scholarly journals Synthesis and Biological Screening of Novel 5-(5-Aryl-1-phenyl-1H-pyrazol-3-yl)-3-aryl-1,2,4-oxadiazole Derivatives

2021 ◽  
Vol 34 (1) ◽  
pp. 209-215
Author(s):  
Pravin S. Kulkarni ◽  
Swapnil R. Sarda ◽  
Amol U. Khandebharad ◽  
Mazahar Farooqui ◽  
Brijmohan R. Agrawal

A new series of 5-(5-aryl-1-phenyl-1H-pyrazol-3-yl)-3-aryl-1,2,4-oxadiazole (6a-o) have been synthesized by a cyclocondensation reaction of ethyl 5-(4-chlorophenyl)-1-phenyl-1H-pyrazole-3- carboxylate (3a-c) with aryl imidoxime (5a-e). The newly synthesized pyrazolyl-1,2,4-oxadiazole (6a-o) derivatives were characterized by spectroscopic techniques and screened for in vitro antibacterial activity against Bacillus subtilis (NCIM 2063), Staphylococcus albus (NCIM 2178), Escherichia coli (NCIM 2574), Proteus mirabilis (NCIM 2388) and in vitro antifungal activity against Aspergillus niger (ATCC 504) Candida albicans (NCIM 3100).

2020 ◽  
Vol 17 (2) ◽  
pp. 136-143
Author(s):  
Yan-Ling Tang ◽  
Yong-Kun Li ◽  
Min-Xin Li ◽  
Hui Gao ◽  
Xiao-Bi Yang ◽  
...  

Background: Infection is a global threat to human health, and there is an urgent need to develop new effective antibacterial drugs to treat bacterial infections. Objective: To study the antibacterial activity of piperazine substituted chalcone sulphonamides. Materials and Methods: A series of novel piperazine substituted chalcone sulphonamides have been prepared, and in vitro antibacterial activity against Staphylococcus aureus, Bacillus subtilis and Escherichia coli strains were evaluated. Results: The results showed that derivatives 6a, 6c and 6h displayed good antibacterial activity against Bacillus subtilis with MIC values of 4.0-8.0 mg/mL. Conclusion: Piperazine substituted chalcone sulphonamides may be used as potential antibacterial agents.


2022 ◽  
Author(s):  
Amna Kamal ◽  
Muhammad Adnan Iqbal ◽  
Haq Nawaz Bhatti ◽  
Abdul Ghaffar

Abstract N-heterocyclic carbene salts bearing alkyl substituents (1-8) and their selenium N-heterocyclic carbene adducts (9-12) were synthesized and characterized by elemental analysis, FT-IR, NMR (1HNMR, 13CNMR) spectroscopic techniques. All the adducts were found to be stable in air and moisture at room temperature. Compounds (5-12) were evaluated against Bacillus subtilis Macrococcus brunensis and Bacillus cereus in vitro. The biological assay revealed that antibacterial activity of Selenium-N-heterocyclic carbene adducts are comparatively better than the salts. MIC and inhibition zone values showed that Bacillus subtilis is more active to selenium adducts (9-12) than Macrococcus brunensis and Bacillus cereus whereas opposite in the salts (5-8). In vitro studies of hemolysis and thrombolysis demonstrated that the synthesized compounds are innocuous for pre-clinical trials to mouse blood.


2016 ◽  
Vol 6 (1) ◽  
Author(s):  
Abdulrahman Syedahamed Haja Hameed ◽  
Chandrasekaran Karthikeyan ◽  
Abdulazees Parveez Ahamed ◽  
Nooruddin Thajuddin ◽  
Naiyf S. Alharbi ◽  
...  

2020 ◽  
Vol 10 (6) ◽  
pp. 7329-7336

Our previous work involved the preparation and characterization of six quercetin derivatives, three of which were novel Schiff bases, while the fourth was a novel ionic salt of iodine. This study involved the investigation of the in vitro antioxidant activity against DPPH free radical as well as the in vitro antibacterial activity against Bacillus cereus, Salmonella spp., Escherichia coli and Staphylococcus aureus of quercetin and its 1-6 derivatives. The results revealed that all the studied quercetin derivatives had shown less antioxidant and antibacterial activity than quercetin itself, except that of compounds 3 and 4, which displayed an improvement in the antibacterial activity against Escherichia coli as compared to that of quercetin.


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