Antibacterial minimum inhibitory concentration

Table 2. Enzyme inhibitory constants (IC50) and antibacterial minimum inhibitory concentration (MIC) results for synergy with ceftriaxone of a series of bridged monobactams. 

Fig. 6.17 Structures of some quinolones, a broad family of synthetic chemotherapeutic antibacterials based on the 4-quinolone (a) and 1,8-naphthyiidine (b) structures. Norfloxacin and nalidixic acid, respectively, are examples of a drug from each of these groups. Qnoxacin is an example of a quinolone antibacterial based on cinnoUne, an aromatic heterocyclic with two attached six-mem-bered tings containing adjacent nitrogens at positions one and two (d). The basic fluoroquinolone pharmacophore is shown in (c). The addition of a fluorine atom at position six of the two-ring nucleus produced a 100-fold increase in the antibacterial minimum inhibitory concentration...

The microdilution method was employed for antibacterial and antifungal activity tests. Media were placed into each well of the 96 well-microplate. Extract solutions at 1,024 pg/ml were added into first raw of microplates and twofold dilutions of the compounds (512-0.25 pg/ml) were made by dispensing the solutions to the remaining wells. Ten microliters of culture suspensions were inoculated into all the wells. The sealed microplates were incubated at 35°C for 24 and 48 h in humid chamber. The lowest concentration of the extracts that completely inhibit macroscopic growth was determined and minimum inhibitory concentrations (MICs) were... 

Table 8.4 Antibacterial and antifungal activities of the LC extracts as minimum inhibitory concentrations (MICs)(ng/ml)... 

Fig. 2. Example of rough activity landscape. This figure shows the activity landscape for a series of related antibacterial compounds plotted in using the 2D BCUT descriptors to arrange the compounds. (A) Shows how the compounds are arrayed in a 2D representation of the chemistry space with the height of the marker being proportional to the minimum inhibitor concentration of the compounds [the smaller the minimum inhibitory concentration (MIC) the more potent the compound]. (B) This second panel presents the upper figure as a 2D figure to enhance the sharp cutoff between active and inactive compounds, emphasizing the point that activity landscapes are rarely smooth continuous functions.

Antibacterial activity. Essential oil, on agar plate, was active on Staphylococcus aureus and Streptococcus faecalis, minimum inhibitory concentration (MIC) 0.5 mg/mL,... 

Anti-amoebic activity. Ethanol (80%) extract of the dried rhizome was inactive on Entamoeba histolytica, minimum inhibitory concentration (MIC) greater than 1 mg/ mL The extract, administered intragas-trically to male hamsters at a dose of 800 mg/kg, was active vs experimentally induced hepatic amebiasis . A dose of 250 mg/kg, administered intragastrically to rats on days 1-5, produced weak activity and a dose of 500 mg/kg was active " ". Anti-atherosclerotic activity. Ethanol (50%) extract of the dried rhizome, administered intragastrically to male rabbits at a dose of 500 mg/kg, reduced atherogenic index from 4.7 to 1.2 on the aorta . Antibacterial activity. Decoction of the dried entire plant, on agar plate, was inactive on Proteus vulgaris, Staphylococcus aureus, and Staphylococcus epidermidis MIC 125 mg/mL. Bacillus subtilis, Bordetella... 

Structure—Activity Relationships. Biological evaluation of penicillins yields information such as in vitro and in vivo antibacterial activities, minimum inhibitory concentration (MIC), minimum bactericidal concentration (MBC), protective effectiveness in laboratory animals (PD50), and pharmacokinetic characteristics including efficiency of absorption, serum levels, tissue distribution, urinary excretion, recycling, etc. Penicillins are also tested for ability to resist inactivation by (S-lactamase produced by both gram-positive and gram-negative bacteria,... 

All four compounds were found to be most active against S. aureus and E. faecalis, with a minimum inhibitory concentration (MIC) of 0.5 pg/mL, followed by E. coli (2 pg/mL), K. pneumoniae (4 pg/mL), A. baumannii, and B. subtilis (8 pg/mL). P. mirabilis and P. aeruginosa were the most resistant bacteria against the compounds (16 and 32 pg/mL, respectively). Notably, antibacterial activity of the compounds was as potent as ampicillin (AMP) and oflaxocin (OFX) towards S. aureus and E. faecalis. These compounds also possessed quite remarkable antifungal activity against C. albicans, as much as ketocanozole (KET) (1 pg/mL). 

The dimaleate salt of 5,5-dimethyl-10-(4-methylpiperazino)-10,ll-dihydro-5H-dibenzo[b,/]silepin (45c) exhibited some antibacterial activity in vitro toward Mycobacterium tuberculosis H37Rv (minimum inhibitory concentration 12,5/igml ), Streptococcus -haemolyticus (25/igml ) and Staphylococcus pyogenes aureus (25/igml ) (76CCCC910). 

Table 7.11. MINIMUM INHIBITORY CONCENTRATIONS (.iiglml) OF A RANGE OF ANTIBACTERIAL COMPOUNDS AGAINST THE WILD TYPE (WT) PS. AERUGINOSA STRAIN AND A SENSITIVE MUTANT...

Table 8.9. IN VITRO ANTIBACTERIAL ACTIVITY OF 3,4-TRICYCLIC CEPHALOSPORINS [86] (MINIMUM INHIBITORY CONCENTRATION, iigim])...

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