Synthesis of (E)-1-(2,4-Bis((1-phenyl-1H-1,2,3-triazol-4-yl)methoxy)phenyl)-
3-phenylprop-2-en-1-one Derivatives and their Antimicrobial Activity

A new series of chalcone based bis 1,4-disubstituted 1,2,3-triazole heterocyclic molecules (6a-j) were synthesized via the reaction of 1-(2,4-bis((1-phenyl-1H-1,2,3-triazol-4-yl)methoxy)phenyl)ethanone (6a-e) with substituted benzaldehyde. All the molecules were characterized by IR, 1H and 13C NMR and MS spectra spectral data. Compounds 6a-j were evaluated for their antimicrobial effects using a broth disc diffusion method. The compounds were evaluated for their in vitro antimicrobial potential against Gram-positive (Micrococcus luteus, Methicillin-resistant Staphylococcus aureus, Bacillus subtilis and Bacillus cereus), Gram-negative (Pseudomonas aeruginosa, Klebsiella pneumoniae, Escherichia coli and Proteus vulgaris) bacterial and fungal (Microsporum canis, Microsporum gypseum and Epidermophyton floccosum) strains by comparison of the reference drugs, zentamycin sulphate (antibacterial) and nystatin (antifungal). The screened compounds 6f, 6e, 6c and 6i were found to be the most active against all the tested bacterial and fungal strains.

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In Vitro Antifungal Activity of Hexahydropyrimidine Derivatives against the Causative Agents of Dermatomycosis

The Scientific World JOURNAL ◽

10.1155/2017/1207061 ◽

2017 ◽

Vol 2017 ◽

pp. 1-8 ◽

Cited By ~ 2

Author(s):

Francislene J. Martins ◽

César A. Caneschi ◽

Mônica P. Senra ◽

Gustavo S. G. Carvalho ◽

Adilson D. da Silva ◽

...

Keyword(s):

Antifungal Activity ◽

Morphological Changes ◽

Trichophyton Mentagrophytes ◽

Microsporum Canis ◽

Microsporum Gypseum ◽

Scanning Electron Micrographs ◽

Epidermophyton Floccosum ◽

Synthetic Drugs ◽

Causative Agents

Nitrogenated heterocyclic compounds are present in both natural and synthetic drugs, and hexahydropyrimidine derivatives may prove to be efficient in treating dermatomycosis causing fungi. This study evaluated the antifungal activity of four hexahydropyrimidine derivatives against the dermatomycosis causing fungi. These derivatives were synthesized, characterized, and assessed in terms of their activity against Trichophyton mentagrophytes, Microsporum canis, Microsporum gypseum, Trichophyton rubrum, Fusarium oxysporum, and Epidermophyton floccosum between concentrations 7.8 and 1,000 μg mL−1. Scanning electron micrographs were assessed for the active derivatives and reference drugs, and these micrographs revealed that new agents cause morphological changes in fungi. The derivatives HHP1, HHP3, and HHP4 revealed poor activity against the four fungal strains (MICs range 500–1000 μg mL−1). Compound HHP3 was found to be the best potential antifungal agent among those tested and was the most effective among all the active derivatives that caused morphological changes in the susceptible strains.

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Antifungal Activity of Eugenia umbelliflora against Dermatophytes

Natural Product Communications ◽

10.1177/1934578x0900400904 ◽

2009 ◽

Vol 4 (9) ◽

pp. 1934578X0900400 ◽

Cited By ~ 3

Author(s):

Karina E. Machado ◽

Valdir Cechinel Filho ◽

Rosana C. B. Cruz ◽

Christiane Meyre-Silva ◽

Alexandre Bella Cruz

Keyword(s):

Antifungal Activity ◽

Betulinic Acid ◽

Fungal Pathogens ◽

Trichophyton Rubrum ◽

Trichophyton Mentagrophytes ◽

Microsporum Canis ◽

Microsporum Gypseum ◽

Epidermophyton Floccosum ◽

Agar Dilution

Antifungal activities of Eugenia umbelliflora Berg. (Myrtaceae) were tested in vitro against a panel of standard and clinical isolates of human fungal pathogens (dermatophytes and opportunistic saprobes). Methanol extracts of leaves and fruits of E. umbelliflora were separately prepared and partitioned, to yield dichloromethane (DCM), ethyl acetate (EtOAc) and aqueous fractions (Aq). Three compounds (1-3) were obtained from the DCM extract using chromatographic procedures. Antifungal assays were performed using agar dilution techniques. Both extracts (fruits and leaves), their DCM and EtOAc fractions, and compound 2 (betulin and betulinic acid) presented selective antifungal activity against dermatophytes (Epidermophyton floccosum, Microsporum canis, Microsporum gypseum, Trichophyton rubrum, Trichophyton mentagrophytes), with MIC values between 200 and 1000 μg/mL, and interestingly, inhibited 4/5 species with MIC values of ≤500 ≤g/mL. The aqueous fractions of fruits and leaves, and compounds 1 (α, β amyrin) and 3 (taraxerol) were inactive up to the maximum concentrations tested (1000 μg/mL).

