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The structure-activity relationships of nine products of the acrylophenone family have been studied. In a previous report 2-(4-methyl-1-piperazinylmethyl)acrylophenone was shown to be an antimicrotubular drug. The effects of these drugs on the bovine brain tubulin polymerization were determined by a turbidimetric assay. The median inhibitory concentrations (ID50) ranged from 1.5 X 10(-5) to 5 X 10(-5) mol/l. Their action on the inhibition of 3H-colchicine binding to tubulin was determined by DEAE (diethylaminoethyl)cellulose filter assay. These compounds are weak inhibitors of colchicine binding. Pharmacological studies of these drugs revealed a strong inhibition of the human ADP-induced platelet aggregation. Moreover, they markedly decreased the serum cholesterol, triglycerides and phospholipids levels of rats after injection of Triton WR 1339 (4-(1,1,3,3-tetramethylbutyl)phenol polymer with formaldehyde and oxirane). They inhibited Candida albicans, Penicillium notatum and Aspergillus versicolor growth. Thus, these nine compounds possess interesting pharmacological properties which are very likely to be related to the acrylic moiety of the molecules.

The activity of metronidazole combined with ofloxacin was investigated by the checkerboard method in liquid medium against 60 obligate anaerobes. The bacteriostatic effect of the combination was assessed by calculating the FIC index. Two metronidazole resistant strains of Propionibacterium acnes (MIC greater than 32 mg/l) were inhibited by 0.125 mg/l of this former antibiotic in presence of an ofloxacin concentration equal to half the value of the MIC. On the 58 other anaerobic strains, the combination of metronidazole plus ofloxacin had an additive bacteriostatic effect (30 strains) or a synergistic effect (26 strains). No antagonism was noted with any strain. For selected anaerobic or mixed infections the combination of metronidazole and ofloxacin may be useful. Killing curves demonstrated that, under good anaerobic conditions, metronidazole acted rapidly against Bacteroides fragilis. At a concentration of 8 mg/l, a decrease of log10 of the population was observed after 2 hours. After a contact ranging from 1 to 8 hours, depending of the investigated strains, a bactericidal effect was observed with metronidazole.

Minimal inhibitory concentrations of 105 anaerobic Gram negative bacilli were determined by two-fold dilution in Wilkins - Chalgren agar following the reference method proposed by Sutter et al. No resistance was observed with thienamycin, which is especially active against the Bacteroides fragilis group (MIC 50 = 0.125 mg/l). Among the beta-lactams investigated, cefoxitin and moxalactam proved more active than ceftizoxime and ceftriaxone, while cefotiam exhibited poor activity. While most Fusobacteria were susceptible to studied beta-lactams, some Fusobacterium varium demonstrated resistance to cephalosporins and cephamycins .

The in vitro activity of imipenem, a new penem antibiotic, was determined against 210 clinical Gram-positive anaerobic isolates and compared with the activities of metronidazole, clindamycin, cefoxitin, moxalactam, ceftizoxime, ceftriaxone and cefotiam. All investigated strains were inhibited by a 4-mg/l concentration of imipenem. Cefoxitin demonstrated good activity against most strains with exception of some Clostridium difficile and Clostridium ramosum strains. Cephalosporins were classed in decreasing activity order as follows: cefoxitin moxalactam ceftriaxone ceftizoxime cefotiam. Metronidazole had better activity against Clostridium spp. than against non-sporulated bacilli. Clindamycin resistance rates were superior to 10% for most groups, with the exception of Clostridium perfringens. Actinomyces and Bifidobacterium. Imipenem was the most potent inhibitor, as 81% and 95% of tested strains were inhibited at concentrations of 0.25 and 0.5 mg/l respectively.