[Structure-activity relationship of cephalosporins. III. Effect of sulfur-containing functional groups on the biological activity of cephalosporins--derivatives of 7-aminocephalosporanic acid].
The relationship between the in vitro antimicrobial activity of cephalosporin antibiotics and the presence and space arrangement of sulfur-containing descriptors of the radical at position 7 in the cefem nucleus was studied. It was noted that the sulfur-containing fragments were markedly less frequent in the structures of the known cephalosporins than the nitrogen- and oxygen-containing descriptors. It was concluded that at present information related only to two of the fragments under investigation might be used as characteristics in predicting antimicrobial activity of cephalosporins by the pattern recognition. On the basis of the studies there were defined two principle paths for synthesis of new antibiotics: introduction into the molecule structure of the functional groups providing with high probability improvement of the antimicrobial properties and preparation of compounds containing descriptors whose impact on the biological activity is not known.
Grabarnik
M S
MS
Iakhkind
M I
MI
Znamenskiĭ
Iu V
IuV
Kocherezhko
N A
NA
D002511:Cephalosporins / Q000737:chemistry / Q000494:pharmacology*; D004353:Drug Evaluation, Preclinical; D004352:Drug Resistance, Microbial; D004926:Escherichia coli / Q000187:drug effects*; D066298:In Vitro Techniques; D008826:Microbial Sensitivity Tests; D011550:Pseudomonas aeruginosa / Q000187:drug effects*; D013211:Staphylococcus aureus / Q000187:drug effects*; D013455:Sulfur / Q000737:chemistry / Q000494:pharmacology*
D002511:Cephalosporins; D013455:Sulfur
Sviaz' struktura-aktivnost' tsefalosporinovykh antibiotikov. III. Vliianie serosoderzhashchikh funktsional'nykh grupp na aktivnost' tsefalosporinov-proizvodnykh 7-aminotsefalosporanovoĭ kisloty.