scholarly journals Amidoalkylation of heterocyclic amines by N-[5-(alkylsulfanyl)-1,3,4-thiadiazol-2-yl]- 2'-chloroacetamide and antimicrobial activity of derivatives

2021 ◽  
Vol 10 (4) ◽  
pp. 427-434 ◽  
Author(s):  
Turdibek Toshmurodov ◽  
Abdukhakim Ziyaev ◽  
Sobirdjan Sasmakov ◽  
Jaloliddin Abdurakhmanov ◽  
Mavluda Ziyaeva ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Inhibition Zone ◽  
Heterocyclic Amines ◽  
Gram Negative Bacteria ◽  
In Vitro Screening ◽  
Gram Negative ◽  
Inhibition Zone Diameter ◽  
Gram Positive Bacteria ◽  
New Compounds

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).

scholarly journals Antimicrobial Activity of Plant Extracts againstBacillus Subtilis,Staphylococcus Aureusand Escherichia Coli

2011 ◽  
Vol 8 (s1) ◽  
pp. S282-S284 ◽  
Author(s):  
Liliwirianis N ◽  
Wan Zuraida Wan Mohd Zain ◽  
Jamaluddin Kassim ◽  
Shaikh Abdul Karim
Keyword(s):  
Escherichia Coli ◽  
Antimicrobial Activity ◽  
Inhibition Zone ◽  
Diffusion Method ◽  
Gram Negative Bacteria ◽  
Gram Positive ◽  
Gram Negative ◽  
Gram Positive Bacteria ◽  
Stemona Tuberosa ◽  
Elephantopus Scaber

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.

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 ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Mixed Oxide ◽  
Sodium Ascorbate ◽  
Diffusion Method ◽  
Gram Negative Bacteria ◽  
Gram Negative ◽  
Triazole Derivatives ◽  
Gram Positive Bacteria ◽  
Isopropylidene Derivatives

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.

scholarly journals Chemical Composition and in vitro Antimicrobial Activity of the Essential Oil of the Flowers of Tridax procumbens

2012 ◽  
Vol 7 (7) ◽  
pp. 1934578X1200700 ◽  
Author(s):  
Rajesh K. Joshi ◽  
Vijaylaxmi Badakar
Keyword(s):  
Gas Chromatography ◽  
Antimicrobial Activity ◽  
Essential Oil ◽  
Gram Negative Bacteria ◽  
Gram Positive ◽  
Gram Negative ◽  
Gram Positive Bacteria ◽  
Flame Ionization ◽  
Tridax Procumbens

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.

scholarly journals Synthesis and Preliminary Biological Activity Evaluation of New N- Substituted Phthalimide Derivatives

2020 ◽  
Vol 29 (1) ◽  
pp. 247-252
Author(s):  
Halah A. Sahib ◽  
Mohammed H. Mohammed
Keyword(s):  
Antimicrobial Activity ◽  
Methyl Ester ◽  
Gram Negative Bacteria ◽  
Gram Positive ◽  
Gram Negative ◽  
Gram Positive Bacteria ◽  
Ft Ir ◽  
Bacteria And Fungi ◽  
Phenylalanine Methyl Ester

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.  

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 ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Pathogenic Fungus ◽  
Fungal Strain ◽  
Diffusion Method ◽  
Gram Negative Bacteria ◽  
Disk Diffusion Method ◽  
Gram Negative ◽  
Gram Positive Bacteria ◽  
The Stability

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.

scholarly journals Synthesis, Characterization and Antimicrobial Activity of some New Oxadiazole Derivatives in DMSO and DMF

2015 ◽  
Vol 56 ◽  
pp. 104-112
Author(s):  
Shipra Baluja ◽  
Sumitra Chanda ◽  
Paras Ramavat
Keyword(s):  
Antimicrobial Activity ◽  
Mass Spectroscopy ◽  
Gram Negative Bacteria ◽  
Gram Positive ◽  
Gram Negative ◽  
Fungal Strains ◽  
Gram Positive Bacteria ◽  
H Nmr ◽  
Oxadiazole Derivatives

