Synthesis and Antimicrobial Activity of Novel Series of Diversely Substituted Acetyl Pyrazoline Bearing Biphenyl Carbonitrile Motif

Novel series of diversely substituted acetyl pyrazoline having biphenyl carbonitrile motif have been synthesized. The reaction of 2-cyno-4’-bromomethyl biphenyl with1-(4-hydroxy-phenyl)-ethanone resulted in acetophenone derivative of biphenyl-2-carbonitrile. This acetophenone derivative was condensed with substituted aromatic aldehyde in mixed solvent resulted in various substituted chalcones. These chalcones were further cyclized using hydrazine hydrate in presence of glacial acetic acid to produce titled compound derivatives. The chemical structures of synthesized compounds were elucidated by 1H-NMR, 13C-NMR FT-IR and mass spectra. Synthesized compounds were screened for their antimicrobial activity by broth dilution method. Out of twelve newly synthesized compounds, eight compounds are found to be equipotent to Ampicillin.

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Isolation and Antimicrobial Activity of β-Sitosterol-3-O-Glucoside from Lannea Kerstingii Engl. & K. Krause (Anacardiacea)

Journal of Health and Allied Sciences NU ◽

10.1055/s-0040-1708607 ◽

2016 ◽

Vol 06 (01) ◽

pp. 004-008

Author(s):

Njinga N. S. ◽

Sule M. I. ◽

Pateh U. U. ◽

Hassan H. S. ◽

Abdullahi S. T. ◽

...

Keyword(s):

Antimicrobial Activity ◽

Wide Spectrum ◽

Diffusion Method ◽

Dilution Method ◽

Minimum Fungicidal Concentration ◽

E Coli ◽

H Nmr ◽

Vacuum Liquid Chromatography ◽

Broth Dilution ◽

C Nmr

AbstractThe emergence of more and more drug resistance bacteria has led to the study of the antimicrobial activity of the compound isolated from Lannea kerstingii Engl. & K. Krause (Anacardiacea) since the active principles of many drugs found in plants are secondary metabolites. A compound was isolated using dry vacuum liquid chromatography and eluting with CHCl3 -EtOAc and monitored using TLC. 3 1 13 The glycoside was characterized using 1 H NMR and 13 C NMR spectra recorded in DMSO-d6 at 400 MHz and 125 MHz, respectively. The antimicrobial activity of the compound was determined using agar diffusion method. The minimum inhibitory concentration (MIC) and minimum bactericidal/minimum fungicidal concentration (MBC/MFC) was determined using broth dilution method. The compound isolated was found to be β-sitosterol-3-O-glucoside. The β-sitosterol-3-O-glucoside (200μg/ml) was active against S. aureus, Methicillin Resistant Staphylococcus aureus, P. mirabilis, S. typhi, K. pneumoniae, E. coli, B. subtilis with zone of inhibition ranging from 24mm to 34mm and inactive against P. aeroginosa and Proteus vulgaris. It was also active against the fungi C. albicans and C. tropicalis but inactive against C. krusei. The MIC ranged from 25 to 50 μg/ml while the MBC/MFC ranged from 50 to 200 μg/ml. These results show the wide spectrum antimicrobial activity of β-sitosterol-3-O-glucoside.

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Synthesis, Characterization, and Antimicrobial Activity of Methyl-2-aminopyridine-4-carboxylate Derivatives

Journal of Chemistry ◽

10.1155/2013/312961 ◽

2013 ◽

Vol 2013 ◽

pp. 1-5 ◽

Cited By ~ 1

Author(s):

S. Nagashree ◽

P. Mallu ◽

L. Mallesha ◽

S. Bindya

Keyword(s):

Antimicrobial Activity ◽

Spectral Studies ◽

H Nmr ◽

Chemical Structures ◽

Elemental Analyses ◽

Ft Ir

A series of methyl-2-aminopyridine-4-carboxylate derivatives,3a–f,were synthesized in order to determine theirin vitroantimicrobial activity. The chemical structures of the synthesized compounds were confirmed by elemental analyses, FT-IR, and1H NMR spectral studies. Among the synthesized compounds,3cand3dshowed good antimicrobial activity compared to other compounds in the series.