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ANTIFUNGAL ACTIVITY OF PIMENTA DIOICA (L.) MERRIL AN AROMATIC MEDICINAL TREE

International Journal of Pharmacy and Pharmaceutical Sciences ◽

10.22159/ijpps.2016v8i10.9924 ◽

2016 ◽

Vol 8 (10) ◽

pp. 92 ◽

Cited By ~ 2

Author(s):

Akhilesh Bhat ◽

Raveesha K. A.

Keyword(s):

Antifungal Activity ◽

Petroleum Ether ◽

Petroleum Ether Extract ◽

Diffusion Method ◽

Phytochemical Analysis ◽

Microsporum Canis ◽

Ether Extract ◽

Disc Diffusion Method ◽

Rf Values ◽

Pimenta Dioica

Objective: To assess the antifungal activities of the extracts of leaves of Pimenta dioica against human pathogenic fungi and identify the class of phytochemical responsible for the biological activity.Methods: The shade dried, and powdered leaves of Pimenta dioica were subjected to polarity based solvent extraction by soaking. The extracts were dried in a rotary flash evaporator and subjected to antifungal activity assay against Candida albicans, Microsporum canis and M. gypseum, by disc diffusion method. Antifungal active petroleum ether extract was subjected to phytochemical analysis to identify the active compound. The extract was then subjected to Thin Layer Chromatography (TLC) and Bioautography, by agar overlay method. The fractions were collected by Preparative TLC method and subjected to antifungal activity assay by disc diffusion method. Further, the Libermann-Burchard test was conducted to detect the broad group of compounds responsible for the bioactivity.Results: Among the five extracts viz. petroleum ether, chloroform, ethyl acetate, methanol and aqueous, the petroleum ether extract showed significant antifungal activity against Microsporum canis (50 mm), Microsporum gypseum (60 mm) and Candida albicans (23 mm). Terpenoids, tannins and flavonoids were found to be the chief constituents of the petroleum ether extract. The TLC of the extract revealed 7 spots with the Rf values 0.37, 0.42, 0.45, 0.52, 0.59, 0.76, 0.96 with the solvent system of hexane and acetone (1:0.5). The bioautography assay revealed inhibitory activity in the spots at Rf values 0.52 and 0.59. These fractions obtained by preparative TLC also confirmed the same. The phytochemical analysis of the fractions on the TLC plate suggests that the compound is triterpene or steroid.Conclusion: The antifungal activity of Pimenta dioica and the bioactive phytochemical has been reported in the present study. Preliminary phytochemical analysis has indicated that the compounds are triterpenes or steroids. The results indicate that the active compounds are potential lead molecules for new antifungal drugs in the management of infectious fungi.

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Essential Oil from Leaves of Lantana canescens and L. lopez-palacii Grown in Colombia

Natural Product Communications ◽

10.1177/1934578x1100600223 ◽

2011 ◽

Vol 6 (2) ◽

pp. 1934578X1100600

Author(s):

Andrés F. Peralta-Bohórquez ◽

Clara Quijano-Célis ◽

Mauricio Gaviria ◽

Consuelo Vanegas-López ◽

Jorge A. Pino

Keyword(s):

Essential Oil ◽

Volatile Compounds ◽

Diffusion Method ◽

Disc Diffusion ◽

Enterobacter Sakazakii ◽

Bacterial Strains ◽

Disc Diffusion Method ◽

Germacrene D ◽

In Vitro Antibacterial Activity

The chemical composition of the volatile compounds from the leaves of Lantana canescens Kunth (Verbenaceae) and L. lopez-palacii Moldenke grown in Colombia were analyzed by GC and GC/MS. One hundred and thirty-nine volatile compounds were identified in L. canescens, of which the major ones were β-caryophyllene (13.5%), germacrene D (10.3%) and 1-octen-3-ol (8.4%). In the oil obtained from L. lopez-palacii, eighty-three compounds were identified, of which the most prominent were 1-octen-3-ol (24.4%) and β-caryophyllene (15.2%). The in vitro antibacterial activity of the L. lopez-palacii essential oil was studied against three bacterial strains using the disc diffusion method. No antimicrobial activity was found against Escherichia coli, Enterobacter sakazakii and Listeria monocytogenes.

