Synthesis and antibacterial activity of novel [1,2,4]triazolo[3,4-h][1,8]naphthyridine-7-carboxylic acid derivatives

Gao, Liuzhou; Xie, Yu; Li, Tao; Huang, Wenlong; Hu, Guoqiang

doi:10.1016/j.cclet.2014.09.017

Cited by 22 publications

(5 citation statements)

References 10 publications

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“…As reported, norfloxacin was used as a positive control in the pipeline publications, including norfloxacin derivatives synthesis. Norfloxacin MIC against Gram-positive is presented in Table 3 [ 1 , 23 , 24 , 26 , 28 , 34 , 35 , 36 , 37 , 38 , 39 , 40 , 41 , 42 , 43 , 44 , 45 , 46 , 47 , 48 , 49 , 50 , 51 , 52 , 53 , 54 , 55 , 56 , 57 , 58 , 59 , 60 , 61 , 62 , 63 , 64 , 65 , 66 , 67 , 68 , 69 , 70 , 71 ]. In brief, norfloxacin inhibitory activity against a panel of Gram-positive bacteria regardless of the strain varied relatively.…”

Section: Fq’s Antibacterial Biological Activitymentioning

confidence: 99%

“…In brief, norfloxacin inhibitory activity against a panel of Gram-positive bacteria regardless of the strain varied relatively. For example, norfloxacin in vitro antibacterial activity reported by Mentese 0.800 [66] 146.978 [49] 1.509 [48] ATCC 29213 0.400 [66] 1.509 [48] 0.082 [67] 1.509 [60,61] 0.296 [50] 0.680 [51] 0.755 [55] ATCC 25923 0.755 [64] 2.960 [57] 0.010 [52] 0.755 [26] 0.368 [46] 3.954 [28] 3.018 [62] Healthcare-acquired MRSA NRS70 0.604 [50] Community-acquired MRSAUSA300 19.014 [50] (MRSA) ATCC 33591…”

Section: Fq's Antibacterial Activity Against Gram-positive Bacteriamentioning

confidence: 99%

“…1.509 [60,61] 0.755 [55] 0.680 [51] MRSA ATCC 33592 ≤0.083 [56] NCDC 110 150.901 [42] 12.072 [47] 0.589 [49] 0.377 [24] As illustrated in Table 3, ciprofloxacin was the most commonly adopted reference by the cited researchers against different Gram positive and negative bacterial stains, ciprofloxacin MIC against Gram-positive bacteria including B. cereus spp. ranged from 0.181 µM [46]-3.954 µM [28], S. aureus ATCC 6538 (ranged from 1.509 µM [48]−146.978 µM) [49], S. aureus ATCC 29213 (MIC ranged from 0.082 µM [67]−1.509 µM [48]), and S. aureus ATCC 25923 (MIC ranged from 0.010 [52] µM −3.954 µM [28]). Remarkably, ciprofloxacin MIC varied within similar bacterial species, one example is S. epidermidis species, according to Liu et al, strain MSSE 12-1 of S. epidermidis species was susceptible to ciprofloxacin (MIC 0.755 µM) [26], whereas it showed very limited activity against MSSE14-2 strain (MIC > 386.308 µM) [53,54].…”

Section: Fq's Antibacterial Activity Against Gram-positive Bacteriamentioning

confidence: 99%

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Fluoroquinolones’ Biological Activities against Laboratory Microbes and Cancer Cell Lines

2022

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Development of novel derivatives to rein in and fight bacteria have never been more demanding, as microbial resistance strains are alarmingly increasing. A multitude of new fluoroquinolones derivatives with an improved spectrum of activity and/or enhanced pharmacokinetics parameters have been widely explored. Reporting novel antimicrobial agents entails comparing their potential activity to their parent drugs; hence, parent fluoroquinolones have been used in research as positive controls. Given that these fluoroquinolones possess variable activities according to their generation, it is necessary to include parent compounds and market available antibiotics of the same class when investigating antimicrobial activity. Herein, we provide a detailed guide on the in vitro biological activity of fluoroquinolones based on experimental results published in the last years. This work permits researchers to compare and analyze potential fluoroquinolones as positive control agents and to evaluate changes occurring in their activities. More importantly, the selection of fluoroquinolones as positive controls by medicinal chemists when investigating novel FQs analogs must be correlated to the laboratory pathogen inquest for reliable results.

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Section: Fq’s Antibacterial Biological Activitymentioning

confidence: 99%

Section: Fq's Antibacterial Activity Against Gram-positive Bacteriamentioning

confidence: 99%

Section: Fq's Antibacterial Activity Against Gram-positive Bacteriamentioning

confidence: 99%

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Fluoroquinolones’ Biological Activities against Laboratory Microbes and Cancer Cell Lines

2022

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“…Triazole-fused fluoroquinolones 33 with a functional Mannich-base moiety at the C-8 position ( Fig. 6 ) exhibited considerable antibacterial activities [ 53 ]. Nalidixic acid based 1,2,4-triazolo[3,4- b ] [ 1 , 3 , 4 ]thiadiazole derivatives 34 were evaluated for their antimicrobial activity against two Gram-positive bacteria ( S. aureus and Bacillus subtilis ), three Gram-negative bacteria ( P. aeruginosa , E. coli and K. pneumoniae ) and two fungi ( A. niger and F. oxysporum ) by Aggarwal et al.…”

Section: Biological Activities Of 124-triazole Derivativesmentioning

confidence: 99%

An insight on medicinal attributes of 1,2,4-triazoles

Aggarwal

Sumran²

2020

European Journal of Medicinal Chemistry

197

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The present review aims to summarize the pharmacological profile of 1,2,4-triazole, one of the emerging privileged scaffold, as antifungal, antibacterial, anticancer, anticonvulsant, antituberculosis, antiviral, antiparasitic, analgesic and anti-inflammatory agents, etc. along with structure-activity relationship. The comprehensive compilation of work carried out in the last decade on 1,2,4-triazole nucleus will provide inevitable scope for researchers for the advancement of novel potential drug candidates having better efficacy and selectivity.

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“…Compounds derived from aliphatic amines were less potent than those derived from heterocyclic amine donors. In particular, 2-methylpiperazine compound 12h was highly active against MDR E. coli bacterial strain with MIC value of 0.25 µg/mL, about 30-fold more potent than ciprofloxacin [ 29 ].…”

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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Synthesis and antibacterial activity of novel [1,2,4]triazolo[3,4-h][1,8]naphthyridine-7-carboxylic acid derivatives

Cited by 22 publications

References 10 publications

Fluoroquinolones’ Biological Activities against Laboratory Microbes and Cancer Cell Lines

Fluoroquinolones’ Biological Activities against Laboratory Microbes and Cancer Cell Lines

An insight on medicinal attributes of 1,2,4-triazoles

1,2,4-Triazoles as Important Antibacterial Agents

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