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SYNTHESIS AND STRUCTURAL ELUCIDATION OF AMINO ACETYLENIC AND THIOCARBAMATES DERIVATIVES FOR 2-MERCAPTOBENZOTHIAZOLE AS ANTIMICROBIAL AGENTS

International Journal of Pharmacy and Pharmaceutical Sciences ◽

10.22159/ijpps.2017v9i2.15760 ◽

2017 ◽

Vol 9 (2) ◽

pp. 192

Author(s):

Aseel Alsarahni ◽

Zuhair Muhi Eldeen ◽

Elham Al-kaissi ◽

Ibrahim Al- Adham ◽

Najah Al-muhtaseb

Keyword(s):

Antimicrobial Activity ◽

Elemental Analysis ◽

Antimicrobial Agents ◽

Diffusion Method ◽

Benzothiazole Derivatives ◽

H Nmr ◽

Ft Ir ◽

Potential Antimicrobial Activity ◽

C Nmr

Objective: To design and synthesize amino acetylenic and thiocarbonate of 2-mercapto-1,3-benthiazoles as potential antimicrobial agents.Methods: A new series of 2-{[4-(t-amino-1-yl) but-2-yn-1-yl] sulfanyl}-1,3-benzothiazole derivatives (AZ1-AZ6), and S-1,3-benzothiazol-2-yl-O-alkyl carbonothioate derivatives were synthesised, with the aim that the target compounds show new and potential antimicrobial activity. The elemental analysis was indicated by the EuroEA elemental analyzer, and biological characterization was via IR, 1H-NMR, [13]C-NMR, DSC were determined with the aid of Bruker FT-IR and Varian 300 MHz spectrometer using DMSO-d6 as a solvent. In vitro antimicrobial activity, evaluation was done for the synthesised compounds, by agar diffusion method and broth dilution test. The minimum inhibitory concentration (MIC) and the minimum bactericidal concentration (MBC) were determined. Results: The IR, 1H-NMR, 13C-NMR, DSC and elemental analysis were consistent with the assigned structures. Compound of 2-{[4-(4-methylpiperazin-1-yl)but-2-yn-1-yl] sulfanyl}-1,3-benzothiazole (AZ1), 2-{[4-(2-methylpiperidin-1-yl)but-2-yn-1-yl]sulfanyl}-1,3-benzothiazole (AZ2), 2-{[4-(piperidin-1-yl) but-2-yn-1-yl]sulfanyl}-1, 3-benzothiazole (AZ6), S-1,3-benzothiazol-2-yl-O-ethyl carbonothioate (AZ7), and S-1,3-benzothiazol-2-yl-O-(2-methylpropyl) carbonothioate (AZ9) showed the highest antimicrobial activity against Pseudomonas aeruginosa (P. aeruginosa), AZ-9 demonstrated the highest antifungal activity against Candida albicans (C. albicans), with MIC of 31.25 µg/ml.Conclusion: These promising results promoted our interest to investigate other structural analogues for their antimicrobial activity further.

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Design, preparation and characterization of a new ionic liquid, 1,3-disulfonic acid benzimidazolium chloride, as an efficient and recyclable catalyst for the synthesis of tetrahydropyridine under solvent-free conditions

RSC Advances ◽

10.1039/c5ra10699k ◽

2015 ◽

Vol 5 (83) ◽

pp. 67405-67411 ◽

Cited By ~ 12

Author(s):

Mohsen Abbasi

Keyword(s):

Ionic Liquid ◽

Mass Spectra ◽

Recyclable Catalyst ◽

Solvent Free ◽

Disulfonic Acid ◽

H Nmr ◽

Solvent Free Conditions ◽

Ft Ir ◽

C Nmr

In the present work, 1,3-disulfonic acid benzimidazolium chloride as a new ionic liquid, is synthesized, and characterized by studying its FT-IR, 1H NMR, 13C NMR as well as mass spectra.

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Synthesis of New Imidazolidine and Tetrahydropyrimidine Derivatives

Advances in Chemistry ◽

10.1155/2014/834641 ◽

2014 ◽

Vol 2014 ◽

pp. 1-4 ◽

Cited By ~ 1

Author(s):

Hamid Beyzaei ◽

Reza Aryan ◽

Zahra Keshtegar

Keyword(s):