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In vitro sensitivity of Hungarian Actinobaculum suis strains to selected antimicrobials

Acta Veterinaria Hungarica ◽

10.1556/avet.51.2003.1.5 ◽

2003 ◽

Vol 51 (1) ◽

pp. 53-59 ◽

Cited By ~ 4

Author(s):

I. Biksi ◽

Andrea Major ◽

L. Fodor ◽

Keyword(s):

Type Strain ◽

Diffusion Method ◽

Resistance Pattern ◽

Disc Diffusion ◽

Disc Diffusion Method ◽

Antimicrobial Sensitivity ◽

Variable Sensitivity ◽

Agar Dilution ◽

Almost All

In vitro antimicrobial sensitivity of 12 Hungarian isolates and the type strain ATCC 33144 of Actinobaculum suis to different antimicrobial compounds was determined both by the agar dilution and by the disc diffusion method. By agar dilution, MIC50 values in the range of 0.05-3.125µg/ml were determined for penicillin, ampicillin, ceftiofur, doxycycline, tylosin, pleuromutilins, chloramphenicol, florfenicol, enrofloxacin and lincomycin. The MIC50 value of oxytetracycline and spectinomycin was 6.25 and 12.5µg/ml, respectively. For ofloxacin, flumequine, neomycin, streptomycin, gentamicin, nalidixic acid, nitrofurantoin and sulphamethoxazole + trimethoprim MIC50 values were in the range of 25-100µg/ml. With the disc diffusion method, all strains were sensitive to penicillin, cephalosporins examined, chloramphenicol and florfenicol, tetracyclines examined, pleuromutilins, lincomycin and tylosin. Variable sensitivity was observed for fluoroquinolones (flumequine, enrofloxacin, ofloxacin), most of the strains were susceptible to marbofloxacin. Almost all strains were resistant to aminoglycosides but most of them were sensitive to spectinomycin. A strong correlation was determined for disc diffusion and MIC results (Spearman's rho 0.789, p<0001). MIC values of the type strain and MIC50 values of other tested strains did not differ significantly. Few strains showed a partially distinct resistance pattern for erythromycin, lincomycin and ampicillin in both methods.

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Synthesis, Spectroscopic, and Antimicrobial Study of Binary and Ternary Ruthenium(III) Complexes of Ofloxacin Drug and Amino Acids as Secondary Ligands

Crystals ◽

10.3390/cryst10030225 ◽

2020 ◽

Vol 10 (3) ◽

pp. 225

Author(s):

Ahmed M. Naglah ◽

Mohamed A. Al-Omar ◽

Abdulrahman A. Almehizia ◽

Ahmad J. Obaidullah ◽

Mashooq A. Bhat ◽

...

Keyword(s):

Electron Microscopy ◽

Amino Acids ◽

Analysis Data ◽

Antimicrobial Activities ◽

Diffusion Method ◽

Disc Diffusion Method ◽

Element Analysis ◽

X Ray ◽

Paper Disc

This article aimed to synthesis, spectroscopic, physicochemical characterizations, and catalytic studies on some ofloxacin (OFL) complexes with ruthenium(III) [Ru(III)] metal ions. The Ru(III)-OFL complex, [Ru(OFL)2(Cl)2]Cl and two mixed-ligand complexes, [Ru(OFL)(AA)(H2O)2]Cl2 derived from OFL as the primary ligand and amino acids [AA; either glycine (Gly) or alanine (Ala)] as the secondary ligands, were synthesized and characterized using microanalytical, spectroscopic, and physical techniques including element composition, molar conductivity, infrared, electronic spectra, thermal, X-ray powder diffraction (XRD), Energy dispersive X-ray spectroscopy (EDX), Scanning electron microscopy (SEM), and Transmittance electron microscopy (TEM) analyses. The element analysis data describe the formation of 1:2 [Ru(III):OFL] and 1:1:1 [Ru(III):OFL:AA] complexes. The octahedral geometry of the complexes was confirmed by their magnetic moment and diffused reflectance. Fourier Transform Infrared spectroscopic (FTIR) measurements suggested that the ligands chelated with Ru(III) ions through the nitrogen atoms of the piperazine ring. In vitro antibacterial efficiency of the OFL compounds was evaluated by paper disc diffusion method. Significant antimicrobial activities were observed for some compounds of the series.

