Synthesis and antimicrobial activity of 3,4-dihydropyrimidin-2(1H)-one derivatives containing a hydrazone moiety

2018 ◽  
Vol 24 (2) ◽  
pp. 113-117 ◽  
Author(s):  
Hua-Nan Peng ◽  
Li-Min Ye ◽  
Ming Zhang ◽  
Yan-Chun Yang ◽  
Jie Zheng

AbstractThe title compounds were synthesized and characterized by IR,1H NMR,13C NMR and HRMS data. Their antimicrobial activities against bacterial strainsEscherichia coliand fungal strainsAspergillus nigerwere evaluated.

Author(s):  
P Danish ◽  
Q Ali ◽  
MM Hafeez ◽  
A Malik

Aloe vera is a well-known medicinal plant used in many therapeutic purposes. Naturally it is composed of many useful compounds that have ability to use for treatment of many diseases. The active compounds reported in this plant are saponins, sugar, enzymes, vitamins, aloesin, aloeemodin, aloin, acemannan aloemannan, aloeride, methylchromones, flavonoids, naftoquinones, sterols, minerals, anthraquinones, amino acids, lignin and salicylic acid and other different compounds including fat-soluble and water-soluble vitamins, enzymes, minerals, simple/complex sugars, organic acid and phenolic compounds. In this study aloe vera is used for antibacterial and antifulgal activity against different strains of bacteria and pathogenic fungal strains. Ethanol extract of Aloe vera leaves and roots is applied on these bacterial and fungal strains in different concentrations (15, 20, 25, 30µl). Bacillus cereus, Bacillus subtitis, Bacillus megaterium, Streptococcus pyogenes, Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, Acinetobacter baumannii, and some other bacterial strains are used for this study. Escherichia coli and Agrobacterium tumefacins shows zone of inhibition around 18mm which consider as good result. Bacillus subtitis and Bacillus megaterium also shows good result around 16mm. Proteus mirabilis and Pseudomonas aeruginosa shows minimum zone of inhibition which is around 11mm. among all used fungal strains (fuserium oxysporum, Candida albicans, Aspergillus fumigatus, Aspergillus niger) fuserium oxysporum and Aspergillus niger shows excellent results around 19mm both against root extract and leaves extract.


2021 ◽  
Vol 37 (2) ◽  
pp. 508-512
Author(s):  
Jaganmohana Rao Saketi ◽  
S N Murthy Boddapati ◽  
Raghuram M ◽  
Geetha Bhavani Koduru ◽  
Haribabu Bollikolla

The in vitroantimicrobial properties of a series of N-methyl-3-aryl indazoles (5a-5j) were screened. In this present work, we describe our efforts towards the development of potent antimicrobial activity of synthesized indazole derivatives. The antimicrobial activities of the prepared compounds were investigated against four bacterial strains: Xanthomonas campestris, Escherichia coli, Bacillus cereus, Bacillus megaterium, and a fungal strain Candida albicans. The biological evaluation studies of these indazole derivatives revealed that some of these tested compounds have shown moderate to goodin vitroantimicrobial activities.


2013 ◽  
Vol 2013 ◽  
pp. 1-6 ◽  
Author(s):  
Naureen Aggarwal ◽  
Vishal Sharma ◽  
Harpreet Kaur ◽  
Mohan Paul Singh Ishar

Novel substituted 1,2,4-dithiazolylchromones 3a–j were synthesized by the reaction of 3-formylchromones (1a–j) with two equivalents of p-chlorothiobenzamide (2) in dry xylene and characterized spectroscopically (IR, 1H and 13C NMR, mass) and elemental analysis. All synthesized compounds were screened for in vitro antimicrobial activity against various pathogenic bacterial and fungal strains and were found to possess good to moderate inhibitory potential against all tested strains. Antimicrobial results reveal that compounds bearing lipophilic electron withdrawing groups such as chloro and bromo displayed significant inhibitory potential against both bacterial and fungal strains. Particularly, compound 3c displayed significant inhibitory against bacterial strains and compound 3h exhibits significant inhibitory potential in comparison to standard drug fluconazole against fungal strain S. cerevisiae.


