Design, synthesis, and docking studies of novel ofloxacin analogues as antimicrobial agents

Selvaraj, Jubie; Prabitha, P.; Kumar, Rohitesh; Rajagopal, Kalirajan; Gayathri, R.; Sankar, S.; Elango, K

doi:10.1007/s00044-011-9655-8

Cited by 16 publications

(15 citation statements)

References 9 publications

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“…Antibiotic resistance is becoming a serious threat to public health and there is an urgent need for new and improved antimicrobial agents [1][2][3][4][5]. The occurrence of 1,2,4-triazole system in numerous biologically active molecules has been recognized to possess activities, such as analgesic [6], antibacterial [7][8][9], antifungal [10,11], anti-inflammatory [12], antitumor [13,14], antitrypanosomal [15], antiproliferative [16] and antibiotics properties [17].…”

Section: Introductionmentioning

confidence: 99%

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Synthesis and antibacterial activity of some new 1,2,4-triazole derivatives bearing carbohydrazide moiety

et al. 2020

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In this study, a series of 1,2,4-triazol-3-carbohydrazide derivatives and compound of 1,2,4-triazole-3-(4H)-thion have been synthesized. Structures and purity of the new compounds were confirmed by the use of their chromatographic and spectral data besides microanalysis. Four different bacterial stains for the study of the biological activity of compounds 6g, 7c, 7g and 7i; two Gram-positive strains, and two Gram-negative strains have been used. Compound 6g was found to be the most active of the four tested compounds against Pseudomonas aeruginosa, Bacillus cereus and Staphylococcus aureus, with an inhibition zone diameter of 16, 9, and 10 mm, respectively. Calculating the minimal inhibitory concentration value (MIC) for the positive drugs who formed an inhibition zone in the agar well diffusion method, we found that both compounds 6g and 7i were the most active of the four tested compounds against Pseudomonas aeruginosa and Bacillus cereus with an MIC value of 0.5 µg/mL for both bacteria. These results suggest that these two compounds could be considered as potential antibacterial agents against a range of bacteria.

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Section: Introductionmentioning

confidence: 99%

“…Methoxy-benzoic acid N'[2-(1,5-diethyl-1H-[1,2,4]triazole-3-yl)-acetyl]-hydrazide (8f): Color: Brown crystals. Yield: 80 %.…”

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confidence: 99%

Synthesis and antibacterial activity of some new 1,2,4-triazole derivatives bearing carbohydrazide moiety

et al. 2020

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“…An Indian research team (2012) designed and synthesized novel ofloxacin analogues 13 ( Figure 6 ) as antimicrobial agents. It was observed that 1,2,4-triazole derivatives of ofloxacin with MIC values ranging from 0.25 to 1 µg/mL had antibacterial properties against all tested Gram-positive ( S. aureus , S. epidermis , B. subtilis ) and one Gram-negative ( E. coli ) pathogens, which were comparable to ofloxacin (MICs: 0.25–1 µg/mL) [ 30 ].…”

Section: Antibacterial Activity Of Derivatives Of 124-triazolementioning

confidence: 99%

1,2,4-Triazoles as Important Antibacterial Agents

2021

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The global spread of drug resistance in bacteria requires new potent and safe antimicrobial agents. Compounds containing the 1,2,4-triazole ring in their structure are characterised by multidirectional biological activity. A large volume of research on triazole and their derivatives has been carried out, proving significant antibacterial activity of this heterocyclic core. This review is useful for further investigations on this scaffold to harness its optimum antibacterial potential. Moreover, rational design and development of the novel antibacterial agents incorporating 1,2,4-triazole can help in dealing with the escalating problems of microbial resistance.

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“…The SAR suggested that the hybrids bearing electron‐withdrawing groups at para ‐position in benzene ring favored the activity while electron‐donating groups were disfavored. Several 1,3,4‐oxadiazole‐5‐thione‐LVFX and 4‐amino‐1,2,4‐triazole‐3‐thione‐LVFX conjugates were examined for their in vitro activities against various pathogens, and most of them were as potent as or better than the parent LVFX against the tested Gram‐negative bacteria .…”

Section: Structure–activity Relationshipmentioning

confidence: 99%

4‐Quinolone Derivatives and Their Activities Against Gram‐negative Pathogens

Jiang

2018

Journal of Heterocyclic Chem

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Gram‐negative pathogens represent a significant global health threat, while the emergency and widespread of drug resistance make the situation even worse. As “privileged building blocks,” 4‐quinolones including fluoroquinolones are mainstays of chemotherapy against various bacterial infections. However, as other antibiotics, the resistance of Gram‐negative bacteria to 4‐quinolones develops rapidly and spreads widely throughout the world. To overcome the resistance and improve the potency, a number of 4‐quinolone derivatives were designed, synthesized, and screened for their in vitro and in vivo activities against representative Gram‐negative pathogens. This review aims to summarize the recent advances made towards the discovery of 4‐quinolone derivatives as anti‐Gram‐negative agents as well as their structure–activity relationship. The enriched structure–activity relationship paves the way to the further rational development of 4‐quinolones with excellent potency against both drug‐susceptible and drug‐resistant Gram‐negative pathogens.

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Design, synthesis, and docking studies of novel ofloxacin analogues as antimicrobial agents

Cited by 16 publications

References 9 publications

Synthesis and antibacterial activity of some new 1,2,4-triazole derivatives bearing carbohydrazide moiety

Synthesis and antibacterial activity of some new 1,2,4-triazole derivatives bearing carbohydrazide moiety

1,2,4-Triazoles as Important Antibacterial Agents

4‐Quinolone Derivatives and Their Activities Against Gram‐negative Pathogens

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