Ring Opening ◽

Reaction Times ◽

Reaction Conditions ◽

Ir Spectrometry ◽

H Nmr ◽

Chemical Structures ◽

Thioamide Group ◽

Solvent Free Conditions ◽

Ft Ir ◽

C Nmr

Synthesis of new imidazolidine and tetrahydropyrimidine derivatives 3a, b and 4a–c as cyclic 1,3-diamines under two reaction conditions (A and B) is described. Under reaction conditions-A, a suspension of (E)-2-cyano-2-(oxazolidin-2-ylidene)ethanethioamide 1 (1 eq.) and diaminoalkanes 2a–e (2 eq.) in absolute ethanol is heated under reflux for 16–22 h to afford 3a, b and 4a–c. Alternatively, under reaction conditions-B, a solution of thioamide 1 (1 eq.) in diaminoalkanes 2a–e (3 eq.) is stirred under solvent-free conditions at room temperature for 3 days to give desired products. Reaction conditions-A for having higher yields, shorter reaction times, and required less diamines is more effective than reaction conditions-B. Oxazolidine ring opening is observed by reacting compound 1 with all of the diamines 2a–e, but the thioamide group only reacts with nonbulky diamines 2a, b. The chemical structures of novel compounds were confirmed by 1H NMR, 13C NMR, elemental analysis, and FT-IR spectrometry.

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Synthesis, Spectral and Microbial Studies of Some Novel Schiff Base Derivatives of 4-Methylpyridin-2-amine

E-Journal of Chemistry ◽

10.1155/2009/247209 ◽

2009 ◽

Vol 6 (4) ◽

pp. 1205-1210 ◽

Cited By ~ 3

Author(s):

J. J. Vora ◽

S. B. Vasava ◽

K. C. Parmar ◽

S. K. Chauhan ◽

S. S. Sharma

Keyword(s):

Schiff Base ◽

Antimicrobial Activities ◽

Dilution Method ◽

Mass Spectral ◽

H Nmr ◽

Schiff Base Derivatives ◽

Ft Ir ◽

Acid Catalyzed ◽

Derivatives Of ◽

Broth Dilution

Schiff base derivatives ofN-{(1E)-[3-(mono or di-substituted aryl)-1-phenyl-1H-pyrazol-4-yl]methylene{-4-methylpyridin-2-amine were synthesized by the acid catalyzed condensation of 3-(mono- or di- substituted aryl)-1-phenyl-1H-pyrazole-4-carbaldehyde derivatives with 4-methylpyridin-2-amine. Schiff base derivatives were characterized by FT-IR,1H-NMR, Mass spectral analysis and elemental analysis. All the synthesized compounds have been screened for their antimicrobial activities by using broth dilution method.

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Approach for the Synthesis of Potent Antimicrobials Containing Pyrazole, Pyrimidine and Morpholine Analogues

International Letters of Chemistry Physics and Astronomy ◽

10.18052/www.scipress.com/ilcpa.69.87 ◽

2016 ◽

Vol 69 ◽

pp. 87-96 ◽

Cited By ~ 1

Author(s):

Nisheeth C. Desai ◽

Bonny Y. Patel ◽

Bharti P. Dave

Keyword(s):

Antimicrobial Activity ◽

Dilution Method ◽

Mass Spectral ◽

H Nmr ◽

Sar Studies ◽

Mueller Hinton ◽

Morpholine Derivatives ◽

Mueller Hinton Broth ◽

C Nmr

The present study is in the interest of some synthesized novel derivatives containing 4-(1,3-diphenyl-1H-pyrazol-4-yl)-N-(morpholinomethyl)-6-arylpyrimidin-2-amines pooled with different bio-active heterocycles such as pyrazole, pyrimidine and morpholine derivatives. The structures of newly synthesized compounds were elucidated by IR, 1H NMR, 13C NMR and mass spectral data. The synthesized compounds were evaluated for their in vitro antimicrobial activity against different bacterial and fungal strains using Mueller-Hinton Broth dilution method. On the basis of SAR studies, it was observed that the presence of electron withdrawing groups remarkably enhanced the antimicrobial activity of synthesized compounds.

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Synthesis, Characterization and Photophysicochemical Properties of Zinc(Ii) Phthalocyanine With New Benzenesulfonamide Derivative Substituents

10.21203/rs.3.rs-1092717/v1 ◽

2021 ◽

Author(s):

Gülen Atiye Öncül ◽

Ömer Faruk Öztürk ◽

Mehmet Pişkin

Keyword(s):

