scholarly journals Synthesis, Antibacterial, and Antifungal Activities of Hybrid Molecules Based on Alzheimer Disease Drugs and Bearing an Amino Acid Fragment

Proceedings ◽  
2019 ◽  
Vol 41 (1) ◽  
pp. 23 ◽  
Author(s):  
Radoslav Chayrov ◽  
Aleksandra Tencheva ◽  
Hristina Sbirkova-Dimitrova ◽  
Boris Shivachev ◽  
Anna Kujumdzieva ◽  
...  

The objective of the current study was to develop novel compounds–memantine derivatives with antimicrobial activity designed for application in treatment of bacterial and fungal infections in patients suffering from Alzheimer’s disease. To realize this objective, a series of six memantine hybrid molecules were synthesized, characterized by 1H NMR, 13C NMR, MS, X-ray, and tested for their biological properties as anti-Alzheimer agents and their antimicrobial potential.

2013 ◽  
Vol 2013 ◽  
pp. 1-5 ◽  
Author(s):  
Cristiana da Purificação Pinto ◽  
Velize Dias Rodrigues ◽  
Fernanda da Purificação Pinto ◽  
Renata da Purificação Pinto ◽  
Ana Paula Trovatti Uetanabaro ◽  
...  

Lippia origanoidesKunth,Lippia alnifoliaSchauer, andLippia thymoidesMartius and Schauer are shrubs used in the traditional Brazilian medicine as antiseptics, as well as in the treatment of infectious diseases. This study was designed to investigate the antibacterial and antifungal activities of the methanolic extracts of these species, as new potential sources of antimicrobial drugs. The antimicrobial activity of methanolic extracts was investigated against resistant yeasts and bacteria by agar disk diffusion. Then, the MIC determination of the most active species and its fractions in hexane, dichloromethane, ethyl acetate, and water was performed. By the agar diffusion assay, all species were active against at least two microorganisms, giving evidence to support their use in the popular medicine.L. origanoidesleaves exhibited the widest antimicrobial action, inhibiting the growth of two Gram-positive bacteria and two yeasts; this activity was also confirmed by the MIC evaluation. The fractionation ofL. origanoidescrude extracts improved the activity in spectrum and intensity. The results obtained in this study indicate thatL. origanoidesmay be a promising alternative in the treatment of bacterial and fungal infections and in the seeking of new antimicrobial drugs.


2020 ◽  
Vol 13 (11) ◽  
pp. 375
Author(s):  
Surendra Babu Lagu ◽  
Rajendra Prasad Yejella ◽  
Richie R. Bhandare ◽  
Afzal B. Shaik

Despite the availability of many drugs to treat infectious diseases, the problems like narrow antimicrobial spectrum, drug resistance, hypersensitivities and systemic toxicities are hampering their clinical utility. Based on the above facts, in the present study, we designed, synthesized and evaluated the antibacterial and antifungal activity of novel fluorinated compounds comprising of chalcones bearing trifluoromethyl (A1–A10) and trifluoromethoxy (B1–B10) substituents. The compounds were characterized by spectroscopic techniques and evaluated for their antimicrobial activity against four pathogenic Gram-positive (Staphylococcus aureus and Bacillus subtilis) and Gram-negative (Escherichia coli and Bacillus subtilis) bacterial and fungal (Candida albicans and Aspergillus niger) strains. In this study, the compounds with trifluoromethoxy group were more effective than those with trifluoromethyl group. Among the 20 fluorinated chalcones, compound A3/B3 bearing an indole ring attached to the olefinic carbon have been proved to possess the most antimicrobial activity compared to the standard drugs without showing cytotoxicity on human normal liver cell line (L02). Further, the minimum inhibitory concentration (MIC) for A3/B3 was determined by serial tube dilution method and showed potential activity. These results would provide promising access to future study about the development of novel agents against bacterial and fungal infections.


1970 ◽  
Vol 5 (1) ◽  
pp. 29-32 ◽  
Author(s):  
Jahan Ara Khanam ◽  
Most. Ferdousi Begum ◽  
Jesmine Ara ◽  
Mele Jesmin ◽  
M Abu Taher ◽  
...  

