The 2-pyridone antibacterial agents: bacterial topoisomerase inhibitors

Synthesis, Biological Evaluation and 2D-QSAR Studies of Novel 6-Oxo-Pyridine-3-Carboxamide Derivatives as Antimicrobial and Antifungal Agents

“…Thus, the development of potent and effective antimicrobial agents is very important to overcome the emerging multi-drug resistance strains of bacteria and fungi. The 2-pyridone has proven to be effective antibacterial and antibacterial agents (Saiki et al, 1999;Li, Mitscher & Shen, 2000;Gupta & Plott, 2004;Khokhani, Khatri, & Patel, 2013;Tipparaju et al, 2008 andVyas et al, 2008) the clinical candidate, CG400549 (Yum et al, 2007& Park et al, 2007 and the promising lead compound, PT171 (Schiebel et al, 2014) were rationally designed as broad spectrum antibacterial agents, figure 1. Moreover, the 2-pyridone CG400549 (Figure 1) was identified as a potent antibacterial against multidrug-resistant staphylococci strains (Kim et al, 2005& Gerusz, 2010.…”

Design synthesis and antibacterial activity studies of new thiadiazoloquinolone compounds

“…Several new members of the quinolone family have emerged with enhanced activities such as grepafloxacin (3), levofloxacin (4), rufloxacin (5), and compounds 6-9 ( Figure 1). Much has been learned about how molecular modifications of the core quinolone structure affect the antibacterial profile.…”

“…Much has been learned about how molecular modifications of the core quinolone structure affect the antibacterial profile. The structure-activity relationship of the quinolones has been the subject of extensive reviews [4][5][6][7][8][9][10][11][12][13][14][15][16] . In our continuous effort to develop new chemotherapeutics with enhanced activities against resistant bacterial strains 17,18 , we introduced a new class of tricyclic compounds, namely thiadiazoloquinolones 19 .…”

“…In our continuous effort to develop new chemotherapeutics with enhanced activities against resistant bacterial strains 17,18 , we introduced a new class of tricyclic compounds, namely thiadiazoloquinolones 19 . In our methodology, we took advantage of many known benzothiadiazoles ( Figure 2) with diverse biopharmaceutical activities [20][21][22][23][24][25][26] and we hybridized the thiadiazole moiety with the fluoroquinolone structure to introduce the new compound 9-cyclopropyl-4-fluoro-6-oxo-6,9-dihydro [1,2,5]thiadiazolo [3,4-h]quinoline carboxylic acid (16). The latter compound was tested against several clinical isolate bacterial strains and did prove to be quite active compared to the drugs used in the market 19 .…”

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AbstractNew 9-(alkyl/aryl)-4-fluoro-6-oxo [1,2,5]thiadiazolo [3,4-h]quinoline-5-carboxylic acids and their esters were designed and synthesized. A detailed discussion of the reactions utilized in the preparation of the intermediate and target compounds is reported.

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