scholarly journals Design, Synthesis, and Antimicrobial Evaluation of Novel Pyrazoles and Pyrazolyl 1,3,4-Thiadiazine Derivatives

Molecules ◽  
2018 ◽  
Vol 23 (9) ◽  
pp. 2092 ◽  
Author(s):  
Ibrahim Radini

A novel series of pyrazolyl 1,3,4-thiadiazines 5a–c, 8a–c, 12, 15a–c, 17a–c, and 20 was prepared from the reaction of pyrazole-1-carbothiohydrazide 1a,b with 2-oxo-N′-arylpropanehydrazonoyl chloride, 2-chloro-2-(2-arylhydrazono)acetate, and 3-bromoacetylcoumarin. Moreover, the regioselective reaction of 5-pyrazolone-1-carbothiohydrazide 1a with 4-substituted diazonium salts and 4-(dimethylamino)benzaldehyde gave the corresponding hydrazones 21a–c and 22. The newly prepared compounds were characterized by spectroscopy and elemental analysis. Many new synthesized compounds showed considerable antimicrobial activity against tested microorganisms. Hydrazones 21a–c and 22 showed remarkable antibacterial and antifungal activities. 4-(2-(p-tolyl)hydrazineylidene)-pyrazole-1-carbothiohydrazide 21a displayed the highest antibacterial and antifungal activities with minimum inhibitory concentration (MIC) values lower than standard drugs chloramphenicol and clotrimazole, in the range of 62.5–125 and 2.9–7.8 µg/mL, respectively.

1970 ◽  
Vol 24 (1) ◽  
pp. 73-75 ◽  
Author(s):  
M Shafiqur Rahman ◽  
M Nural Anwar

Ethanolic extract of Plumbago zeylanica root was investigated for its antimicrobial activities against 11 human pathogenic bacteria and 6 phytopathogenic fungi using disc diffusion method and poisoned food technique respectively. The extract exhibited good antibacterial and antifungal activities against the test organisms. Among the test bacteria, Vibrio cholerae was found to be the most sensitive to the extract showing the highest diameter of zone of inhibition and lowest minimum inhibitory concentration (MIC) value (200 μg/ml). The extract was also very effective against Escherichia coli and Pseudomonas aeruginosa showing MIC value of 250 μg/ml. Among the phytopathogenic fungi tested, Curvularia lunata exhibited the highest sensitivity to the extract with an MIC value of 150 μg/ml, which was followed next by Colletotrichum corchori and Fusarium equiseti (MIC value 250 μg/ml). The root extract from P. zeylanica seems promising since it showed both antibacterial and antifungal activities.  Keywords: Antimicrobial activity, Plumbago zeylanica, Ethanolic extract, Minimum inhibitory concentration (MIC)DOI: http://dx.doi.org/10.3329/bjm.v24i1.1244  Bangladesh J Microbiol, Volume 24, Number 1, June 2007, pp73-75


2021 ◽  
Vol 25 (1) ◽  
pp. 113-117
Author(s):  
T.T. Alawode ◽  
L. Lajide ◽  
B.J. Owolabi ◽  
M.T. Olaleye

This study investigates the bulb extracts of Crinum jagus for antimicrobial activities. The bulb samples were dried, ground and subjected to successive extraction using hexane, ethylacetate and methanol. The extracts were screened for activity against Staphylococcus aureus, Escherichia coli, Bacillus subtilis, Pseudomonas aeruginosa, Salmonella typhi, Klebisidlae pneumonae, Candida albicans, Aspergillus niger, Penicillium notatum and Rhizopus stolonifer at concentrations between 6.25 and 200 mg/ml. Antimicrobial assays werecarried out using agar diffusion method. The Minimum Inhibitory Concentration (MIC) of the extracts was determined. The percentage yields obtained for the hexane, ethylacetate and methanol extracts of the bulbs are 0.28 %, 0.44% and 24.68 % respectively. Results showed that the methanolic extract had better antibacterial and antifungal activities than the other extracts. The methanol extract showed the highest antibacterial activity against S. aureus with a zone of inhibition of 28 mm at 200 mg/ml. Also, the methanol extract showed the highest antifungal activities against C. albicans, A. niger and P. notatum with a zone of inhibition of 20 mm at 200 mg/ml. The hexane and ethylacetate extracts had no activity against the microorganisms at 6.25 mg/ml.The methanol extract had the lowest Minimum Inhibitory Concentration (MIC) of 2.50 mg/ml against S. aureus, E. coli, B. subtilis, P. aeruginosa and S. typhi. The methanol extract could be a source of potent antimicrobial compounds. Keywords: Antibacterial, Antifungal, Crinum jagus, Agar diffusion, MIC


