scholarly journals Synthesis and Antimicrobial Screening of Some Novel 2, 5-Disubstituted 1, 3, 4-oxadiazole Derivatives

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.

2020 ◽  
Vol 18 (2) ◽  
pp. 128-134
Author(s):  
Dhanapal Visagaperumal ◽  
Vineeth Chandy

Background: In this study, synthesis of some novel 1-(3-(4-chlorophenylimino)-3,4- dihydroquinoxalin-2-yl)-3-substituted phenyl-1H-pyrazole-4-carbaldehyde were done by cyclization of dehydrated hemiketal using VilsmeierHaack reaction. The structures of synthesized compounds were in accordance of the basis of IR, 1HNMR, Mass spectral data and elemental analyses. The synthesized compounds had given good yields and high purity. Methods: The antimicrobial activity of the synthesized compounds was preliminarily screened by paper disc diffusion technique. The determination of minimum inhibitory concentrations (MIC) of the synthesized compounds were done by using tube dilution method. Results and Conclusion: All the screened compounds showed antibacterial and antifungal activity against selected strains of Gram positive and Gram negative bacteria and two strains of fungus, respectively but exhibited considerably less activity when compared to the reference drug ciprofloxacin and Fluconazole for antibacterial and antifungal activity, respectively. Among the synthesized compounds VV5 exhibited significant activity.


2014 ◽  
Vol 2014 ◽  
pp. 1-9 ◽  
Author(s):  
Gadada Naganagowda ◽  
Reinout Meijboom ◽  
Amorn Petsom

Various novel Schiff base compounds have been synthesized by reaction of 2-hydroxy-4-pentadecylbenzaldehyde with substituted benzothiophene-2-carboxylic acid hydrazide and different substituted aromatic or heterocyclic amines in the presence of acetic acid in ethanol. The structures of all these compounds were confirmed by elemental analysis, IR, 1H-NMR, 13C-NMR, and mass spectral data and have been screened for antibacterial and antifungal activity.


Author(s):  
Mahesh Chidara ◽  
Satla Shobha Rani

Novel antibacterial compounds are needed to combat the emerging bacterial infections. In this study, synthesis of 4-substituted benzylpiperazin-1-yl methanone derivatives was carried out by 4-substituted benzyl chloride (I) with piperazine in presence of ethanol to obtain 4-substituted benzylpiperazines (II). Benzylpiperazines (II) was condensed with different substituted esters in presence of diluted acid to produce title compounds (IIIa–e, IVa-e and Va-e). All the title compounds were screened for possible antibacterial activity against P. Vulgaris, S. Aureas, E. Coli, B. Subtillus and antifungal activity against Altenaria, Culvalaria, C. Albicans and A. Niger. Among the compounds synthesized IVb, IVd and IVf demonstrated good antibacterial activity; IVb, IVc, and IVe showed good antifungal activity. The activities of the synthesized compounds are compared with the standard and other test compounds. The structures of synthesized compounds were established by elemental analysis, IR, H NMR and Mass spectral data. Future studies will confirm their efficacy and utility as antibacterial agents. 


2020 ◽  
Vol 20 (29) ◽  
pp. 2681-2691
Author(s):  
Athina Geronikaki ◽  
Victor Kartsev ◽  
Phaedra Eleftheriou ◽  
Anthi Petrou ◽  
Jasmina Glamočlija ◽  
...  

Background: Although a great number of the targets of antimicrobial therapy have been achieved, it remains among the first fields of pharmaceutical research, mainly because of the development of resistant strains. Docking analysis may be an important tool in the research for the development of more effective agents against specific drug targets or multi-target agents 1-3. Methods: In the present study, based on docking analysis, ten tetrahydrothiazolo[2,3-a]isoindole derivatives were chosen for the evaluation of the antimicrobial activity. Results: All compounds showed antibacterial activity against eight Gram-positive and Gram-negative bacterial species being, in some cases, more potent than ampicillin and streptomycin against all species. The most sensitive bacteria appeared to be S. aureus and En. Cloacae, while M. flavus, E. coli and P. aeruginosa were the most resistant ones. The compounds were also tested for their antifungal activity against eight fungal species. All compounds exhibited good antifungal activity better than reference drugs bifonazole (1.4 – 41 folds) and ketoconazole (1.1 – 406 folds) against all fungal species. In order to elucidate the mechanism of action, docking studies on different antimicrobial targets were performed. Conclusion: According to docking analysis, the antifungal activity can be explained by the inhibition of the CYP51 enzyme for most compounds with a better correlation of the results obtained for the P.v.c. strain (linear regression between estimated binding Energy and log(1/MIC) with R 2 =0.867 and p=0.000091 or R 2 = 0.924, p= 0.000036, when compound 3 is excluded.


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.


