Design, synthesis and molecular modeling studies on novel moxifloxacin derivatives as potential antibacterial and antituberculosis agents

Türe, Aslı; Kulabaş, Necla; Dingiş, Serap İpek; Birgül, Kaan; Bozdeveci, Arif; Karaoğlu, Şengül Alpay; Krishna, Vagolu Siva; Sriram, Dharmarajan; Küçükgüzel, İlkay

doi:10.1016/j.bioorg.2019.102965

Cited by 20 publications

(14 citation statements)

References 42 publications

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“…Nevertheless, Gorityala et al [ 56 ] reported that ciprofloxacin potency against P. aeruginosa were superior compared to moxifloxacin. This pattern was also noticed in results published by Türe et al and Garza et al, [ 28 , 50 ].…”

Section: Fq’s Antibacterial Biological Activitysupporting

confidence: 87%

“…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%

“…Following scientific reports in the literature, levofloxacin exhibited superior antibacterial activity against Gram-positive S. epidermis strains [ 51 , 55 , 63 ] and moxifloxacin is generally the most potent amongst FQs a, gainst Gram-positive and negative bacteria [ 26 ]. Moxifloxacin was the latent agent against the food poisoning pathogen L. monocytogenes ATCC 43251 (MIC < 1.370 µM [ 28 ]) when compared with other FQs as ciprofloxacin (MIC 3.954 µM−12.072 [ 28 , 64 ]) and norfloxacin (MIC < 8.267 µM [ 28 ]).…”

Section: Fq’s Antibacterial Biological Activitymentioning

confidence: 99%

“…It is noticeable that ciprofloxacin has potential antibacterial activity against Gram-negative bacteria as P. aeruginosa and E. coli . [ 28 , 48 ]. Moreover, ciprofloxacin had prospective growth inhibitory activity against H. pylori NCTC 11916 and 12 more H. pylori clinical isolates as reported by Abu-Sini et al [ 72 ].…”

Section: Fq’s Antibacterial Biological Activitymentioning

confidence: 99%

“…However, a wide range in ciprofloxacin MIC against E. coli ATCC 25922 is perturbing as MIC reported ranged from 0.002 µM [ 24 ]−61.869 µM [ 49 ] in different publications. This fluctuation in ciprofloxacin antibacterial activities may explain the current abundant application of levofloxacin and moxifloxacin as positive standards by medicinal chemists when designing and synthesizing novel FQs analogues [ 24 , 28 , 53 , 54 , 55 , 68 , 69 , 70 , 73 , 74 , 75 ].…”

Section: Fq’s Antibacterial Biological Activitymentioning

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 Activitysupporting

confidence: 87%

Section: Fq’s Antibacterial Biological Activitymentioning

confidence: 99%

Section: Fq’s Antibacterial Biological Activitymentioning

confidence: 99%

Section: Fq’s Antibacterial Biological Activitymentioning

confidence: 99%

Section: Fq’s Antibacterial Biological Activitymentioning

confidence: 99%

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Fluoroquinolones’ Biological Activities against Laboratory Microbes and Cancer Cell Lines

2022

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Novel fluoroquinolones containing 2‐arylamino‐2‐oxoethyl fragment: Design, synthesis, evaluation of antibacterial and antituberculosis activities and molecular modeling studies

Kulabaş

Türe

Bozdeveci

et al. 2022

Journal of Heterocyclic Chem

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Novel substituted fluoroquinolone derivatives, compounds 6-20 were designed, synthesized, and evaluated for antituberculosis and antibacterial activity. Antibacterial activities of the compounds were determined and compound 14 was found to be the most potent antimicrobial agent owing to minimal inhibitory concentration (MIC) value of <1.16 μg/μl for all tested bacteria. Further, compounds were tested in vitro for their antimycobacterial activity against Mycobacterium tuberculosis H37Rv. Most of the compounds showed antimycobacterial effects with 1.56-25.00 μg/ml MIC values. Compounds 14 and 18 were found to be the most active derivatives due to their MIC at 1.56 μg/ml. Selected compounds 11, 14, 17, and 18 were tested for M. tuberculosis DNA supercoiling assay and they had IC 50 values within a range of 6.35-15 μM. Mechanism of binding to DNA gyrase enzymes was evaluated using in silico molecular modeling studies and it was shown that compounds 6-20 adopt a similar binding mode as already known for fluoroquinolone drugs.

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Design, synthesis, and anticancer activity of novel 4-thiazolidinone-phenylaminopyrimidine hybrids

et al. 2020

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Design, synthesis and molecular modeling studies on novel moxifloxacin derivatives as potential antibacterial and antituberculosis agents

Cited by 20 publications

References 42 publications

Fluoroquinolones’ Biological Activities against Laboratory Microbes and Cancer Cell Lines

Fluoroquinolones’ Biological Activities against Laboratory Microbes and Cancer Cell Lines

Novel fluoroquinolones containing 2‐arylamino‐2‐oxoethyl fragment: Design, synthesis, evaluation of antibacterial and antituberculosis activities and molecular modeling studies

Design, synthesis, and anticancer activity of novel 4-thiazolidinone-phenylaminopyrimidine hybrids

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