Elemental Analysis ◽

Mass Spectra ◽

Spectroscopic Methods ◽

H Nmr ◽

Maldi Tof Mass Spectra ◽

New Type ◽

Ft Ir ◽

Photochemical Properties ◽

Photocatalytic Applications ◽

C Nmr

Abstract Novel (E)-4-((5-bromo-2-hydroxy-3-methoxybenzylidene)amino)-N-(pyridin-2-yl)benzenesulfonamide 1, (E)-4-((5-bromo-2-(3,4-dicyanophenoxy)-3-methoxybenzylidene)amino)-N-(pyridin-2-yl)benzene sulfonamide 2 and 2(3),9(10),16(17),23(24)-tetra-[(E)-4-((5-bromo-3-methoxy-2-(λ1-oxidanyl)benzyl idene)amino)-N-(pyridine-2-yl)benzenesulfonamide]phthalocyaninato zinc(II) phthalocyanine 3 were synthesized. Their (1-3) structures were illuminated with spectroscopic methods such as FT-IR, 1H NMR,13C NMR, UV–vis, MALDI-TOF mass spectra and also elemental analysis. The spectroscopic, photophysical and photochemical properties of the zinc(II) phthalocyanine 3 were investigated in dimethyl sulfoxide and its effects on the above mentioned properties were reported as a result of containing new type benzenesulfonamide derivatives as substituents. In addition, its above-mentioned properties were reported by comparing different species with those of their substituted and/or unsubstituted counterparts. The zinc(II) phthalocyanine 3 has photosensitizing abilities suitable and sufficient especially for photocatalytic applications.

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Synthesis and antimicrobial activities of some novel thiazole compounds

Turkish Journal of Biochemistry ◽

10.1515/tjb-2017-0093 ◽

2017 ◽

Vol 43 (3) ◽

pp. 220-227

Author(s):

Gülhan Turan-Zitouni ◽

Betül Kaya Çavuşoğlu ◽

Begüm Nurpelin Sağlık ◽

Ulviye Acar Çevik

Keyword(s):

Antimicrobial Activity ◽

Antimicrobial Activities ◽

Phenacyl Bromide ◽

Antimicrobial Drugs ◽

H Nmr ◽

Chemical Structures ◽

Microdilution Method ◽

Broth Microdilution Method ◽

Ft Ir ◽

Better Than

Abstract Objective: The advent of resistant pathogenic microorganisms against current antimicrobial drugs prompted scientists to investigate novel molecules with new mechanisms. In this paper, some new 2-[2-[4-(ethyl/phenyl)cyclohexylidene]hydrazinyl]-4-(4-substitutedphenyl)thiazole (2a–2o) derivatives were synthesized and studied for their antimicrobial activities. Materials and methods: The title compounds (2a–2o) were obtained via the reaction of 4-(ethyl/phenyl)cyclohexane-1-one with appropriate phenacyl bromide in ethanol at room temperature. The chemical structures of the compounds were elucidated by FT-IR, 1H-NMR, 13C-NMR, HRMS and elemental analysis. Antimicrobial activity of the compounds was measured by using broth microdilution method. Chloramphenicol and ketoconazole were used as reference drugs. Results: Among the synthesized compounds, 2-[2-(4-phenylcyclohexylidene)hydrazinyl]-4-phenylthiazole (2h) and 2-[2-(4-phenylcyclohexylidene)hydrazinyl]-4-(4-chlorophenyl)thiazole (2l) have been found to exhibit potency almost four-fold better than ketoconazole against C. albicans with MIC90 value of 1.95. Conclusion: The current study contributed to the knowledge of the antimicrobial activity of thiazole bearing compounds.

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Synthesis and Pharmacological Evaluation of a Novel Series of Cyclopentenone Derivatives

Journal of Chemical Research ◽

10.3184/174751917x14837116219654 ◽

2017 ◽

Vol 41 (1) ◽

pp. 50-56 ◽

Cited By ~ 1

Author(s):

Fatma A. El-Samahy ◽

Marwa El-Hussieny ◽

Naglaa F. El-Sayed ◽

Elsayed M. Shalaby ◽

Fayez H. Osman

Keyword(s):

Mass Spectra ◽

Secondary Amines ◽

X Ray Diffraction ◽

X Ray ◽

H Nmr ◽

Chemical Structures ◽

Pharmacological Evaluation ◽

New Compounds ◽

C Nmr ◽

Boiling Toluene

A novel series of cyclopent-2-enone derivatives have been synthesised by the reaction of 4-hydroxy-3,4-diphenylcyclopent-2-enone, cyclic secondary amines, phosphorus reagents, hexamethylphosphoramide and Lawesson's reagent in boiling toluene/THF. The chemical structures of new compounds were identified by 1H NMR, 13C NMR, 31P NMR and mass spectra. Furthermore, the structure of one of the synthesised compounds has been confirmed using single crystal X-ray diffraction. The pharmacological evaluation results of antilung and anticolon carcinoma cell line properties for the products are discussed.

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