PRELIMINARY MICROBIOLOGICAL AND PHARMACOLOGICAL EVALUATION OF 6-(R-a-AMINO-3-THIENYLACETAMIDO) PENICILLANIC ACID (BL-P 875)

β-Lactam Antibiotics: Their Physicochemical Properties and Biological Activities in Relation to Structure

“…p-Aminobenzylpenicillin (169) has a spectrum similar to that of penicillin N. The ortho-and meta-aminobenzylpenicillins (8,9) have spectra similar to that of the para-isomer toward Gram-positive bacteria, but they are sIightIy less active against the Gram-negative organisms. Other amino group-containing penicillins, such as cyclacillin (WY-4508) (209) and BL-P875 (210), are also excellent broad spectrum penicillins but may be similarly sensitive to penicillinase. It is effective against infections of the gastrointestinal, respiratory, and urinary tracts due to Staphylococci, Streptococci, Haemophilus injluenzae, Proteus mirabilis, Neisseria gonorrhoeae, certain strains of Escherichia coli, and some species of Salmonella, Shigella, and Moraxella.…”

7-[α-(1-Methyl-4-Pyridinothio)-Acetamido] Cephalosporanic Acid

“…The drug concentrations in the blood of normal male Swiss-Webster mice, averaging 20 g in weight, were determined by periodic orbital sinus bleedings after oral, intramuscular, and subcutaneous drug administration. The technique for blood collection and bioassay was identical to that previously described by Price et al (2), except that Sarcinia lutea ATCC 9341 was employed as the assay organism. Differences in average drug concentrations in the blood were analyzed by means of Student's T test.…”

SYNTHESES AND ANTIBACTERIAL ACTIVITIES OF PENICILLINS FROM (+)- AND (-)-a-AMINO- 4-ISOTHIAZOLYLACETIC ACIDS

“…-Bromo-4-isothiazolylacetic acid (2) was obtained in good yield by bromination of methyl 4-isothiazolylacetate** with N-bromosuccinimide, followed by acid hydrolysis of the bromo ester (Scheme 1). The amino acid 3…”