The future of new oral antibiotics including the quinolones.

It is estimated that more than 110 million dollars'' worth of oral antibiotics will have been sold in Canada in 1987. In the next few years several new oral antimicrobial agents will reach the market, including beta-lactamase inhibitors, cephalosporins, monobactams, erythromycins and quinolones. Most of these new agents have a broader spectrum of antibacterial activity than the presently available oral antibiotics. A few have a longer half-life and can be administered once a day. The new oral drugs, especially the quinolones and possibly beta-lactams, will now be used to treat infections that in the past could be treated only parenterally. Exacerbations of pulmonary infections due to Pseudomonas aeruginosa in cystic fibrosis can now be successfully treated at home with the new quinolones. Osteomyelitis, arthritis, pneumonia and pyelonephritis will most likely be treated at home in the future. In severe infections patients will be admitted to hospital for short courses of parenteral therapy, followed by oral treatment. If used appropriately the new oral agents may lead to new approaches to the treatment of infectious diseases.     

Dihydropyrimidinones--a new class of anti-staphylococcal antibiotics

We report the synthesis and pharmacological evaluation of new derivatives of natural dipeptide antibiotic TAN-1057 A, B. In the course of this program, we identified novel analogues of the natural product that display similar antibacterial activity and showed improved tolerability.     

Canine blood groups. 1. Description of new erythrocyte specificities

Methods of production and characterization of immune typing reagents reactive with the erythrocytes of the dog are described. Five of the reagents (agglutinins) were reactive with previously unknown blood group factors and were shown by statistical and genetic tests on 222 random samples and 28 families to belong to 5 previously unrecognized blood group systems. The five new systems were one-blood factor, two-allele, three-genotype systems like the B, C, D and F systems. These were arbitrarily named J, K, L, M-and N.     

New sequences and new fungal producers of peptaibol antibiotics antiamoebins.

Mixtures of the microheterogeneous 16-mer peptaibol antibiotics called antiamoebins (AAM) have been isolated from the culture broths of strains of the filamentous fungi Stilbella erythrocephala ATCC 28144, Stilbella fimetaria CBS 548.84 and Gliocladium catenulatum CBS 511.66. Sequences were determined using on-line HPLC together with positive- and negative-ion electrospray ionization mass spectrometry. Some characteristic features are recognized in the mass spectrometric fragmentation pattern of AAM. From a sample originally used for sequencing AAM (from Hindustan Antibiotics, Ltd., Pimpri, Poona-411018, India), and a sample of AAM commercially available (from Sigma Chemicals, St. Louis, MO, USA) HPLC elution profiles and sequences were assigned. Further, sequences of AAM previously isolated from Emericellopsis synnematicola CBS 176.60 and Emericellopsis salmosynnemata CBS 382.62 were determined. The peptide designated AAM I was the most abundant in all isolates and its structure could be confirmed. AAM II was detectable as a minor component (1.9%) only in the original sample of AAM, but not in the other isolates. The structures of AAM III, IV and V, which had previously been partly assigned, were definitely established, and the new sequences AAM VI-XVI were elucidated. AAM showing Phe1/Leu1 or Phe1/Val1 exchange, respectively, are produced in amounts only by S. erythrocephala. Sequences, HPLC elution profiles ('fingerprints') and relative amounts of peptides of all isolates were correlated.