scholarly journals Synthesis and Antimicrobial Activity of Bis-4,6-sulfonamidated 5,7-Dinitrobenzofuroxans

2014 ◽  
Vol 2014 ◽  
pp. 1-6 ◽  
Author(s):  
Irina V. Galkina ◽  
Elena V. Tudriy ◽  
Yuliya V. Bakhtiyarova ◽  
Luiza M. Usupova ◽  
Marina P. Shulaeva ◽  
...  

A new series of bis-4,6-sulfonamidated 5,7-dinitrbenzofuroxans  7–11had been synthesized and tested for antimicrobial activity. The structures of new sulfanilamide derivatives were characterized by elemental analysis, IR spectroscopy, and mass spectrometry (MALDITOF). The synthesized compounds were tested for theirin vitroantimicrobial activity using the disk diffusion method against Gram-positive bacteriaStaphylococcus aureus; the Gram-negative bacteriaEscherichia coli, Pseudomonas aeruginosa, andProteus mirabilis; the fungal strainAspergillus niger; and the yeast-like pathogenic fungusCandida albicans. Our results indicate that the compounds7–11exhibit potent antimicrobial activity. The stability of the compounds was evaluated by TG and DSC methods.

2020 ◽  
Vol 7 (7) ◽  
pp. 200290 ◽  
Author(s):  
Ricardo Corona-Sánchez ◽  
Alma Sánchez-Eleuterio ◽  
Claudia Negrón-Lomas ◽  
Yarisel Ruiz Almazan ◽  
Leticia Lomas-Romero ◽  
...  

A series of carbohydrate-linked 1,2,3-triazole derivatives were synthesized in good yields from glucofuranose and allofuranose diacetonides using as key step a three-component 1,3-dipolar azide–alkyne cycloaddition catalysed by a Cu–Al mixed oxide. In this multi-component reaction, Cu–Al mixed oxide/sodium ascorbate system serves as a highly reactive, recyclable and efficient heterogeneous catalyst for the regioselective synthesis of 1,4-disubstituted 1,2,3-triazoles. The reported protocol has significant advantages over classical CuI/ N , N -diisopropylethylamine (DIPEA) or CuSO 4 /sodium ascorbate conditions in terms of efficiency and reduced synthetic complexity. In addition, the selective deprotection of synthesized di- O -isopropylidene derivatives was also carried out leading to the corresponding mono- O -isopropylidene products in moderate yields. Some of the synthesized triazole glycoconjugates were tested for their in vitro antimicrobial activity using the disc diffusion method against Gram-positive bacteria ( Staphylococcus aureus and Bacillus subtilis ), Gram-negative bacteria ( Escherichia coli and Pseudomonas aeruginosa ), as well as fungus ( Aspergillus niger ) and yeast ( Candida utilis ). The results revealed that these compounds exhibit moderate to good antimicrobial activity mainly against Gram-negative bacteria.


2021 ◽  
Vol 2 (2) ◽  
Author(s):  
Eti Nurwening Sholikhah ◽  
Maulina Diah ◽  
Mustofa ◽  
Masriani ◽  
Susi Iravati ◽  
...  

Pycnarrhena cauliflora (Miers.) Diels., local name sengkubak, is one of indigenous plants from West Kalimantan that has been used as natural flavor. Pycnorrhena cauliflora is one of species of Menispermaceae family which is rich in bisbenzylisoquinoline alkaloids. This alkaloids are known to have various biological activities including antiprotozoal, antiplasmodial, antifungal and antibacterial activities. This study aimed to investigate antimicrobial activity of  the P. cauliflora (Miers.) Diels. methanolic extracts against gram-positive and gram-negative bacteria. The methanolic extract of P. cauliflora (Miers.) Diels., root, leaf and stem were prepared by maceration. The disk-diffusion method was then used to determine the antimicrobial activity of the extracts against Streptococcus pyogenes, S. mutants, Staphylococcus aureus, S. epidermidis, Salmonella typhi, Shigella flexneri, Pseudomonas aeruginosa and Escherichia coli after 18-24 h incubation at 37 oC. Amoxicillin was used as positive control for gram-positive bacteria and ciprofloxacin was used as gram-negative bacteria. The inhibition zones were then measured in mm. Analysis were conducted in duplicates. The results showed in general the methanolic extracts of P. cauliflora (Miers.) Diels. root (inhibition zone diameter= 10-23 mm) were more active than that leaf (0-15 mm) and stem (0-17 mm) extracts against gram-positive bacteria. The zone inhibition diameter of amoxicillin as positive control was 8-42 mm. In addition, the methanolic extracts of P. cauliflora (Miers.) Diels. root (12-17 mm) were also more active than that leaf (0-12 mm) and stem (0-12 mm) extracts against gram-negative bacteria. The zone inhibition diameter of ciprofloxacin as positive control was 33-36 mm. In conclusion, the methanolic extract of P. caulifloria (Miers.) Diels. root is the most extract active against both gram-positive and gram-negative bacteria. Further study will be focused to isolate active compounds in the methanolic extract of the root.


