Antibacterial Activity Testing

A strong antifungal activity against Aspergillus flavus, Penicillium notatum, Helminthosporium anomalum, and Fusarium oxysporum and antibacterial activity (tested on Bacillus subtilis and Klebsiella pneumoniae) were found for 2,3-dihydro-5-bcnzovl-l //-l. 3.2-bcnzodiazaphosphole 2-oxides 87 and 2-sulfides 88 (see Section 6.13.4.4) <2002HAC340>. 

Antibacterial activity testing. Determined using the broth microdilution method. Incubations were performed for 18 h using an Ominolog automated incubator (Biolog Inc. 21124 Cabot Boulevard, Hayward, CA 94545, USA). 

Other specific discovery assays have been used such as differential inhibition of a vancomycin resistant S. aureus strain and its susceptible parent, and an assay based on antagonism of the antibacterial activity by N,A/-diacetyl-L-Lys-D-Ala-D-Ala [24570-39-6] a tripeptide analogue of the dalbaheptides receptor. AppHcation of this latter test to 1936 cultures (90) led to the isolation of 42 dalbaheptides, six of which, including kibdelin (Table 3), parvodicin (Table 3), and actinoidin A2 (68) were novel. A colorimetric assay based on competition between horseradish peroxidase bound teicoplanin and the... 

Amino-2 -deoxypurines. 2 -AmiQo-2 -deoxyadenosine (15) is a naturally occurring A[-nucleoside isolated from A.ctinomadura that shows antknycoplasmal activity (1,4). Adenosine is the direct precursor for its biosynthesis (30). 2 -Arnino-2 -deoxyguanosine (16), isolated from a strain of Enterobacter cloacae (1,4), shows the growth of HeLa S3 cells and Sarcoma 180 in vivo and has been tested for antibacterial activity. 

Sulfaphenazole (684) and sulfazamet (685) are both examples of relatively short acting sulfonamides (B-80MI40406) and their antibacterial activity has been tested against Escherichia coli, the former being more effective than the latter. Sulfaphenazole also displaces sulfonyl ureas from protein binding sites on human serum albumin and consequently increases the concentration of the free (active) drug and produces a more intense reaction that may result in hypoglycemia. 

Tributyltin(IV) derivatives of six different pharmaceutically active carboxylates were synthesized and their antibacterial activities were tested using 10 different bacteria (B. cereus, C. diphtheria, E. C. ETEC, K. pneumonia, P. mirabilis, P. aeroginosa,... 

A number of tests have been deseribed which imitate, at least in part, the principle of the phenol eoeffieient test for liquid disinfectants. A culture of the test organism is mixed intimately with the semi-sohd preparation, and the mixture subcultuied by means of a loop into a suitable broth designed to disperse the base and neutrahze the antibacterial activity of the medicament. 

The antibacterial activity of the obtained 3H-pyrazoles 63a,b and 64 has been studied. They have been tested opposite a pathogenic bacterial stump and have shown antibacterial activity against the original Staphyloccocusaureus. The 3H-pyrazole 63b offers the strongest antibacterial activity [56]. 

Some representative examples of the new compounds were tested against a pathogenic bacterial strain and have shown activity against Staphylococcus aureus ATCC 25923. The benzodiazepin-2-one 69 offers the strongest antibacterial activity. The results are summarized in Table 8. 

The results of enzymatic and antibacterial assays demonstrated that compound 165 (as a racemic mixture) exhibits activities similar to those of the parent oxazoline L-159,692 [103]. In order to identify the enantioselectiv-ity of this compound, the corresponding R and S enantiomers were separately synthesized from (R)- or (S)-3-(4-methoxyphenyl)-5-hydroxymethyl-4,5-dihydroisoxazole (166) according to the method of Ukaji et al. [107,108] and tested for LpxC inhibitory and antibacterial activities [103]. Interestingly, only the S enantiomer of 166 exhibited strong enzyme inhibitory and antibacterial activity, while the R enantiomer of L-159,692 was the active component. The enantiomeric synthesis of compound 165 is depicted in Scheme 33. 

Compoimd 9 was tested for antibacterial activity and found to exhibit moderate antibacterial activity against E. coli at the does of 25 pg/ml. 

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... 

Hydrox5rpyranonate and hydroxypyridinonate complexes have been patented for the treatment of zinc deficiency (451) and are used in zinc supplements. Maltolate and ethylmaltolate complexes of zinc, copper, and tin have been included as essential constituents in patents for formulations for oral care (96). The arylmercury(II) complexes RHgL, where R = 4-XCgH4, X — Me, OMe, NO2, and L — malt, koj, have been tested for antibacterial activity (101). 

Twenty-five dibenzothiophenes, composed mainly of amino and acetamidodibenzothiophenes and their sulfoxides and sulfones, have been tested for antibacterial activity against Staphylococcus aureus, Escherichia coli, and Mycobacterium tuberculosis. Activity was found against the latter with 2- and 3-aminodibenzothiophene in synthetic culture media, but the effect was reversed by the addition of serum. " ... 

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