A novel tricyclic β-lactam exhibiting potent antibacterial activities against carbapenem-resistant Enterobacterales: Synthesis and structure-activity-relationships

2021 ◽  
pp. 116343
Author(s):  
Jun Sato ◽  
Hiroki Kusano ◽  
Toshiaki Aoki ◽  
Satoru Shibuya ◽  
Katsuki Yokoo ◽  
...  
Keyword(s):  
Antibacterial Activities ◽  
Structure Activity Relationships ◽  
Carbapenem Resistant ◽  
Structure Activity

scholarly journals Antibacterial activities and structure–activity relationships of a panel of 48 compounds from Kenyan plants against multidrug resistant phenotypes

SpringerPlus ◽  
2016 ◽  
Vol 5 (1) ◽  
Author(s):  
Leonidah K. Omosa ◽  
Jacob O. Midiwo ◽  
Armelle T. Mbaveng ◽  
Simplice B. Tankeo ◽  
Jackson A. Seukep ◽  
...  
Keyword(s):  
Antibacterial Activities ◽  
Multidrug Resistant ◽  
Structure Activity Relationships ◽  
Structure Activity

scholarly journals Structure-activity relationships of 3-substituted-5,5- diphenylhydantoins as potential antiproliferative and antimicrobial agents

2011 ◽  
Vol 76 (12) ◽  
pp. 1597-1606 ◽  
Author(s):  
Nemanja Trisovic ◽  
Bojan Bozic ◽  
Ana Obradovic ◽  
Olgica Stefanovic ◽  
Snezana Markovic ◽  
...  
Keyword(s):  
Escherichia Coli ◽  
Staphylococcus Aureus ◽  
Antimicrobial Agents ◽  
Human Colon ◽  
Antibacterial Activities ◽  
E Coli ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
Almost All

A series of twelve 3-substituted-5,5-diphenylhydantoins was synthesized, including some whose anticonvulsant activities have already been reported in the literature. Their antiproliferative activities against HCT-116 human colon carcinoma cells were evaluated to determine structure-activity relationships. Almost all of the compounds exhibited statistically significant antiproliferative effects at a concentration of 100 ?M, while the derivative bearing a benzyl group was active even at lower concentrations. Moreover, their in vitro antibacterial activities against Escherichia coli ATCC 25922, Staphylococcus aureus ATCC 25923 and clinical isolates of Escherichia coli, Proteus mirabilis, Pseudomonas aeruginosa, Enterococcus faecalis and Staphylococcus aureus were evaluated. Only the 3-iso-propyl and 3-benzyl derivatives showed weak antibacterial activities against the Gram-positive bacterium E. faecalis and the Gram-negative bacteria E. coli ATCC 25922 and E. coli.

scholarly journals Antimycobacterial Activities of Novel 5-(1H-1,2,3-Triazolyl)Methyl Oxazolidinones

2012 ◽  
Vol 2012 ◽  
pp. 1-7 ◽  
Author(s):  
Oludotun Adebayo Phillips ◽  
Edet Ekpenyong Udo ◽  
Reny Varghese
Keyword(s):  
Mycobacterium Tuberculosis ◽  
Vero Cells ◽  
Antibacterial Activities ◽  
Mice Model ◽  
Active Compounds ◽  
Structure Activity Relationships ◽  
Structure Activity

The antibacterial activities of a series of triazolyl oxazolidinones againstMycobacterium tuberculosisstrainin vitroandin vivoin a mice model are presented. Most active compounds were noncytotoxic against VERO cells with acceptable selectivity indexes (SI) as measures of compound tolerability. Structure activity relationships (SARs) revealed that analogs with alkylcarbonyl (IC90: < 0.2 to 0.422 μg/mL) and arylcarbonyl (IC90: < 0.2 to 2.103 μg/mL) groups at the piperazine 4N-position-displayed potent antimycobacterium activities, comparable to the methanesulfonyl (IC90: < 0.2 μg/mL) analog, linezolid (IC90: < 0.2 μg/mL), and isoniazid (IC90: < 0.034 μg/mL). The furanylcarbonyl derivative also displayed potent activity, while the arylsulfonyl analogs were inactive. Of the triazolyl oxazolidinones, the morpholino (PH-27) derivative with medium bioavailability in plasma was most activein vivo, but relatively less efficacious than isoniazid.

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