2013 ◽  
Vol 2013 ◽  
pp. 1-7 ◽  
Author(s):  
Bhimagouda S. Patil ◽  
G. Krishnamurthy ◽  
N. D. Shashikumar ◽  
M. R. Lokesh ◽  
H. S. Bhojya Naik

A series of novel [1,2,4]-triazolo piperidine (8), [1,2,4]-triazolo piperazine (9a-c), [1,2,4]-triazolo phenylether (10a-e), and [1,2,4]-triazolo aniline (11a-c) derivatives have been synthesized. The chemical structures of the newly synthesized compounds were characterized by IR,1H NMR,13C NMR, and LCMS. The newly synthesized compounds were screened for antimicrobial activity. Among all the compounds tested,11b(R4=4-MeO–) showed the highest activity againstStaphylococcus aureusandEscherichia coli, and9a(R1andR2=Cl) showed the highest activity againstPseudomonas aeruginosa.


2011 ◽  
Vol 189-193 ◽  
pp. 1049-1055
Author(s):  
Xi Rong Zhao

A new chitosan ester derivative, chitosan p-hydroxybenzoate is synthesized, which is expected to have antimicrobial activity similar to parabens. The amino group of chitosan reacts well with acyl chloride to prepare a N-amic acid-chitosan. The amino group of chitosan must be protected before synthesizing a 6-O-chitosan ester. Phthalic anhydride is selected to react with chitosan to form N-phthalimide chitosan whose free amino group is protected. By six steps chitosan p-hydroxybenzoate is synthesized. FTIR,1H NMR and13C NMR spectra show that the ester bond is formed between p-hydroxybenzonic acid and chitosan. Water solubility of the ester is slightly better than that of heptyl p-hydroxybenzoate, and its solubility in alcohol is greatly improved. Chitosan p-hydroxybenzoate showes broader spectrum antimicrobial activities. It has strong antimicrobial effects against Gram-negative, Gram-positive bacteria and yeasts. The MICs of chitosan p-hydroxybenzoate for Staphylococcus aureus and Escherchia coli are 0.01% and 0.025%, respectively.


Author(s):  
K. Sathiyamoorthi ◽  
V. Mala ◽  
R. Suresh ◽  
S.P. Sakthinathan ◽  
D. Kamalakkannan ◽  
...  

Some 2’-hydroxyphenylchalcones have been synthesized under microwave irradiation by Claisen-Schmidt condensation between substituted 2-hydroxyacetophenone and substituted benzaldehydes using catalytic amount of SiO2-H3PO4. These chalcones were established by their physical constants and spectroscopic data published earlier. The UV, IR, 1H NMR and 13C NMR spectral data of these chalcone have correlated with Hammett substituent constants, F and R parameters. All the compounds have been subjected to screened for antimicrobial activity.


Author(s):  
Nisheeth C. Desai ◽  
Tushar J. Karkar

The synthesis of a novel series of 6-((arylidene) amino)-2-oxo-1-((1-(2-oxo-2H-chromen-3-yl) ethylidene) amino)-4-phenyl-1,2-dihydropyridine-3,5-dicarbonitriles 4a-o were synthesized and structures of compounds have been elucidated by IR,1H NMR,13C NMR and mass spectral data. Antimicrobial activity was measured against certain strains of bacteria and fungi by serial broth dilution. Evaluation of antimicrobial activity shown that the compounds (4g, 4j, 4k and 4o) were found to be most active against selected bacterial strains and compounds (4d, 4m and 4n) were found to be most active against selected fungal strains.


