Synthesis and Biological Evaluation of Chalconyl Incorporated Schiff’s Bases of Sulphonamides

Author(s):  
Neeraj Kumar ◽  
Dhruti Bhatt ◽  
Chandra Shekhar Sharma ◽  
Hamendra Pratap Singh ◽  
Harshda Pandiya ◽  
...  

A series of of Chalconyl Incorporated Schiff’s Bases of Sulphonamides was synthesized by reacting substituted chalcone derivatives with Sulphacetamide sodium in methanol. All the title compounds synthesized (2a-2d) were tested for antibacterial and antifungal activity using E. coli, P. aeruginosa, S. aureus, S. pyogenus and C. albicans, A. niger and A. clavatus respectively as microbial strains and Sulphacetamide sodium as standard. The compound 2d showed significant antibacterial activity and 2a showed moderate antifungal activity as compared with Sulphacetamide Sodium.

2020 ◽  
Vol 8 (6) ◽  
pp. 179-187
Author(s):  
Titik Taufikurohmah ◽  
Tasha Anandya Tantyani

This Research on the antibacterial and antifungal activity of nanosilver against Neisseria gonorrhoeae and Candida albincas fungi has been carried out. The purpose of this study was to determine antibacterial activity of nanosilver against Neisseria gonorrhoeae and antifungal activity against Candida albincas. Synthesis Nanosilver uses bottom up method and characterized using UV-Vis Spectrophotometer. Nanosliver concentrations used were 30, 40, 50, and 60 ppm. Antibacterial and antifungal activity tests using disk diffusion method. Observations obtained in form of the presence or absence of clear zones formed around paper discs indicate the inhibition of nanosilver on microbial growth. The results of testing the antifungal activity of Candida albicans on nanosilver with concentrations of 30, 40, 50 and 60 ppm resulted in clear zones of 9.73 nm, 11.46 nm, 11.93 nm, and 13 nm with fungal inhibition response categories is medium and strong. The results antibacterial activity test of Neisseria gonorrhoeae on nanosilver with concentrations of 30, 40, 50 and 60 ppm did not show any clear zone around the disc, it showed that nanosilver in this study did not have antibacterial activity against Neisseria gonorrhoeae.


2021 ◽  
Vol 2 (2) ◽  
pp. 93-103
Author(s):  
Nathaniel Hiwandika ◽  
Susana Elya Sudrajat ◽  
Ika Rahayu

Cloves is one of the native Indonesian plants and is used in many aspects of life. Cloves are used in multiple industries and as detergents, soaps, perfumes, food seasonings, aromatherapy, etc. Cloves are mainly used for ingredients in kretek cigarettes in Indonesia. Various studies of cloves reported they have good pharmacological and therapeutic effects. The main compounds of clove extract are eugenol and β-caryophyllene, which are powerful antibacterial and antifungal agents. The clove ethanolic extract showed the activity to inhibit Gram positive and negative bacteria such as B. cereus, S. aureus, E. coli, P. aeruginosa, S. pneumoniae, S. aureus, S. epidermidis, A. hydrophila, K. pneumoniae, P. gingivalis, and P. mirabilis. Clove essential oil has shown the ability to inhibit the growth of V. inaequalis, C. albicans, C. glabrata, and C. tropicalis. Cloves extract can be used as an essential ingredient of various medicines. However, it requires further research and trials.


2020 ◽  
Vol 13 (9) ◽  
pp. 229
Author(s):  
Volodymyr Horishny ◽  
Victor Kartsev ◽  
Vasyl Matiychuk ◽  
Athina Geronikaki ◽  
Petrou Anthi ◽  
...  