2017 ◽  
Vol 9 (3) ◽  
pp. 297-306 ◽  
Author(s):  
R. Ali ◽  
A. Rahim ◽  
A. Islam

7-Hydroxy-3',4'-methylenedioxy- and 7-benzyloxy-3',4'-methylenedioxy flavanones have been synthesized starting from 2,4-dihydroxyacetophenone. Subsequently biocidal activities of the flavanones have been investigated along with their corresponding chalcones against some bacterial and fungal strains. 2'-Hydroxy-4'-benzyloxy-3,4-methylenedioxy chalcone (5) and its corresponding flavanone (7) showed good antibacterial and antifungal activities against some selected bacterial and fungal strains. On the other hand, 2',4'-dihydroxy-3,4-methylenedioxy chalcone (4) showed no antibacterial and antifungal activities while its corresponding flavanone (6) showed a little antibacterial activity only at higher concentration but did not show antifungal activity. The synthesized chalcones and flavanones have been characterized using UV-Vis, IR and 1H NMRspectral data together with elemental analysis.


2011 ◽  
Vol 61 (2) ◽  
pp. 171-185 ◽  
Author(s):  
Mosaad Mohamed ◽  
Samir Awad ◽  
Naglaa Ahmed

Synthesis and antimicrobial evaluation of some 6-aryl-5-cyano-2-thiouracil derivativesA series of 6-aryl-5-cyano-2-thiouracil derivatives (1a-d) was synthesized by the reaction of ethyl cyanoacetate with thiourea and aldehydes. These products were used as intermediate compounds for the synthesis of a number of thiouracil derivatives (2a-dto10a-d). All compounds were screened for antibacterial and antifungal activities. Some of the prepared compounds, 6-(4-fluorophenyl)-4-oxo-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide (2a), 4-oxo-2-thioxo-6-(3,4,5-trimethoxyphenyl)-1,2,3,4-tetrahydropyrimidine-5-carboxamide (2d), 6-(4-fluorophenyl)-4-hydrazino-2-thioxo-1,2-dihydropyrimidine-5-cabonitrile (7a) and 4-hydrazino-2-thioxo-6-(3,4,5-trimethoxyphenyl)-1,2-dihydropyrimidine-5-carbonitrile (7d) revealed promising antimicrobial activity.


2010 ◽  
Vol 7 (4) ◽  
pp. 1435-1439 ◽  
Author(s):  
Gopal Krishna Rao ◽  
R. B. Kotnal ◽  
P. N. Sanjay Pai

A series of quinoxaline derivatives was prepared and evaluated for antitubercular, antibacterial and antifungal activities. The title compounds were prepared by condensation of substituted aromatic aldehydes and substituted acetophenones with 2-(3-methyl-2-oxoquinoxalin-1(2H)-yl) acetohydrazide. Structures of all these compounds were confirmed by their spectral studies. Among synthesized compounds (4r, 4t, 4u, 4wand4x) have shown good anti tubercular activity (25 µg mL-1) when compared to reference drugs pyrazinamide (10 µg mL-1) and streptomycin (7.5 µg mL-1). In this study, few derivatives showed broad spectrum of antimicrobial activity at low concentration. The MICs (Minimum inhibitory concentration) of some compounds are 2-4 µg mL-1.


2008 ◽  
Vol 5 (1) ◽  
pp. 23-33 ◽  
Author(s):  
N. M. Raghavendra ◽  
P. P. Thampi ◽  
P. M. Gurubasavarajaswamy

Several substituted-quinazolin-3(4H)-ones were synthesized by condensation of 2-chloro-N-(4-oxo-substituted-quinazolin-3(4H)-yl)-acetamides with various substituted piperazines through single step reaction. Elemental analysis, IR,1HNMR and mass spectral data confirmed the structure of the newly synthesized compounds. Synthesized quinazolin-4-one derivatives were investigated for their antibacterial and antifungal activities.