Metal cystine complexes of nickel(II), mercury(II) and cadmium(II) have been synthesized and their antimicrobial activities have been evaluated. It is found that mercury(II) cystine and cadmium(II) cystine complexes have pronounced antibacterial and antifungal activities. On the other hand nickel(II) cystine shows moderate activities. The LC50 values of nickel(II) cystine, mercury(II) cystine and cadmium(II) cystine are found to be 5.2, 8.0 and 7.2 ?g ml-1, respectively. These values were obtained from cytotoxic studies indicating that they are biologically active compounds. Key words: Antimicrobial activity, Cytotoxic activity; Metal amino acid complexes. Dhaka Univ. J. Pharm. Sci. Vol.5(1-2) 2006 The full text is of this article is available at the Dhaka Univ. J. Pharm. Sci. website


2021 ◽  
Vol 68 (4) ◽  
pp. 990-996
Author(s):  
Mohamed A. Salem ◽  
Samir Y. Abbas ◽  
Marwa A. M. Sh. El-Sharief ◽  
Mohamed H. Helal ◽  
Moustafa A. Gouda ◽  
...  

One of the best ways to design new biocidal agents is synthesizing hybrid molecules by combining two or more bioactive moieties in a single molecular scaffold. So, new series of pyrroles bearing a thiazole moiety were synthesized using 1-methyl-1H-pyrrole-2-carbaldehyde thiosemicarbazones 1a–c. Cyclization of thiosemicarbazone derivatives 1a–c with ethyl chloroacetate, ethyl 2-chloropropanoate, chloroacetone and phenacyl bromide afforded the corresponding thiazolidin-4-ones 2a–c, 5-methylthiazolidin-4-ones 3a–c, 4-methyl-2,3-dihydrothiazoles 4a–c, and 4-phenyl-2,3-dihydrothiazoles 5a–c, respectively. The antimicrobial activity of the new thiazole derivatives was evaluated.


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.


2016 ◽  
Vol 11 (2) ◽  
pp. 248 ◽  
Author(s):  
Kathirvel Poonkodi ◽  
Subban Ravi

<p class="Abstract">The present study was aimed to evaluate the phytochemical screening and antimicrobial activity of the petroleum ether and methanol extracts from the mature leaves of <em>Richardia scabra</em> from India. Disc diffusion method was used to determine the zone inhibition of the tested samples for antibacterial and agar plug method was used to determine the antifungal activity, while the microtube-dilution technique was used to determine the minimum inhibitory concentration. Both extracts showed significant antibacterial and antifungal activities when tested against 10 bacterial and four fungal strains. The minimum inhibitory concentrations of the methanol extract of<em> R. scabra</em> ranged between 12.5–100 μg/mL for bacterial strains. Alkaloids, steroids, flavonoids, fatty acids, terpenoids and simple sugar were detected as phytoconstituents of extracts. To the best of our knowledge, this is the first report against antimicrobial activity of common weed species <em>R. scabra</em> found in India.</p><p> </p>


2008 ◽  
Vol 5 (3) ◽  
pp. 461-466 ◽  
Author(s):  
Y. Rajendra Prasad ◽  
A. Lakshmana Rao ◽  
R. Rambabu

In an effort to develop antimicrobial agents, a series of chalcones were prepared by Claisen-Schmidt condensation of appropriate acetophenones with appropriate aromatic aldehydes in the presence of aqueous solution of potassium hydroxide and ethanol at room temperature. The synthesized compounds were characterized by means of their IR,1H-NMR spectral data and elemental analysis. All the compounds were tested for their antibacterial and antifungal activities by the cup plate method.


Peptides ◽  
2013 ◽  
Vol 45 ◽  
pp. 78-84 ◽  
Author(s):  
Andre L.A. Souza ◽  
Paola Díaz-Dellavalle ◽  
Andrea Cabrera ◽  
Patricia Larrañaga ◽  
Marco Dalla-Rizza ◽  
...  

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.


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