2013 ◽  
Vol 2013 ◽  
pp. 1-13 ◽  
Author(s):  
Vivekanand D. Biradar ◽  
B. H. M. Mruthyunjayaswamy

A series of new coordination complexes of Cu(II), Co(II), Ni(II), Zn(II), Hg(II), Mn(II), and Fe(III) with the Schiff base 3-chloro-N′-[(1E)-(2-hydroxy phenyl)methylene]-6-methoxy-1-benzothiophene-2-carbohydrazide (HL) have been synthesized and characterized by elemental analysis, electrical conductivity measurements, IR spectra,1H NMR, mass spectral data, electronic spectra, magnetic susceptibility, ESR spectra, TGA, and Powder XRD data. The Schiff base behaves as tridentate ONO donor ligand and forms the complexes of the type ML2(metal-ligand) stoichiometry for Cu(II), Co(II), Ni(II), and Mn(II) complexes and ML stoichiometry for Zn(II), Hg(II), and Fe(III) complexes. All the complexes are colored and nonelectrolytes. It is found that Cu(II), Co(II), Ni(II), Mn(II) and Fe(III) complexes have exhibited octahedral geometry whereas Zn(II) and Hg(II) complexes exhibited tetrahedral geometry. The ligand and its metal complexes have been screened for their antibacterial activity againstE. coliandS. aureusand antifungal activity againstA. nigerandA. flavus.


2009 ◽  
Vol 6 (3) ◽  
pp. 775-779 ◽  
Author(s):  
B. Rajeeva ◽  
N. Srinivasulu ◽  
S. M. Shantakumar

Some new 2-(5-substituted-1,3,4-oxadiazole-2-yl)-1,3- benzothiazole(3a-j)were synthesized by refluxing benzothiazolyl carboxyhydrazide with different aryl acids in phosphoryl chloride. Structures of the synthesized compounds were established on the basis of1H NMR and Mass spectral data. The anti microbial activity of the synthesized compounds was evaluated by disc diffusion method.


2020 ◽  
Vol 8 (2) ◽  
pp. 48
Author(s):  
Feskaharny Alamsjah ◽  
Djong Hon Tjong ◽  
Zil Fadhillah Rahma

The research on antimicrobial activity of skin secretion derived from Rana hosii (Anura: Ranidae) against several pathogenic microbes had been conducted at Microbiology Laboratory and at Genetics and Biomolecular Laboratory, both in the Biology Department, Universitas Andalas. The research used to survey and experimental methods. The study aimed to determine the effectivity of Rana hosii skin secretion to inhibit microbial activity, hence it tested onto some pathogenic microbes such as Escherichia coli, Staphylococcus aureus and Candida albicans. The results showed that the biggest inhibition zone formed against E. coli was 10.96 + 0.63 mm, on S. aureus was 11.74 + 1.00 mm, while on C. albicans was 7.42 + 0.80 mm. The results indicated that the skin secretions from Rana hosii frog could be a potential broad-spectrum antibacterial, and antifungal activity against C. albicans.


Author(s):  
Vijay N. Bhadani ◽  
Piyush A. Patel ◽  
Heta D. Purohit ◽  
Dipak M. Purohit

Various isopropylacetoacetanilides were treated with 4-(difluoromethoxy)-3-hydroxy benzaldehyde and thiourea/urea in the presence of acid catalyst to produce the 1,4-dihydropyrimidine derivatives (4a-5i and 5a-5i) with good yields. All the synthesized compounds were characterized by mass, 1H-NMR and IR spectrum, also evaluated for antibacterial and antifungal activity against two Gram +ve and two Gram-ve bacterial and fungi strains. The compounds 4e, 4g and 5d were found comparatively promising active against all the bacterial and fungal strains.


2014 ◽  
Vol 10 (7) ◽  
pp. 2901-2915 ◽  
Author(s):  
Shawkat A. Abdelmohsen ◽  
Talaat I El Emary

The present work describes the synthesis of a novel series of heterocyclic moieties derived from 5-acetylpyrazolo[3,4-b]pyridine (1). The formation of chalcones (2a-d) was utilized to synthesize pyrazoline, isoxazoline and pyrimidine derivatives (3-10). Thiosemicarbazone and semicarbazone (11, 17) were utilized to synthesize other new triazolethiones, thiadiazole and selenadiazole derivatives (11-19). Some new spiro derivatives (22-25) were synthesized by the reaction of chalcone (21) of 1 and isatine with hydrazines, hydroxyl amines and thiourea. Also, The reaction of 1 with cyanoacetyl hydrazine gave the hydrazide-hydrazone derivative 26, which was allowed to react with aromatic aldehydes and α-cyanocinnamonitrile to afford coumarine and substituted pyridine derivatives (28, 29). The structures of all the new compounds have been established on the basis of their analytical and spectral data. Twenty two of the synthesized compounds were also evaluated for their antibacterial and antifungal activity against various strains of bacteria and fungi and most are found to possess promising antimicrobial activity when compared with Chloramphenicol and Clotrimazole


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