fluoroquinolone derivatives
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Author(s):  
NAWAZ MOHAMMED KHAN ◽  
PAWAN KUMAR ◽  
HEMANTH SUDHEER KUMAR K ◽  
BHARATH RATHNA KUMAR P

Objective: The present study envisages a series of oxadiazole fluoroquinolone derivatives that were synthesized (D1–D12) with added derivatives such as phenyl, aminophenyl, amino hydroxyphenyl along with cyclopropyl, ethyl, piperazine, and imidazole. Methods: All of the newly produced molecules were characterized by infrared, 1H nuclear magnetic resonance, mass spectrometry, and elemental analysis technique and screened for docking stimulation to find out binding modes of synthesized derivatives with 3FV5, 5IMW, and 5ESE and evaluated for in vitro antimicrobial activity. Results: From this study, it was found that the compound D8 showed good antibacterial activity against Gram-positive (Staphylococcus aureus), compound D9 showed good antibacterial activity against Gram-negative (Escherichia coli), and compound D3 showed good antifungal activity against fungi (Saccharomyces cerevisiae) in comparison with standard drugs (Ciprofloxacin and fluconazole). The zone of inhibition and minimum inhibitory concentration studies was performed on synthesized compounds. Conclusion: The analogs of oxadiazole flouroquinolone are suggested to be potent inhibitors with sufficient scope for further exploration.


2021 ◽  
Author(s):  
Luis Constantino ◽  
João Pais ◽  
Margarida Policarpo ◽  
David Pires ◽  
Bernard Testa ◽  
...  

Plant Direct ◽  
2021 ◽  
Vol 5 (9) ◽  
Author(s):  
Michael D. Wallace ◽  
Aleksandra W. Debowski ◽  
Kirill V. Sukhoverkov ◽  
Joshua S. Mylne ◽  
Keith A. Stubbs

2021 ◽  
Author(s):  
Michael D Wallace ◽  
Aleksandra W Debowski ◽  
Kirill V Sukhoverkov ◽  
Joshua S Mylne ◽  
Keith A Stubbs

Development of herbicides with novel modes of action are crucial for weed control and to hinder herbicide resistance. An attractive novel herbicidal target is plant DNA gyrase, which has been demonstrated to be effectively inhibited by the known antimicrobial ciprofloxacin. Despite this good herbicidal activity ciprofloxacin is not suitable as a herbicide due to its antimicrobial activity, therefore, a diverse library of analogues was analysed to gain insight into the aspects required for herbicidal activity. This analysis revealed significant structural modifications were tolerated and that the fluoride at C-6 and a cyclic amino group at C-7 were not crucial for herbicidal activity. The analysis also revealed that these modifications also affected the antibacterial activity with one compound demonstrating good herbicidal activity and weak antibacterial activity, against both Gram-positive and Gram-negative bacteria.


2021 ◽  
Vol 6 (10) ◽  
pp. 2483-2491
Author(s):  
Aasia Shaheen ◽  
Uzma Ashiq ◽  
Rifat Ara Jamal ◽  
Khalid Mohammed Khan ◽  
Sana Gul ◽  
...  

2021 ◽  
Vol 4 ◽  
pp. 100044
Author(s):  
Rajat Goyal ◽  
Archana Sharma ◽  
Vijay Kumar Thakur ◽  
Monika Ola ◽  
Prabodh Chander Sharma

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