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In VitroAntifungal Activity of Naftifine Hydrochloride against Dermatophytes

Antimicrobial Agents and Chemotherapy ◽

10.1128/aac.01084-13 ◽

2013 ◽

Vol 57 (9) ◽

pp. 4369-4372 ◽

Cited By ~ 23

Author(s):

M. Ghannoum ◽

N. Isham ◽

A. Verma ◽

S. Plaum ◽

A. Fleischer ◽

...

Keyword(s):

Developed Countries ◽

Microsporum Canis ◽

Test Panel ◽

Resistance Development ◽

Epidermophyton Floccosum ◽

Content Type ◽

Development Of Resistance ◽

Time Kill ◽

Dose Dependent

ABSTRACTThe incidence of superficial dermatophytoses is high in developed countries, and there remains a need for effective topical antifungals. In this study, we evaluated thein vitroantifungal activity of naftifine hydrochloride, the active ingredient in naftifine hydrochloride cream and gel 1% and 2%, against dermatophytes. The MICs and minimum fungicidal concentrations (MFCs) of naftifine hydrochloride against 350 clinical strains, includingTrichophyton rubrum,T. mentagrophytes,T. tonsurans,Epidermophyton floccosum, andMicrosporum canis, were determined using the CLSI methodology. Subsets from this test panel were subsequently tested in a time-kill assay at 0.125×, 0.25×, 0.5×, and 1× the MFC for each isolate. CFU counts were performed over a period of 48 h of incubation. Additionally, in order to determine the potential for resistance development, six strains were subjected to 15 serial passages in concentrations higher than the MIC for each strain. MICs were determined following each passage. The MIC range against the dermatophyte isolates tested was 0.015 to 1.0 μg/ml, with naftifine hydrochloride being fungicidal against 85% of theTrichophytonspecies. The time-kill assay showed dose-dependent activity, with the greatest reduction in the numbers of CFU corresponding to the highest drug concentration. There was no increase in MIC for any strains following repeated exposure to naftifine hydrochloride. Naftifine hydrochloride demonstrated potent activity against all dermatophytes tested, and none of the isolates within this test panel demonstrated the potential for the development of resistance. Thus, future clinical studies of naftifine hydrochloride against dermatophytes may be warranted for the treatment of superficial dermatophytoses.

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Synthesis and in vitro antibacterial activity of Cephradine Benzoate

Bangladesh Journal of Medical Science ◽

10.3329/bjms.v10i3.8356 ◽

1970 ◽

Vol 10 (3) ◽

pp. 148-151

Author(s):

M Ahmad ◽

M Rahman ◽

P Kumar Paul

Keyword(s):

Antibacterial Activity ◽

Salmonella Typhi ◽

Shigella Dysenteriae ◽

Diffusion Method ◽

Disc Diffusion ◽

Disc Diffusion Method ◽

Nmr Studies ◽

Shigella Boydii ◽

Group B

Aims & Methods: The present study was undertaken to compare the antibacterial activity of a cephradine derivative with that of the parent antibiotic cephradine. Cephradine was converted to its benzoyl derivative by Schotten-Baumann method for the first time. Disc diffusion method was employed to find out the antibacterial activity against EPEC, ETEC, E. Agg, Salmonella typhi, Salmonella group B, Shigella boydii, Shigella dysenteriae 1, Shigella dysenteriae 2, Shigella flexinariae and Shigella sonnei. Melting point, TLC, HPLC, UV, FTIR and 1H NMR studies were carried out to check the purity and confirm that the derivative was cephradine benzoate. Results: The benzoyl derivative showed promising activity against tested bacteria. The results obtained from the study demonstrate that the benzoyl derivative could be a potential antibacterial agent. Key words: Cephradine benzoate, antibacterial activity, disc diffusion method. DOI: http://dx.doi.org/ 10.3329/bjms.v10i3.8356 BJMS 2011; 10(3): 148-151

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Studies of Antimicrobial Activity of 2',4',5'- and 2',3',4'-Trimethoxy Flavanones

Journal of Scientific Research ◽

10.3329/jsr.v8i2.26622 ◽

2016 ◽

Vol 8 (2) ◽

pp. 209-216

Author(s):

A. Rahim ◽

R. Ali ◽

A. Islam

Keyword(s):

Pathogenic Bacteria ◽

Sclerotium Rolfsii ◽

Antibacterial Activities ◽

Diffusion Method ◽

Disc Diffusion ◽

Disc Diffusion Method ◽

Filter Paper Disc ◽

Antibacterial And Antifungal ◽

Paper Disc

2',4',5'- and 2',3',4'-trimethoxy flavanones have been synthesized starting with 2-hydroxyacetophone and substituted aldehyde. Antibacterial activities of the flavanones have been tested along with their corresponding chalcones against two human pathogenic bacteria (Streptococcus-b-haemolyticus and Klebsiella sp. (G-)). Antifungal activities of the flavanones have also been investigated against two plants pathogenic mold fungi (Rhizactonia solani Sclerotium rolfsii). The structures of the synthesized compounds have been characterized with the help of UV, IR and 1H NMR and 13C-NMR spectra. The antibacterial and antifungal screening were performed in vitro by the filter paper disc diffusion method and poisoned food technique. The flavanones showed antibacterial activity while no activity was observed to their corresponding chalcones against the tested bacteria. On the other hand, chalcones and their corresponding flavanones both showed fungicidal activities.

