scholarly journals Microwave-Assisted Synthesis of Some 1,3,4-Oxadiazole Derivatives and Evaluation of Their Antibacterial and Antifungal Activity

2014 ◽  
Vol 2014 ◽  
pp. 1-6 ◽  
Author(s):  
Deepak Swarnkar ◽  
Rakshit Ameta ◽  
Ritu Vyas

A series of substituted 1,3,4-oxadiazole derivatives (3a–f) and (6a–f) have been synthesized from diphenylacetic acid hydrazide under microwave irradiation in various reaction conditions. The structures of the synthesized compounds were assigned on the basis of elemental analysis, IR, and 1H NMR. These targeted compounds have been tested for their antibacterial and antifungal activities compared to ampicillin and griseofulvin as standard drug. Compounds 3a, 3e, 3f, 6c, 6d, 6e, and 6d exhibited the maximum antibacterial activities while 3b, 3c, 3d, 3e, 6a, 6d, and 6e exhibited the maximum antifungal activities.

2021 ◽  
Vol 43 (5) ◽  
pp. 578-578
Author(s):  
Khalil Ahmad Khalil Ahmad ◽  
Habib ur Rehman Shah Habib ur Rehman Shah ◽  
Areeba Ashfaq Areeba Ashfaq ◽  
Muhammad Ashfaq Muhammad Ashfaq ◽  
Muhammad Kashif Muhammad Kashif ◽  
...  

In this study, In Vitro antibacterial and antifungal activities of azo series based on transition metal complexes (Cu2+, Zn2+, Mn2+, Co2+ and Ni2+) with already our reported ligands named as; [(E)-1-(1, 3-dioxolan-2-yl)-2-phenyldiazene] (K-1), [(E)-1-(1, 3-dioxolan-2-yl)-2-(4-methylphenyl)diazene] (K-2), 2-[(E)-phenyl diazenyl]-1H-benzimidazole] (K-3), [(E)-1-(1, 3-dioxolan-2-yl)-2-(4-ethylphenyl)diazene] (K-4), and [(E)-1-(1, 3-dioxolan-2-yl)-2-(2-methylphenyl)-diazene] (K-5) were studied. FTIR 1H-NMR and mass spectrometric techniques were applied for interpretation of synthesized complexes. 4.05-4.07 ppm chemical shift appearance of azo group confirms azo coupling with transition metal complexes. N=N, C-H, C-N and C-O groups are also confirmed by FTIR which exhibited peaks at 1400-1500, 2090-3090, 1100-1180, 1010-1060 and 625-780 cm-1. Furthermore, mass spectroscopic data also gives strong indication for the synthesis of metal complexes. All the newly synthesized complexes were screened for their antibacterial and antifungal activities. Antibacterial and antifungal activity against S. aureus, E.coli and A.niger, A.ustus and C.albican at conc. 250 and#181;g/ml showed excellent activity by K-1 complexes (Co2+, Cu2+, Ni2+), K-5 complexes (Zn2+, Mn2+, Cu2+), K-2 complexes (Co2+, Cu2+, Mn2+) and K-3 (Zn2+, Mn2+, Co2+, Cu2+) as compared to standard drug (Ampicillin). Hence, based on this study, it was concluded that these azo based complexes may act as a platform for designing more active antibacterial and antifungal agents.


2013 ◽  
Vol 2013 ◽  
pp. 1-7 ◽  
Author(s):  
Serkan Yavuz ◽  
Hilal Yıldırım

In the present study, some novel ferrocene derivatives carrying urea, thiourea, and sulfonamide groups were synthesized, and all compounds were characterized by spectral and elemental analyses. These compounds were screened for their antibacterial activities and also their minimum inhibitory concentration (MIC) against Gram-positive bacteria (Staphylococcus aureusandBacillus subtilis) and Gram-negative bacteria (Klebsiella pneumoniaandEscherichia coli) and antifungal activities againstSaccharomyces cerevisiaeandCandida albicans. Amongst the tested compounds,4b,4c,5b, and6bdisplayed excellent antimicrobial activity.


Author(s):  
Sarkar M.A. Kawsar ◽  
Khaleda Mymona ◽  
Refat Asma ◽  
Mohammad A. Manchur ◽  
Yasuhiro Koide ◽  
...  

This study was carried out to regioselective myristoylation of methyl α-D-glucopyranoside (1) using the direct acylation method gave the corresponding methyl 6-O-myristoyl-α-D-glucopyranoside (2) in fair yield. A number of 2,3,4-tri-O-acyl derivatives (3-15) of this 6-O-substitution product using a wide variety of acylating agents were also prepared in order to obtain newer derivatives of synthetic and biological importance. The reaction conditions are reasonably simple and yields were very good. The structures of the title compounds (2-15) were established by using analytical, physicochemical techniques and spectroscopic data (IR and 1H-NMR). All the synthesized compounds were employed as test chemicals for in vitro antimicrobial functionality test against Gram-positive Bacillus subtilis, Staphylococcus aureus, Gram-negative Escherichia coli, Pseudomonas aeruginosa bacteria and plant pathogenic fungi Aspergillus niger and Candida albicans. For comparative studies, antimicrobial activity of standard antibiotics, Ampicillin and Nystatin were also carried out against these microorganisms. The study revealed that the tested samples exhibited moderate to good antibacterial and antifungal activities. It was also observed that the test substances were more effective against fungal phytopathogens than those of the human bacterial strains. Encouragingly, a number of tested chemicals showed nearest antibacterial and antifungal activities with the standard antibiotics employed.