Herein we report the design, synthesis, computational, and experimental evaluation of the antimicrobial activity of fourteen new 3-amino-5-(indol-3-yl) methylene-4-oxo-2-thioxothiazolidine derivatives. The structures were designed, and their antimicrobial activity and toxicity were predicted in silico. All synthesized compounds exhibited antibacterial activity against eight Gram-positive and Gram-negative bacteria. Their activity exceeded those of ampicillin and (for the majority of compounds) streptomycin. The most sensitive bacterium was S. aureus (American Type Culture Collection ATCC 6538), while L. monocytogenes (NCTC 7973) was the most resistant. The best antibacterial activity was observed for compound 5d (Z)-N-(5-((1H-indol-3-yl)methylene)-4-oxo-2-thioxothiazolidin-3-yl)-4-hydroxybenzamide (Minimal inhibitory concentration, MIC at 37.9–113.8 μM, and Minimal bactericidal concentration MBC at 57.8–118.3 μM). Three most active compounds 5d, 5g, and 5k being evaluated against three resistant strains, Methicillin resistant Staphilococcus aureus (MRSA), P. aeruginosa, and E. coli, were more potent against MRSA than ampicillin (MIC at 248–372 μM, MBC at 372–1240 μM). At the same time, streptomycin (MIC at 43–172 μM, MBC at 86–344 μM) did not show bactericidal activity at all. The compound 5d was also more active than ampicillin towards resistant P. aeruginosa strain. Antifungal activity of all compounds exceeded those of the reference antifungal agents bifonazole (MIC at 480–640 μM, and MFC at 640–800 μM) and ketoconazole (MIC 285–475 μM and MFC 380–950 μM). The best activity was exhibited by compound 5g. The most sensitive fungal was T. viride (IAM 5061), while A. fumigatus (human isolate) was the most resistant. Low cytotoxicity against HEK-293 human embryonic kidney cell line and reasonable selectivity indices were shown for the most active compounds 5d, 5g, 5k, 7c using thiazolyl blue tetrazolium bromide MTT assay. The docking studies indicated a probable involvement of E. coli Mur B inhibition in the antibacterial action, while CYP51 inhibition is likely responsible for the antifungal activity of the tested compounds.


2019 ◽  
Vol 18 (5) ◽  
pp. 213-221 ◽  
Author(s):  
Dumrul Gulen ◽  
Temine Sabudak ◽  
Hakime H. Orak ◽  
Hilmican Caliskan ◽  
Merve Ozer

In the GC-MS analysis, 81 bioactive phytochemical compounds were identified in the hexane extracts of Cirsium creticum and Cirsium italicum. Terpenoids constituted the main fractions of C. italicum (70.95 %) while hydrocarbons were most abundant compounds of C. creticum (41.11 %). The antibacterial activity and antifungal activity of extracts from two Cirsium species was tested by using microdilution methods. According to the results of antibacterial activity, highest inhibition effect of C. creticum was found on B. subtilis, E. coli and P. aeruginosa. The highest inhibition effect of C. italicum was found on B. subtilis. In the results of antifungal activity, highest inhibition effect of C. creticum was found on P. chrysogenum and highest inhibition effect of C. italicum was found on C. krusei. The present work is the first report on hexane extracts compounds of two Cirsium species as well as the antibacterial and antifungal activities.


Author(s):  
Janaki H. Chauhan ◽  
Haresh K. Ram

An efficient Synthesis of a novel series of N,7-bis(substitutedphenyl)-4,7-dihydro-5-isopropyl-[1,2,4]triazolo-[1,5-a]pyrimidine-6-carboxamide (4a-j) was accomplished from N-(substituedphenyl)-4-methyl-3-oxopentanamide, 3-amino-1,2,4-triazole and different aldehyde reflex 20 min with DMF and then after the cooling product was obtained. All the recently synthesized compounds were characterized by the Mass, IR, 1H-NMR and mass spectroscopic techniques and by elemental analyses. The newly synthesized compounds were assessed for their antibacterial and antifungal activity.