A series of oxadiazole derivatives were synthesized and were characterized by IR, 1H NMR and mass spectroscopy. All these synthesized compounds were tested for in vitro antimicrobial against four Gram positive bacteria, four Gram negative bacteria and four fungal strains in DMSO and DMF.

scholarly journals Synthesis and Evaluation of Some Coumarin Based Schiff's Bases as Potential Antimicrobial Agents'

2012 ◽  
Vol 9 (4) ◽  
pp. 2079-2088 ◽  
Author(s):  
Vishakha Bansode ◽  
Meenakshi N. Deodhar
Keyword(s):  
Antimicrobial Activity ◽  
Antimicrobial Agents ◽  
Gram Negative Bacteria ◽  
Gram Positive ◽  
Gram Negative ◽  
Gram Positive Bacteria ◽  
H Nmr ◽  
Nmr Data ◽  
Bacteria And Fungi

A series of the title compounds 3-(4-(4, 5-dihydro-5-(substituted phenyl)-1H-3-pyrazolyl) phenylimino) methyl)-4-chloro-2H-chromen-2-one 5(a-g) have been synthesized. These compounds were characterized on the basis of their spectral (IR,1H NMR) data and evaluated for antimicrobial activityin vitroagainst gram positive bacteria, gram negative bacteria and fungi. The compound (5b) was found to be the most active with MIC of 20 µg/ml against all the tested organisms.

scholarly journals Enaminone-Derived Pyrazoles with Antimicrobial Activity

2019 ◽  
Vol 2019 ◽  
pp. 1-10
Author(s):  
Mashooq Ahmad Bhat ◽  
Mohamed A. Al-Omar ◽  
Ahmed M. Naglah ◽  
Abdul Arif Khan
Keyword(s):  
Antimicrobial Activity ◽  
Gram Negative Bacteria ◽  
Significant Activity ◽  
Disc Diffusion ◽  
Initial Screening ◽  
Gram Positive ◽  
Gram Negative ◽  
Disc Diffusion Assay ◽  
Gram Positive Bacteria ◽  
Diffusion Assay

A series of pyrazoles derived from the substituted enaminones were synthesized and were evaluated for antimicrobial activity. All the compounds were characterized by the spectral data and elemental analysis. The synthesized compounds were initially screened for their antimicrobial activity against ATCC 6538, NCTC 10400, NCTC 10418, and ATCC 27853. During initial screening, compounds (P1, P6, and P11) presented significant antimicrobial activity through disc diffusion assay. These compounds were further evaluated for antimicrobial activity at different time points against Gram-positive and Gram-negative bacteria and presented significant activity for 6 hours. The activity was found to be greater against Gram-positive bacteria. In contrast at 24 hours, the activity was found only against Gram-positive bacteria except compound (P11), showing activity against both types of bacteria. Compound (P11) was found to have highest activity against both Gram-positive and Gram-negative bacteria.

scholarly journals In Vitro and In Vivo Antibacterial Activities of DW-224a, a New Fluoronaphthyridone

2006 ◽  
Vol 50 (6) ◽  
pp. 2261-2264 ◽  
Author(s):  
Hee-Soo Park ◽  
Hyun-Joo Kim ◽  
Min-Jung Seol ◽  
Dong-Rack Choi ◽  
Eung-Chil Choi ◽  
...  
Keyword(s):  
Antibacterial Activities ◽  
The Other ◽  
Vitro Activity ◽  
Gram Negative Bacteria ◽  
In Vitro Activity ◽  
Gram Positive ◽  
Gram Negative ◽  
Gram Positive Bacteria

ABSTRACT DW-224a showed the most potent in vitro activity among the quinolone compounds tested against clinical isolates of gram-positive bacteria. Against gram-negative bacteria, DW-224a was slightly less active than the other fluoroquinolones. The in vivo activities of DW-224a against gram-positive bacteria were more potent than those of other quinolones.

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