2012 ◽  
Vol 7 (5) ◽  
pp. 1934578X1200700 ◽  
Author(s):  
Alexis Peña ◽  
Luis Rojas ◽  
Rosa Aparicio ◽  
Libia Alarcón ◽  
José Gregorio Baptista ◽  
...  

The essential oil of the leaves of Espeletia nana Cuatrec, obtained by hydrodistillation, was analyzed by GC-MS, which allowed the identification of 24 components, which made up 99.9% of the oil. The most abundant compounds were α-pinene (38.1%), β-pinene (17.2%), myrcene (15.0%), spathulenol (4.2%), bicyclogermacrene (4.0%), α-zingiberene (4.0%), and γhimachalene (3.7%). Antibacterial activity was tested against Gram-positive and Gram-negative bacteria using the agar disk diffusion method. Activity was observed only against Gram-positive bacteria. MIC values were determined for Staphylococcus aureus ATCC 25923(200 μg/mL) and Enterococcus faecalis ATCC 29212 (600 μg/mL).


2013 ◽  
Vol 11 (1) ◽  
pp. 45-53 ◽  
Author(s):  
Igor Stojanovic ◽  
Niko Radulovic ◽  
Vladimir Cvetkovic ◽  
Tatjana Mitrovic ◽  
Slavisa Stamenkovic

Antimicrobial activity of methanol extracts of four Parmeliaceae lichens (Hypogymnia physodes (L.) Nyl., Evernia prunastri (L.) Ach., Flavoparmelia caperata (L.) Hale and Parmelia sulcata Taylor) against a panel of microbial strains (11 Gram-positive (Enterococus sp., Bacillus subtilllis, Sarcina lutea, Micrococus luteus, Staphylococcus aureus, Clostridium sporogenes) and Gram-negative bacteria (Escherichia coli, Proteus vulgaris, Salmonela enteritidis, Pseudomonas aeruginosa, Klebsiella pneumoniae), the filamentous fungus A. niger and the yeast C. albicans) was assayed using a disk diffusion method (1 mg of the extract per disc; extracts were dissolved in methanol, 25 mg/mL). All tested extracts showed moderate antimicrobial activity. Multivariate statistical treatment (agglomerative hierarchical clustering analysis, AHC) of the obtained results allowed grouping of the samples according to their antimicrobial potential against different strains: antimicrobial profile of H. physodes and E. prunastri extracts were comparable; the similar is true for F. caperata and P. sulcata samples. In addition, based on the similarities/ dissimilarities in their susceptibility toward the tested extracts, two groups of microorganisms could be distinguished: Group I - P. vulgaris, K. pneumoniae (Gram-negative bacteria), A. niger and C. albicans; Group II - E. coli, S. enteritidis, P. aeruginosa (Gram-negative bacteria) and all of the assayed Gram-positive strains.


2021 ◽  
Vol 10 (4) ◽  
pp. 427-434 ◽  
Author(s):  
Turdibek Toshmurodov ◽  
Abdukhakim Ziyaev ◽  
Sobirdjan Sasmakov ◽  
Jaloliddin Abdurakhmanov ◽  
Mavluda Ziyaeva ◽  
...  

Amidoalkylation of secondary heterocyclic amines by N-[5-(alkylsulfanyl)-1,3,4-thiadiazol-2-yl]-2'-chloroacetamide resulted the new compounds 5-10 that contain 1,3,4-thiadiazole-5-thione moiety alongside pyperidine, morpholine, and cytisine fragments. In vitro screening of antimicrobial activity of synthesized compounds showed that N-[5-(amylsulfanyl)-1,3,4-thiadiazol-2-yl]-2'-morpholinacetamide exhibited an appreciable antibacterial activity against gram-negative bacteria of Escherichia coli (inhibition zone diameter of 16 mm) and gram-positive bacteria of Staphylococcus aureus and Bacillus subtilis (10-13 mm).


2011 ◽  
Vol 8 (s1) ◽  
pp. S282-S284 ◽  
Author(s):  
Liliwirianis N ◽  
Wan Zuraida Wan Mohd Zain ◽  
Jamaluddin Kassim ◽  
Shaikh Abdul Karim

Local herbs have many potential that may be active with antimicrobial activity. A screening was conducted with 11 species of herbs collected in UiTM Pahang Forest Reserve.Epipremnumsp.,Zingibersp.Tetracera indica, Tectaria crenata, Piper stylosum, Homalomena propinque, Goniothalamus sp., Elephantopus scaber, Mapania patiolale, Melastomasp.,Stemona tuberosa, Phullagathis rotundifolia, Thotea grandifoliaandSmilaxsp. were extracted with methanol to obtain their crude. The agar diffusion method using blank disc of 6 mm diameter were loaded with 1000 µg/mL of methanol crude and applied to the inoculate plate was used to assess the antimicrobial activity against two gram positive bacteria (Bacillus subtilisandStaphylococcus aeureus) and one gram negative bacteria (Escherichia coli). The results evaluated as the diameter of the inhibition zone of microbial growth, showed that all the extracts were active against gram-positive bacteria and gram-negative bacteria. The extract ofStemona tuberosewas found to be the most active against theE. coliandS. aeureuswhilePiper stylosumactive againstB. subtilis.


