Antibacterial activated carbons

Oya, A., Yoshida, S., Abe, Y., Iizuka, T. and Makiyama, N., Antibacterial activated carbon fiber derived from phenolic resin containing silver nitrate, Carbon, 1993, 31(1), 71 73. 

Oya, A., Wakahara, T, andYoshida, S., Preparation of pitch-based antibacterial activated carbon fiber, Carbon, 1993, 31(8), 1243 1247. 

Oya, A., Yoshida, S, Alcafliz-Monge, J. and Linares-Solano, A., Preparation and properties of an antibacterial activated carbon fiber containing mesopores, Carbon, 1996, 34(1), 53 57. 

Oya, A., Kimura, M., Sugo, T., et al. (1994). Antibacterial activated carbon fiber derived from methyl methacrylate-grafted phenolic resin fiber. Carbon, 32, 107-10. 

Interposition of a methylene group between the phenyl ring and the heterocycle leads to the benzyldiami nopyrimidines, a class of compounds notable for their antibacterial activity. Condensation of hydrocinnamate 54 with ethyl formate leads to the hydroxymethylene derivative 55. In this case, too, the heterocyclic ring is formed by reaction with guanidine. This sequence probably involves initial addition-elimination to the forniyl carbon to form 56 cyclization in this case involves simple amide formation. Tautomerization then affords the hydroxy derivative 57. This is converted to tetroxoprim (58) by first... 

Chlorhexidine base is not readily soluble in water therefore the freely soluble salts, acetate, gluconate and hydrochloride, are used in formulation. Chlorhexidine exhibits the greatest antibacterial activity at pH 7-8 where it exists exclusively as a di-cation. The cationic nature of the compound results in activity being reduced by anionic compounds including soap and many anions due to the formation of insoluble salts. Anions to be wary of include bicarbonate, borate, carbonate, chloride, citrate and phosphate with due attention being paid to the presence of hard water. Deionized or distilled water should preferably be used for dilution purposes. Reduction in activity will also occur in the presence of blood, pus and other organic matter. 

More recently, screening efforts at Novartis have identified a hydroxamic acid containing a benzothiazinone ring system (32) [108]. This inhibitor is very potent versus S. aureus Ni -PDF (<5nM) and displays good selectivity versus matrix metalloprotease-2 (MMP-2) and MMP-13. Unfortunately (32), and all other analogues prepared, such as carbon isosteres (33), sulfones (34), N-substituted analogues (35) and N-formyl-N-hydroxylamines (36), lacked appreciable antibacterial activity in spite of their potent enzyme inhibitory activity. Further studies performed by Novartis suggest that these molecules are unable to penetrate the outer cell membrane of E. coli, and may bind to the cell membrane of S. aureus [108]. 

It is of interest that antibacterial activity can be retained even when the imine carbon-nitrogen bond is replaced by a carbon to carbon double bond. Base-catalyzed condensation of 5-nitrofurfuraldehyde (24) with 2,6-dimethylpyridine (38) affords olefin 39. Treatment of this compound with hydrogen peroxide gives the corresponding N-oxide (40). Heating of... 

The long-chain fatty acids (containing mainly 16 or 18 carbon atoms) have antibacterial activity. 

Sulfanilamides, 1, 145 carbonic anhydrase inhibition by, 1, 173 Sulfaphenazole antibacterial activity, 5, 291 Sulfapyridine, 1, 161 as antibacterial, 2, 517 veterinary use, 1, 209 Sulfaquinoxaline coccidiostat veterinary use, 1, 212 Sulfasomidine, 3, 151 Sulfasomizole... 

---