The therapeutic effect of ME1228, a new parenteral cephalosporin, was compared with that of broad-spectrum cephems in normal and neutropenic mice infected with various species of bacteria. The results showed that ME1228 was more active than were the other cephems against infections with various pathogens.

01 Mar 1991·Diagnostic Microbiology and Infectious DiseaseQ4 · MEDICINE

In vitro activity of an oxycephem OCP 9-176 compared with its sulfur analog and other β-lactams

Q4 · MEDICINE

Article

Author: Gu, Jian Wei ; Chin, Nai Xun ; Neu, Harold C.

OCP 9-176 is an oxycephem antibiotic that contains a 2-aminothiazolyl, carboxypropyl side chain at C-7 and a pyridinium thiomethyl group at C-3. OCP 9-176 was generally twofold less active than its sulfur-containing analog ME 1228 against Escherichia coli, Klebsiella pneumoniae, Klebsiella oxytoca, Providencia stuartii, Proteus vulgaris, and Serratia marcescens. Activity against Enterobacter cloacae and Citrobacter freundii was equivalent. OCP 9-176 was twofold less active than ME-1228 against Pseudomonas aeruginosa and Acinetobacter species. Activity of the two agents was similar against Staphylococcus aureus and Staphylococcus epidermidis. Although OCP 9-176 inhibited E. coli containing TEM-1 and TEM-2, it was less active than ME-1228. Klebsiella organisms with SHV-1 and K-2 beta-lactamases were inhibited, but TEM-3-containing isolates had MICs of 16 micrograms/ml. OCP 9-176 was minimally hydrolyzed by TEM-1, PSE-1, K-1, and P99, and it was a poor inhibitor of P99. Replacement of sulfur with oxygen does not increase the activity of compounds with sulfopyridinium methyl groups at C-3.

01 Jan 1990·The Journal of AntibioticsQ4 · MEDICINE

A new aminothiazolylcephalosporin having 1-carboxyethoxyimino group, ME1228.

Q4 · MEDICINE

Article

Author: Yasushi Murai ; Toshiaki Kudo ; Seiji Shibahara ; Shinichi Kondo ; Tsuneo Okonogi ; Shigeharu Inouye ; Takashi Yoshida

Aminothiazolylacetamidocephalosporins having 1-carboxyethoxyimino groups were synthesized and found to have excellent antibacterial activities including anti-pseudomonal activity and low toxicities. Among these cephalosporins, ME1228 having (S)-1-carboxyethoxyimino substituent and being combined with an (N-ethyl-4-pyridinio)thiomethyl group at C-3 showed marked therapeutic effects against systemic infections in mice and was selected as the best candidate for further evaluation.

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Indication	Highest Phase	Country/Location	Organization	Date
Bacterial Infections	Phase 2	-	Meiji Seika Pharma Co., Ltd.	-
Bacterial Infections	Phase 2	JP	Meiji Seika Kaisha Ltd.	-

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