Chemotherapy ◽  
2017 ◽  
Vol 62 (3) ◽  
pp. 194-198 ◽  
Author(s):  
Socorro Leyva-Ramos ◽  
Denisse de Loera ◽  
Jaime Cardoso-Ortiz

Background: Fluoroquinolones are widely prescribed synthetic antimicrobial agents. Quinolones act by converting their targets, gyrase and topoisomerase IV, into toxic enzymes that fragment the bacterial chromosome; the irreversible DNA damage eventually causes the killing of bacteria. Thorough knowledge of the structure-activity relationship of quinolones is essential for the development of new drugs with improved activity against resistant strains. Methods: The compounds were screened for their antibacterial activity against 4 representing strains using the Kirby-Bauer disk diffusion method. Minimal inhibitory concentration (MIC) was determined by measuring the diameter of the inhibition zone using concentrations between 250 and 0.004 μg/mL. Results: MIC of derivatives 2, 3, and 4 showed potent antimicrobial activity against gram-positive and gram-negative bacteria. The effective concentrations were 0.860 μg/mL or lower. MIC for compounds 5-11 were between 120 and 515 μg/mL against Escherichia coli and Staphylococcus aureus, and substituted hydrazinoquinolones 7-10 showed poor antibacterial activity against gram-positive and gram-negative bacteria compared with other quinolones. Conclusion: Compounds obtained by modifications on C-7 of norfloxacin with the acetylated piperazinyl, halogen atoms, and substituted hydrazinyl showed good in vitro activity - some even better than the original compound.


2019 ◽  
Vol 35 (2) ◽  
pp. 648-657 ◽  
Author(s):  
Wasim Ahmad ◽  
Ennus T. Tamboli ◽  
Abuzer Ali ◽  
Mohd Amir ◽  
S. M. A. Zaidi ◽  
...  

A Gas Chromatography and Maas Spectroscopy method was developed and validated for determination and identification of α-humulene in a traditional medicinal herb Didymocarpous pedicellatus R. Br. (DP) (Gesneriaceae) and its poly herbal formulation, Safoof-e-pathar phori (SPP) including their essential oil. Hydrodistillation method were used for the isolation of essential oils from the leaves of DP and SPP herbal formulation. The proposed analysis method was found to be linear r2 = 0.999 in a wide concentration range (0.1-1000 µgmL-1), with good precision (RSD < 2.0%). Antimicrobial activity of α-humulene, DP and SPP oil was assessed by using agar well diffusion method against clinically important Gram-positive, Gram-negative bacteria and fungi. α-Humulene was found to be more active in contrast to Gram-negative bacteria while DP oil and SPP oil were exhibited maximum inhibition against fungal strains. Antioxidant activity of α-humulene, DP oil and SPP oil were determined using 2, 2-diphenyl-1-picryl hydrazyl radical (DPPH) 96 well plate method, which showed antioxidant activity in the following order: standard ascorbic acid (DPPH FRS50 = 2.40 µg) > DP oil (DPPH FRS50 = 3.68 µg) > SPP oil (DPPH FRS50 = 12.54 µg) > and α-humulene (DPPH FRS50 = 36.19 µg).


2012 ◽  
Vol 7 (7) ◽  
pp. 1934578X1200700 ◽  
Author(s):  
Rajesh K. Joshi ◽  
Vijaylaxmi Badakar

The essential oil of the flowers of Tridax procumbens L. was obtained by hydro-distillation and analyzed by gas chromatography equipped with a flame ionization detector (GC-FID) and gas chromatography coupled with mass spectrometry (GC/MS). Twenty-six compounds were identified, which comprised 90.6% of the total constituents. The most abundant compound was ( Z)-falcarinol (25.9%), followed by α-selinene (15.3%), limonene (8.3%) and zerumbone (4.3%). Antimicrobial activity was tested against six Gram-positive and eight Gram-negative bacteria, and three fungi. The oil was active against the tested Gram-positive bacteria at a concentration range of 0.14 ± 0.03 - 0.57±0.05 mg/mL, while 0.67 ± 0.12 - 4.58 ± 0.41 mg/mL was effective against the studied Gram-negative bacteria. Remarkable antifungal activity was found against the tested fungi at a concentration range of 0.06 ± 0.008 - 0.10 ± 0.01 mg/mL.


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