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

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.

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

10.31221/osf.io/g7mx8 ◽

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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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

Medicinal Chemistry ◽

10.2174/1573406417666210803170637 ◽

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.

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Convenient one pot synthesis of some novel derivatives of thiazolo[2,3-b]dihydropyrimidinone possessing 4-methylthiophenyl moiety and evaluation of their antibacterial and antifungal activities

European Journal of Medicinal Chemistry ◽

10.1016/j.ejmech.2006.09.003 ◽

2007 ◽

Vol 42 (3) ◽

pp. 380-385 ◽

Cited By ~ 122

Author(s):

Mithun Ashok ◽

Bantwal Shivarama Holla ◽

Nalilu Suchetha Kumari

Keyword(s):

One Pot ◽

Antifungal Activities ◽

One Pot Synthesis ◽

Antibacterial And Antifungal Activities ◽

Antibacterial And Antifungal ◽

Derivatives Of

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Studies on Antibacterial and Antifungal Activities of Some Derivatives of Tributyltin (IV) of Salicylic Acid

10.9734/bpi/nvst/v2/3899f ◽

2021 ◽

pp. 128-132

Author(s):

Pankaj Mittal

Keyword(s):

Salicylic Acid ◽

Antifungal Activities ◽

Antibacterial And Antifungal Activities ◽

Antibacterial And Antifungal ◽

Derivatives Of

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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

Zeitschrift für Naturforschung B ◽

10.1515/znb-2019-0006 ◽

2019 ◽

Vol 74 (6) ◽

pp. 473-478 ◽

Cited By ~ 2

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.

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

Pharmaceutical Chemistry Journal ◽

10.1007/s11094-011-0551-9 ◽

2011 ◽

Vol 45 (1) ◽

pp. 15-18 ◽

Cited By ~ 9

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

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

Latin American Applied Research - An international journal ◽

10.52292/j.laar.2014.454 ◽

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

Amrit Research Journal ◽

10.3126/arj.v2i01.39894 ◽

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.

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Synthesis of some 1H-1,5-benzodiazepine Series Containing Chromene Ring from α,β-Unsaturated Ketones of 6-Acetyl-5-Hydroxy-4-Methylcoumarin

Current Organic Synthesis ◽

10.2174/1570179417666200415152105 ◽

2020 ◽

Vol 17 (5) ◽

pp. 404-410 ◽

Cited By ~ 3

Author(s):

Duong Ngoc Toan ◽

Nguyen Dinh Thanh ◽

Mai Xuan Truong ◽

Nguyen Minh Thao

Keyword(s):

Biological Activities ◽

Absolute Ethanol ◽

Diffusion Method ◽

Disk Diffusion Method ◽

Unsaturated Ketones ◽

Molar Ratios ◽

Antibacterial And Antifungal Activities ◽

Substituted Benzaldehydes ◽

Antibacterial And Antifungal ◽

Layer Chromatography

Background: Reaction of α,β-unsaturated ketones with o-phenylenediamine afforded corresponding 2,3-dihydro-1H-1,5-benzodiazepines. Objective: α,β-Unsaturated ketones of 6-acetyl-5-hydroxy-4-methylcoumarin are precursors for synthesis of 2,3-dihydro-1H-1,5-benzodiazepines by a reaction with o-phenylenediamine. Methods: Enones of 6-acetyl-5-hydroxy-4-methylcoumarin were prepared from this ketone and (un)substituted benzaldehydes in the presence of piperidine, triethylamine, or pyridine as a catalyst in absolute ethanol with 1:1 molar ratios, respectively. 2',3'-Dihydro-1H-1',5'-benzodiazepines were synthesized by using the reaction of these enones with o-phenylenediamine in absolute ethanol in the presence of glacial acetic acid as a catalyst. Their biological activities were evaluated using the disk diffusion method. Results: Seven new 2',3'-dihydro-1H-1',5'-benzodiazepines were obtained and their structures were confirmed by thin-layer chromatography, IR, NMR and MS spectra. Some synthesized benzodiazepines showed antibacterial and antifungal activities against Escherichia coli (Gram-(−) bacterium), Staphylococus epidermidis (Gram-(+) bacterium). Candida albicans (fungus). Conclusion: The formation of enones from 6-acetyl-5-hydroxy-4-methylcoumarin and (un)substituted benzaldehydes could be catalyzed by piperidine, triethylamine, pyridine to afford similar yields. 2',3'-dihydro-1H- 1',5'-benzodiazepines have been synthesized from the aforementioned enones and o-phenylenediamine.

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