Author(s):  
Laila Jarin ◽  
Md Shafiqur Rahman ◽  
MN Anwar

Petroleum ether, carbon tetrachloride, chloroform and ethyl acetate extracts of Plumeria rubra leaves were studied for their antimicrobial activities against eleven human pathogenic bacteria, viz., Shigella dysenteriae, S. sonnei, Salmonella typhi, S. paratyphi, Bacillus subtilis, B. megaterium, B. cereus, Staphylococcus aureus, Pseudomonas aeruginosa, Escherichia coli and Vibrio cholerae and four human pathogenic fungi, viz., Aspergillus niger, A. ochraceus, A. ustus and Candida albicans using disc diffusion and poisoned food method, respectively. Chloroform and ethyl acetate extract exhibited moderate to good antibacterial and antifungal activity against all the pathogens tested. The ethyl acetate extracts exhibited the largest zone of inhibition (25 mm in diameter with 2000 mg/disc extract) against E. coli. The highest inhibition of fungal radial mycelial growth (62.00% with 100 mg extract/ml medium) was recorded against A. ustus with ethyl acetate extract. The MICs were determined by broth macrodilution technique. The ethyl acetate extract exhibited the lowest MIC (750 mg/ml) against E. coli. However, for fungi the lowest MIC was 500 mg/ml against A. ustus with the same extract. DOI: http://dx.doi.org/10.3329/cujbs.v3i1.13409 The Chittagong Univ. J. B. Sci.,Vol. 3(1&2):87-94, 2008


2000 ◽  
Vol 68 (4) ◽  
pp. 333-341 ◽  
Author(s):  
Jerzy Cieplik ◽  
Janusz Pluta ◽  
Olaf Gubrynowicz

The paper presents the synthesis of 5-substituted pyrimidine sulphonamides as well as the results of studies on the antibacterial and antifungal activity of obtained derivatives.


2008 ◽  
Vol 5 (4) ◽  
pp. 963-968 ◽  
Author(s):  
Sabir Hussain ◽  
Jyoti Sharma ◽  
Mohd Amir

Various 4-amino-2-[4-(4-substituted phenyl)-5-sulfanyl-4H-1,2,4-triazol-3-yl] phenol (4a-c), 4-amino-2-{4-amino-5-[(4-substituted phenyl)amino]-4H-1,2,4-triazol-3-yl} phenol (5a-c) and 4-amino-2-{5-[(4-substituted phenyl)amino]-1,3,4-thiadiazole-2-yl} phenol (6a-g) were synthesized and evaluated for their antibacterial and antifungal activity. The compounds showed significant antibacterial activity againstS. aureus(gram-positive) andE.coli(gram-negative) bacteria and antifungal activity againstA. nigerfungi using cup plate technique


2011 ◽  
Vol 8 (s1) ◽  
pp. S149-S154 ◽  
Author(s):  
P. Panneerselvam ◽  
G. Geete Ganesh

The syntheses of series of 2, 5-disubstituted 1, 3, 4-oxadiazole derivatives are described. A total of twelve new compounds were synthesized and characterized by IR,1H-NMR and Mass spectral data. All newly synthesized compounds were screened for their antimicrobial activityi.e. antibacterial activity againstS. aureusandE. coliand antifungal activity against fungusA. nigar. CompoundsG5andG7exhibited significant both antibacterial and antifungal activity whileG2,G10andG3,G9showed antibacterial and antifungal activity respectively. These compounds were 2, 5-disubstituted 1, 3, 4-oxadiazole moiety at position two and five showed reasonable antibacterial and antifungal activity.


Author(s):  
Jatin Vora ◽  
Kartik Vyas

A cogent synthesis of completely new compound series of by 6-(3,5-bis(trifluoromethyl)phenyl)-4-(4-chlorophenyl)-3,4-dihydro pyrimidine-2(1H)-one (Biginelli reaction) was achieved by continue heating of (E)-1-(3,5-bis(trifluoromethyl)phenyl)-3-(substituted phenyl)prop-2-en-1-one and urea for 5 hours with 40% KOH and ethyl alcohol. (E)-1-(3,5-bis(trifluoromethyl)phenyl)-3-(substituted phenyl)prop-2-en-1-one is produced by Claisen-Schmidt Condensation. In this condensation 1-(3,5-bis(trifluoromethyl)phenyl)ethanone and different aldehyde are mixed. All the novel compound series were characterized by infrared and 1H nuclear magnetic resonance and mass spectroscopic techniques and by elemental analyses. The newly synthesized compounds were evaluated for their antibacterial and antifungal activity


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