scholarly journals Cu–Al mixed oxide-catalysed multi-component synthesis of gluco- and allofuranose-linked 1,2,3-triazole derivatives

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.

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.


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.


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.


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.


2018 ◽  
Vol 42 (1) ◽  
pp. 119-123
Author(s):  
Charlie Longtine ◽  
Adrian Tejedor

Medicinal plants are important components of traditional medicine and sources of novel antimicrobial compounds against drug resistance pathogen strains. This study tested the antimicrobial activity of ethanolic and aqueous extracts of medicinally used Neotropical tree ferns Cyathea microdonta and Alsophila cuspidata against gram positive bacteria and gram negative bacteria using the Kirby-Bauer disc diffusion method. Highest antimicrobial activity was observed in ethanolic extracts, and extracts were more active against gram positive bacteria than gram negative bacteria. No difference was observed in antimicrobial activity between species or between extracts made from the leaves, stipe, or caudex. These results suggest that the traditional use of tree fern mucilage as a topical agent for cuts and leishmaniasis lesions may reduce risk of secondary infection with skin bacteria such as Staphylococcus aureus, and that Neotropical Cyatheaceae are a potential source of novel antimicrobial compounds.


Author(s):  
Halah A. Sahib ◽  
Mohammed H. Mohammed

A A new series of bases of Schiff (H2-H4) derived from phthalic anhydrideweresynthesized. These Schiff bases were prepared by the reaction of different amines (tyrosine methyl ester, phenylalanine methyl ester, and isoniazid) with the phthalimide derived aldehyde with the aid of glacial acetic acid or triethylamine ascatalysts. All the synthesized compounds were characterized by (FT-IR and 1HNMR) analyses and were in vitro evaluated for their antimicrobial activity against six various kinds of microorganisms. All the synthesized compounds had been screened for their antimicrobial activity against two Gram-positive bacteria “Staph. Aureus, and Bacillus subtilis”, two Gram-negative bacteria “Escherichia coli, and Klebsiella pneumoniae”, and two fungi species “Candida tropicalis and Candida albicans” using concentrations of 62.5, 125 and 250 µg\mLof derivative in dimethyl sulfoxide(DMSO). All the synthesized compounds showed no activity at all against Gram-positive bacteria, for Gram-negative bacteria and fungi they showed moderate or no activity except compound H1revealedhigh antifungal activityagainstCandida tropicalisat concentrations 125 and 250 µg\ mL. Keywords: Schiff base, phthalic anhydride, antimicrobial.  


2007 ◽  
Vol 53 (1) ◽  
pp. 75-81 ◽  
Author(s):  
M Shahid ◽  
Anwar Shahzad ◽  
Abida Malik ◽  
M Anis

Leaves, stem, and flowers of Saraca asoca, an endangered medicinal plant in India, and young explants cultivated on Murashige & Skoog's medium containing 6-benzylaminopurine were analyzed for antibacterial potential. Alcoholic and aqueous extracts from parent explants and their in vitro raised calli were tested by an agar well diffusion method. Minimal inhibitory concentrations (MICs) of the extracts were determined by broth microdilution method. Aqueous extracts showed antibacterial activity against limited bacterial species, whereas alcoholic extracts were active against a wider range of bacteria. Although the alcoholic extracts of all the explants and calli showed antibacterial activity, the extracts derived from flowers and their calli showed better results. Extracts derived from calli showed comparable results to the extracts from explants. Overall, the MICs of the extracts ranged from 0.039 to 1.25 mg/mL. MICs against Gram-positive bacteria ranged from 0.078 to 1.25 mg/mL, whereas they ranged between 0.039 and 0.625 mg/mL against Gram-negative bacteria. A MIC distribution plot showed that Gram-negative bacteria were more susceptible to the extracts than Gram-positive bacteria. It is concluded that extracts of S. asoca contain antibacterial agent, and as the calli gave good results, in vitro cultivation of the explants may be used to obtain antibacterial compounds. This is the first report on antibacterial activity of S. asoca, especially through in vitro raised calli.Key words: Saraca asoca, antibacterial activity, in vitro, callus, minimal inhibitory concentration.


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