Reference

a-Amino-3-halo-cephem compounds

a-Amino-3-halo-cephem compounds. Matsumoto, Kunio; Suzuki, Kazuhiro; Yaso, Masao; Kabari, Sadami; Kuramoto, Masashi; Fujii, Tadashiro (Toyo Jozo Co., Ltd., Japan). Japan. Kokai JP 53038693 8 Apr 1978 Showa, 10 pp. (Japanese). (Japan). CODEN: JKXXAF. CLASS: IC: C12D009-04. APPLICATION: JP 76-112080 18 Sep 1976. DOCUMENT TYPE: Patent CA Section: 16 (Fermentations) a-Amino-3-halo-cephem compds. are produced by reaction of 7-amino-3-halo-3-cephem-4-carboxylic acid and an a-amino-deriv., catalyzed by an acylase. For example, 7-(D-phenylglycylamido)-3-chloro-3-cephem-4-carboxylic acid (I) [53994-73-3] was produced by reacting 1.4 g 7-amino-3-chloro-3-cephem-4-carboxylic acid and 4.7 g Me D-phenylglycine-HCl in 280 mL 0.1 M acetate buffer (pH 6.0) contg. a cell suspension of Achromobacter B-402-2 at 37° for 3 h. The reaction filtrate was subjected to column chromatog. on Diaion HP-20 to sep. 1.3 g cryst. I.

Use of a heavy inoculum in the in vitro evaluation of the anti-staphylococcal activity of 19 cephalosporins

Use of a heavy inoculum in the in vitro evaluation of the anti-staphylococcal activity of 19 cephalosporins. Laverdiere, Michel; Welter, Diane; Sabath, L. D. (Dep. Med., Univ. Minnesota Med. Sch., Minneapolis, Minn., USA). Antimicrob. Agents Chemother., 13(4), 669-75 (English) 1978. CODEN: AMACCQ. ISSN: 0066-4804. DOCUMENT TYPE: Journal CA Section: 3 (Biochemical Interactions) The in vitro activity of 19 cephalosporins against 105 clin. isolates of Staphylococcus aureus and S. epidermidis was detd. by using a heavy inoculum, i.e., 108-109 organisms/mL, to maximally challenge the antibiotics. The antistaphylococcal activities of cephaloridine [50-59-9] and 87/312 Na [61618-29-9] were consistently decreased by the use of a heavy inoculum when compared with the activity obtained with 2 less-concd. inocula. The activity of most of the other compds. was also decreased with the use of a heavy inoculum, but this was obsd. only with selected isolates. Cephapirin [21593-23-7], cephalothin [153-61-7], and cefazaflur [52123-49-6] were the most active drugs against the methicillin-susceptible isolates. Cephaloridine, cefamandole [34444-01-4], cefazaflur, and 87/312 had substantial activity against methicillin-resistant staphylococci even with heavy inocula. With the exception of cefaclor [53994-73-3] against S. aureus, the orally absorbed cephalosporins were generally 6.25-50% as active as the parenterally administered cephalosporins. The median minimal inhibitory concns. of 5 of the 12 parenteral cephalosporins were lower with the methicillin-susceptible S. aureus than with the methicillin-susceptible S. epidermidis strains.