2013 ◽  
Vol 2013 ◽  
pp. 1-6
Author(s):  
Awaz Jamil Hussein ◽  
Hashim Jalal Azeez

A number of derivatives of 2-(substituted phenyl)-3-(4-(6-methylbenzo[d]thiazol-2-yl)phenyl) thiazolidin-4-one (3a–j) have been synthesized from the reaction of 4-(6-methylbenzo[d]thiazol-2-yl)benzenamine(1), with different substituted benzaldehydes (2a–j), followed by cyclocondensation reaction of the prepared imines with 2-meraptoacetic acid in high yields. Furthermore, the structures of the newly synthesized compounds were confirmed by FT-IR,13C-NMR,13C-DEPT, and1H-NMR spectral data. The imines and thiazolidin-4-one derivatives were evaluated for their antibacterial activity againstEscherichia colias gram negative andStaphylococcus aureusas gram positive, the results have shown significant activity against both types of bacteria.


2017 ◽  
Vol 2017 ◽  
pp. 1-6 ◽  
Author(s):  
Muhammad Abdul Qadir ◽  
Syeda Kiran Shahzadi ◽  
Asad Bashir ◽  
Adil Munir ◽  
Shabnam Shahzad

The study was designed to evaluate the phenolic, flavonoid contents and antioxidant and antimicrobial activities of onion (Allium cepa), garlic (Allium sativum), mint (Mentha spicata), thyme (Thymus vulgaris), oak (Quercus), aloe vera (Aloe barbadensis Miller), and ginger (Zingiber officinale). All extracts showed a wide range of total phenolic contents, that is, 4.96 to 98.37 mg/100 g gallic acid equivalents, and total flavonoid contents, that is, 0.41 to 17.64 mg/100 g catechin equivalents. Antioxidant activity (AA) was determined by measuring reducing power, inhibition of peroxidation using linoleic acid system, and 2,2-diphenyl-1-picrylhydrazyl radical (DPPH) scavenging activity. Different extracts inhibited oxidation of linoleic acid by 16.6–84.2% while DPPH radical scavenging activity (IC50 values) ranged from 17.8% to 79.1 μg/mL. Reducing power at 10 mg/mL extract concentration ranged from 0.11 to 0.84 nm. Furthermore the extracts of these medicinal herbs in 80% methanol, 80% ethanol, 80% acetone, and 100% water were screened for antimicrobial activity by disc diffusion method against selected bacterial strains, Staphylococcus aureus, Escherichia coli, Bacillus subtilis, and Pasteurella multocida, and fungal strains, Aspergillus niger, Aspergillus flavus, Rhizopus solani, and Alternaria alternata. The extracts show better antimicrobial activity against bacterial strains as compared to fungal strains. Results of various assays were analyzed statistically by applying appropriate statistical methods.


2012 ◽  
Vol 2012 ◽  
pp. 1-8 ◽  
Author(s):  
Mohamad Yusuf ◽  
Indu Solanki ◽  
Payal Jain

The diisochromenochromen-4-one3a-3b,4a-4c,5a-6a  & 7have been prepared from the photocyclization reaction of bischromen-4-one2a-2e. The later compounds are obtained from the O-alkylation of the suitable 3-hydroxy-2-aryl-4H-chromen-4-one1a-1ewith 4,4′-bischloromethyl-diphenyl in dry acetone, anhydrous K2CO3, and PTC (Bu4N+I−) under refluxing conditions. The structures of compounds2a-2e,3a-3b,4a-4c,5a-6a  & 7have been characterized from the rigorous analysis of their IR,1H-NMR,13C-NMR, ESI-Mass, and elemental analysis. The antibacterial and antifungal activities of the synthesized products were also evaluated against theKlebsiella pneumoniae, Pseudomonas aeruginosa, Escherichia coli, Staphylococcus aureus, Bacillus subtilis, andAspergillus janusandPenicillium glabrum, respectively. Some of the tested compounds showed significant activity against the above-said microorganisms.


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