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Efek Antimikroba Ekstrak Air Daun Mengkudu (Morinda citrifolia L.) terhadap Bakteri Shigella dysenteriae Secara In Vitro

Jurnal Integrasi Kesehatan & Sains ◽

10.29313/jiks.v3i1.7452 ◽

2021 ◽

Vol 3 (1) ◽

pp. 14-18

Author(s):

Qyana Al Farisi ◽

Yuke Andriane ◽

Miranti Kania Dewi

Keyword(s):

Water Extract ◽

Antimicrobial Effect ◽

Negative Control ◽

Shigella Dysenteriae ◽

Morinda Citrifolia ◽

High Price ◽

Diffusion Method ◽

Disc Diffusion ◽

Disc Diffusion Method

Kematian akibat infeksi Shigella, terutama Shigella dysenteriae dapat mencapai lebih dari 10% terutama pada anak dan lanjut usia pada kondisi tanpa pemberian terapi yang efektif. Siprofloksasin merupakan lini pertama untuk pengobatan infeksi Shigella, akan tetapi obat ini memiliki beberapa kekurangan di antaranya harga yang mahal dan resistensi. Daun mengkudu merupakan tanaman tradisional yang diduga memiliki efek antimikro dan diharapkan dapat menjadi alternatif terapi antibiotik bagi Shigella dysenteriae yang saat ini sudah banyak mengalami resistensi. Tujuan penelitian ini adalah mengetahui efek antimikro ekstrak air daun mengkudu (Morinda citrifolia L.) terhadap bakteri Shigella dysenteriae. Penelitian ini bersifat eksperimental laboratorium murni. Zona hambat ditentukan melalui metode difusi cakram. Objek penelitian yang digunakan adalah Shigella dysenteriae ATCC nomor 13313. Sampel uji berupa ekstrak air daun mengkudu konsentrasi 100%, kontrol positif (siprofloksasin) dan kontrol negatif (aquadest) dengan 9 kali pengulangan. Hasil uji antimikro dengan metode difusi cakram menunjukkan tidak terbentuk zona hambat pada ekstrak air daun mengkudu konsentrasi 100%. Hal tersebut menunjukkan ekstrak air daun mengkudu konsentrasi 100% tidak memiliki efek antimikro terhadap bakteri Shigella dysenteriae. Kadar flavonoid, tanin, dan alkaloid yang terdapat dalam ekstrak air daun mengkudu konsentrasi 100% pada penelitian ini kemungkinan belum cukup untuk menghasilkan efek yang diharapkan. Antimicrobial Effect of Water Extract of Noni (Morinda citrifolia L.) Leaves against Shigella dysenteriae In VitroDeath due to infection with Shigella, especially Shigella dysenteriae, can reach more than 10%, especially in children and the elderly in conditions without effective therapy. Ciprofloxacin is the first line for the treatment of Shigella infection, however this drug has several disadvantages including high price and resistance. Noni leaf is a traditional plant that is thought to have antimicrobial effects and is expected to be an alternative antibiotic therapy for Shigella dysenteriae which is currently experiencing a lot of resistance. The purpose of this study was to determine the antimicrobial effect of the water extract of noni leaves (Morinda citrifolia L.) on Shigella dysenteriae bacteria. This research is a pure laboratory experimental study. The zone of inhibition is determined by the disc diffusion method. The research object used was Shigella dysenteriae ATCC number 13313. The test sample was a water extract of noni leaves with a concentration of 100%, positive control (ciprofloxacin) and negative control (aquadest) with 9 repetitions. The results of the antimicrobial test using the disc diffusion method showed no inhibition zone was formed in the water extract of noni leaves with a concentration of 100%. This shows that a water extract of noni leaves with a concentration of 100% did not have an antimicrobial effect against the Shigella dysenteriae bacteria. The levels of flavonoids, tannins, and alkaloids contained in the water extract of noni leaves with a concentration of 100% in this study may not be sufficient to produce the expected effect.

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