2014 ◽  
Vol 20 ◽  
pp. 153-160
Author(s):  
AH Molla ◽  
MG Zakaria ◽  
MTH Molla ◽  
MT Alam ◽  
MS Ahsan

Context: Plants have been used in treating human diseases for thousands of years. Medicinal plant drug discovery continues to provide new and important leads against various pharmacological targets including cancer, malaria, HIV/AIDS, Alzheimer's, and pain. Objectives: The chemical investigation, antimicrobial activity and toxicity of the active principles isolated from the plant. Materials and Methods: The rectified spirit extract of the fresh stem of the plant Tinospora cordifolia was fractionated using standard chromatographic techniques to afford several fractions. The fraction TC-1 was purified by crystallization and screened. FTIR, 1H NMR, 13C NMR spectral analyses were performed to characterize the compound. The antibacterial and antifungal activities of TC-1 were observed by “Disc diffusion method” against a number of pathogenic bacteria and fungi. Standard antibiotics “Kanamycin” (30?g/disc) and “Fluconasol” (500 ?g/disc) were used respectively for comparison. The minimum inhibitory concentration (MIC) of the compound TC-1 was carried out by the “Serial Dilution Technique”. The compound also showed significant activity against the brine shrimp nauplii. Results: The compound TC-1 showed promising antibacterial and antifungal activities against all tested organisms.The minimum inhibitory concentration (MIC) of TC-1 against Bacillus megaterium and Salmonella typhi-A was found to be 128?g/ml in nutrient broth medium. The value of medium lethal concentration, LC50 (9.34 ?g/ml) indicated the high toxic effect of the compound TC-1. Conclusion: It may be concluded that the compound TC-1 is an alkaloid having significant activities. DOI: http://dx.doi.org/10.3329/jbs.v20i0.17737 J. bio-sci.  20:  153-160, 2012


2018 ◽  
Vol 10 (4) ◽  
pp. 1
Author(s):  
Helen Oluwatola Omoregie

Nickel(II) complex of 4,4,4-trifluoro-1-(2-Naphthyl)-1,3-butanedione(tfnb) and its 2,2′-bipyridine (bipy), ethylenediamine (en) and 1,10-phenanthroline (phen) adducts were synthesized and characterized by elemental analysis, infrared, electronic spectral, magnetic susceptibility measurements and antimicrobial activities. Three other nickel(II) compounds were synthesized along with these compounds. The bands in the 1651-1513 cm-1 have been assigned as ν(C=O) + ν(C=C). The infrared and electronic spectral measurements are indicative of a probable six-coordinate octahedral geometry for all the nickel(II) complexes and adducts. The antimicrobial activity shows that [Ni(tfnb)2]2H2O complex and its adducts have no antibacterial and antifungal activities.


2016 ◽  
Vol 11 (7) ◽  
pp. 1934578X1601100
Author(s):  
Simona Casiglia ◽  
Maurizio Bruno ◽  
Sergio Rosselli ◽  
Felice Senatore

The chemical composition of the essential oil from flowers of Eringium triquetrum Vahl. collected in Sicily was evaluated by GC and GC-MS. The main components were pulegone (50.6%), piperitenone (30.5%) and menthone (7.0%). Comparison of this oil with other studied oils of Eringium species is discussed. The oil showed good antibacterial and antifungal activities against some microorganisms that infest historical art works.


Molecules ◽  
2018 ◽  
Vol 23 (8) ◽  
pp. 2013 ◽  
Author(s):  
Ricardo Murcia ◽  
Sandra Leal ◽  
Martha Roa ◽  
Edgar Nagles ◽  
Alvaro Muñoz-Castro ◽  
...  

In this work, six complexes (2–7) of Cr(III) and Co(II) transition metals with triazole ligands were synthesized and characterized. In addition, a new ligand, 3,5-bis(1,2,4-triazol-1-ylmethyl)toluene (1), was synthesized and full characterized. The complexes were obtained as air-stable solids and characterized by melting point, electrical conductivity, thermogravimetric analysis, and Raman, infrared and ultraviolet/visible spectroscopy. The analyses and spectral data showed that complexes 3–7 had 1:1 (M:L) stoichiometries and octahedral geometries, while 2 had a 1:2 (M:L) ratio, which was supported by DFT calculations. The complexes and their respective ligands were evaluated against bacterial and fungal strains with clinical relevance. All the complexes showed higher antibacterial and antifungal activities than the free ligands. The complexes were more active against fungi than against bacteria. The activities of the chromium complexes against Candida tropicalis are of great interest, as they showed minimum inhibitory concentration 50 (MIC50) values between 7.8 and 15.6 μg mL−1. Complexes 5 and 6 showed little effect on Vero cells, indicating that they are not cytotoxic. These results can provide an important platform for the design of new compounds with antibacterial and antifungal activities.


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