2014 ◽  
Vol 2014 ◽  
pp. 1-7 ◽  
Author(s):  
Namratha Bhandari ◽  
Santosh L. Gaonkar

The paper describes a convenient method for the preparation of 4-substituted phenyl-5-[1-(4-fluorophenyl)-1,3-dihydroisobenzofuran-5-yl]-2H-1,2,4-triazole-3-thiones. The structures of the synthesized compounds are established by the results of LCMS, 1H NMR, 13C NMR, and IR and elemental analyses. The mercaptotriazoles are indicated to be in thione form by 1H NMR spectra. All the synthesized compounds have been screened for antibacterial and antifungal activities. Compounds 12d and 12h exhibit encouraging results, while the remaining compounds show moderate activities. On the basis of spectral studies, formation of 2-amino-1,3,4-thiadiazoles from the isobenzofuran acyl thiosemicarbazides 11(a–h) is ruled out.


2012 ◽  
Vol 9 (1) ◽  
pp. 318-322 ◽  
Author(s):  
Bhikan J Khairnar ◽  
Rahul S. Salunke ◽  
Premchand B. Patil ◽  
Sanjay A . Patil ◽  
Rajeshwar J . Kapade ◽  
...  

A series of novel 3- methyl-7-substituted-4H,4-benzothiazine-2-carbohydrazide (3a-e) and corresponding thiosemicarbazides (4-a-q); 2-[3-methyl-7-substituted- 4H-1, 4-benzothiazine-2-yl]-N-(aryl) hydrazine carbothiamide have been synthesized. The thiosemicarbazide when cyclized with iodine via intramolecular cyclisation gave benzothiazonyl oxadiazoles (5-a-q); 5-(3-methyl -7-substitued-4H- 1,4-benzothiazin-2-yl)-N—aryl- 1,3,4- oxadiazol -2-amine and the compounds were tested for antibacterial and antifungal activities against different microorganisms.


2013 ◽  
Vol 2013 ◽  
pp. 1-7 ◽  
Author(s):  
Ghazala Yaqub ◽  
Abdul Hannan ◽  
Erum Akbar ◽  
Muhammad Usman ◽  
Almas Hamid ◽  
...  

Strategy to synthesize novel carbazole, that is, 2,3-dihydro-2-phenyl-6H-pyridazino[4, 5-b]carbazole-1,4-dione (2), is developed as key reaction. This novel compound showed ideal reactivity toward different functional groups like methyl, carboxylic, nitro, piperazine, and amine; thus series of its derivatives are synthesized sequentially with the aim to fuel up the carbazole compounds with new versatile derivatives. All compounds were investigated for their activity against bacteria (MRSA andS. typhi) and fungi (Candida albicans). Among tested compounds3,6, and8exhibited pronounced antibacterial activities while2,5, and9also showed moderate activities.2,3,5,7, and9showed stronger antifungal activity againstCandida albicanscomparable to positive control.


2008 ◽  
Vol 5 (1) ◽  
pp. 120-129 ◽  
Author(s):  
N. D. Argade ◽  
B. K. Kalrale ◽  
C. H. Gill

Disubstituted oxazol-5-one and pyrazoles are known to exhibit various biological activities. Therefore, in this work, we designed pyrazole containing 2,4-disubstituted oxazol-5-one(3a-g)as a new class of antimicrobial agents. Synthesis of titled compounds was carried out by two different methods. In the first method (conventional Method A), disubstituted oxazol-5-one(3a-g)was prepared by reacting 1-phenyl-3-p-tolyl-1H-pyrazole-4-carbaldehyde(1a-g)with hippuric acid(2)and sodium acetate, in an acetic anhydride for 2.5 - 4 h. In the second method (Method B), the above reaction was carried out under microwave assistance. Compared to the conventional method, the microwave-assisted synthesis of 3,4,5-trisubstituted imidazoles demonstrate several advantages, in terms of reaction time and overall yield. All the test compounds were evaluated forin vitroantibacterial and antifungal activities. In general, compounds with electron withdrawing groups showed good antibacterial and antifungal activities. Among the compound tested, compound(3d)showed highest activity.


Molecules ◽  
2021 ◽  
Vol 26 (15) ◽  
pp. 4391
Author(s):  
Lingling Xiao ◽  
Lu Yu ◽  
Pei Li ◽  
Jiyan Chi ◽  
Zhangfei Tang ◽  
...  

In this study, using the botanical active component thiochromanone as the lead compound, a total of 32 new thiochromanone derivatives containing a carboxamide moiety were designed and synthesized and their in vitro antibacterial activities against Xanthomonas oryzae pv. oryzae (Xoo), Xanthomonas oryzae pv. oryzicolaby (Xoc), and Xanthomonas axonopodis pv. citri (Xac) were determined, as well as their in vitro antifungal activities against Botryosphaeria dothidea (B. dothidea), Phomopsis sp., and Botrytis cinerea (B. cinerea). Bioassay results demonstrated that some of the target compounds exhibited moderate to good in vitro antibacterial and antifungal activities. In particular, compound 4e revealed excellent in vitro antibacterial activity against Xoo, Xoc, and Xac, and its EC50 values of 15, 19, and 23 μg/mL, respectively, were superior to those of Bismerthiazol and Thiodiazole copper. Meanwhile, compound 3b revealed moderate in vitro antifungal activity against B. dothidea at 50 μg/mL, and the inhibition rate reached 88%, which was even better than that of Pyrimethanil, however, lower than that of Carbendazim. To the best of our knowledge, this is the first report on the antibacterial and antifungal activities of this series of novel thiochromanone derivatives containing a carboxamide moiety.


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