K. Gerzon
1970
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Journal
Annual Reports in Medicinal Chemistry
Abstract
Publisher Summary This chapter describes the various aspects of antibiotics and related compounds. The clinical investigation of new antimicrobial agents constitutes a challenge demanding broad knowledge of antibiotic action in the management of the patient with infectious disease. The study of soil and stool samples obtained from drug-free, antibiotic-virgin communities revealed the presence of E. coli strains harboring R factors, which mediate resistance to tetracycycline and streptomycin, ampicillin and chloramphenicol. The mannosidostreptomycin, a biologically active analog, is not adenylated by a kinase capable of inactivating streptomycin. Adenosine, as well as the C-nucleoside formycin, is a competitive inhibitor of ATP that serves as phosphate donor in the inactivation of kanamycin by a phosphorylase of P. aeruginosa. The growth of 50 different strains of Neisseria meningitidis in vitro was found to be inhibited by rifampin in the concentrations of 1 μg/ ml or less and subsequently the antibiotic was shown to be uniquely effective in the eradication of these meningococci from asymptomatic carriers. A potentially predictive relationship between the sum of molar attraction constants, indicative of the relative degree of drug–receptor interaction, and observed in vivo antibacterial activities appears to exist for a group of substituted α-phenoxy-6-acyla-midopenicillanic acids.