3,4-oxadiazole and 2-amino-1,3,4-thiadiazole derivatives and evaluate their potential anticancer, antibacterial and antifungal activities. Methods: Twenty-seven derivatives were synthesized by iodine-mediated cyclization of semicarbazones or thiosemicarbazones obtained from condensation of semicarbazide or thiosemicarbazide and aldehydes. The structures were confirmed by 1H-NMR, 13C-NMR and MS spectra. The antibacterial and antifungal activities were evaluated by diffusion method and the anticancer activities were evaluated by MTT assay. Results: Twenty-seven derivatives have been synthesized in moderate to good yields. A number of derivatives exhibited potential antibacterial, antifungal and anticancer activities. Conclusion: Compounds (1b, 1e and 1g) showed antibacterial activity against Streptococcus faecalis, MSSA and MRSA with MIC ranging between 4 to 64 µg/mL. Compound (2g) showed antifungal activity against Candida albicans (8 µg/mL) and Aspergillus niger (64 µg/mL). Compound (1o) exhibited high cytotoxic activity against HepG2 cell line (IC50 value 8.6 µM), which is comparable to the activity of paclitaxel, and is non-toxic on LLC-PK1 normal cell line. The structure activity relationship and molecular docking study of the synthesized compounds are also reported.

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 Synthesis and Characterizations ofN2(Aryl)-N4,N6-bis (6, 7-dichloro-1, 3-benzothiazol-2-yl)-1, 3, 5-triazine-2, 4, 6-triamines as Biological Potent Agents

2010 ◽  
Vol 7 (1) ◽  
pp. 210-214 ◽  
Author(s):  
B. B. Baldaniya
Keyword(s):  
Antibacterial Activity ◽  
Mass Spectra ◽  
Antifungal Activities ◽  
Antibacterial And Antifungal Activities ◽  
Elemental Analyses ◽  
Frame Work ◽  
Different Strains ◽  
Antibacterial And Antifungal

Some novelN2-(Aryl)-N4,N6-bis (6, 7-dichloro-1, 3-benzothiazol-2-yl)-1, 3, 5-triazine-2, 4, 6-triamines (4a-u) have been synthesized and characterized by elemental analyses, IR, NMR, and mass spectra. The products have been tested for their antibacterial activity against gram (+)ve and gram (-)ve bacteria and also on different strains of fungi. Introduction of –OH, -OCH3, -NO2, -Cl and –Br groups to the heterocyclic frame work enhanced antibacterial and antifungal activities.

scholarly journals Ferrocene Derivatives Carrying Urea, Thiourea, and Sulfonamide Moieties: Synthesis and Evaluation of Antibacterial and Antifungal Activities

2013 ◽  
Vol 2013 ◽  
pp. 1-7 ◽  
Author(s):  
Serkan Yavuz ◽  
Hilal Yıldırım
Keyword(s):  
Inhibitory Concentration ◽  
Antibacterial Activities ◽  
Klebsiella Pneumonia ◽  
Gram Negative Bacteria ◽  
Ferrocene Derivatives ◽  
Antifungal Activities ◽  
Gram Positive Bacteria ◽  
Antibacterial And Antifungal Activities ◽  
Elemental Analyses ◽  
Antibacterial And Antifungal

In the present study, some novel ferrocene derivatives carrying urea, thiourea, and sulfonamide groups were synthesized, and all compounds were characterized by spectral and elemental analyses. These compounds were screened for their antibacterial activities and also their minimum inhibitory concentration (MIC) against Gram-positive bacteria (Staphylococcus aureusandBacillus subtilis) and Gram-negative bacteria (Klebsiella pneumoniaandEscherichia coli) and antifungal activities againstSaccharomyces cerevisiaeandCandida albicans. Amongst the tested compounds,4b,4c,5b, and6bdisplayed excellent antimicrobial activity.

Synthesis and antibacterial and antifungal activities of thiourea derivatives of the alkaloid anabasine

2011 ◽  
Vol 45 (1) ◽  
pp. 15-18 ◽  
Author(s):  
I. V. Kulakov ◽  
O. A. Nurkenov ◽  
S. B. Akhmetova ◽  
R. B. Seidakhmetova ◽  
Z. M. Zhambekov
Keyword(s):  
Thiourea Derivatives ◽  
Antifungal Activities ◽  
Antibacterial And Antifungal Activities ◽  
Antibacterial And Antifungal ◽  
Derivatives Of

scholarly journals Synthesis and Antimicrobial Screening of Novel 4-Substituted Phenyl-5-[1-(4-fluorophenyl)-1,3-dihydroisobenzofuran-5-yl]-2H-1,2,4-triazole-3-thiones

2014 ◽  
Vol 2014 ◽  
pp. 1-7 ◽  
Author(s):  
Namratha Bhandari ◽  
Santosh L. Gaonkar
Keyword(s):  
Convenient Method ◽  
Nmr Spectra ◽  
Spectral Studies ◽  
Antimicrobial Screening ◽  
Antifungal Activities ◽  
H Nmr ◽  
Antibacterial And Antifungal Activities ◽  
Elemental Analyses ◽  
Antibacterial And Antifungal ◽  
C Nmr

The paper describes a convenient method for the preparation of 4-substituted phenyl-5-[1-(4-fluorophenyl)-1,3-dihydroisobenzofuran-5-yl]-2H-1,2,4-triazole-3-thiones. The structures of the synthesized compounds are established by the results of LCMS, 1H NMR, 13C NMR, and IR and elemental analyses. The mercaptotriazoles are indicated to be in thione form by 1H NMR spectra. All the synthesized compounds have been screened for antibacterial and antifungal activities. Compounds 12d and 12h exhibit encouraging results, while the remaining compounds show moderate activities. On the basis of spectral studies, formation of 2-amino-1,3,4-thiadiazoles from the isobenzofuran acyl thiosemicarbazides 11(a–h) is ruled out.

scholarly journals SYNTHESIS, CHARACTERIZATION AND IN VITRO STUDY OF ANTIBACTERIAL, ANTIFUNGAL ACTIVITIES OF SOME NOVEL DIHYDROPYRIMIDINTHIONE DERIVATIVES

2014 ◽  
Vol 44 (4) ◽  
pp. 289-293
Author(s):  
S. BALUJA ◽  
S. CHANDA ◽  
R. BHALODIA ◽  
R. TALAVIYA
Keyword(s):  
Biological Activities ◽  
Wide Spectrum ◽  
In Vitro Study ◽  
Dimethyl Formamide ◽  
Mass Spectral Data ◽  
Antifungal Activities ◽  
Mass Spectral ◽  
Antibacterial And Antifungal Activities ◽  
Antibacterial And Antifungal

Dihydropyrimidinthione is an important class of heterocyclic compounds which exhibits wide spectrum of biological activities. In the present study, some bio-active dihydropyrimidinthione derivatives have been synthesized and their characterization was done by IR, NMR and mass spectral data. The antibacterial and antifungal activities of synthesized compounds have also been studied in N,N-dimethyl formamide and Dimethyl sulfoxide.

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