The novel 1-(2-fluorovinyl)-4-quinolone-3-carboxylic acid derivatives Z-15a − c, E-15a − c, Z-16a − c, and E-16a − c, conformationally restricted analogues of fleroxacin (5), were synthesized, and ...their in vitro antibacterial activity was evaluated. A dehydrosulfenylation of a 2-fluoro-2-(4-methoxyphenyl)sulfinylethyl group was employed as a key step for the construction of a 2-fluorovinyl group at the N-1 position. It appeared evident that the Z-isomers Z-15a − c and Z-16a − c exhibited 2- to 32-fold more potent in vitro antibacterial activity than the corresponding E-isomers E-15a − c and E- 16a − c. Furthermore, since Z-15b showed in vitro antibacterial activity and DNA gyrase inhibition comparable to that of 5, it was hypothesized that the conformation of Z-15b would be equivalent to the active conformer of 5. The results revealed that the antibacterial Z-1-(2-fluorovinyl)quinolone derivatives carry the novel N-1 substituent of the fluoroquinolones.
Novel 1-trifluoromethyl-4-quinolone derivatives (8a,b) were synthesized, and the antibacterial activity of each was evaluated. An oxidative desulfurization−fluorination reaction was employed to ...introduce a trifluoromethyl group at the N-1 position as a key step. Among the derivatives, 8a was found to exhibit antibacterial activity comparable to that of norfloxacin (1) against Staphylococcus aureus Smith, Streptococcus pneumoniae IID1210, and Escherichia coli NIHJ JC-2.
As an aim toward developing new antiulcer agents, new N-substituted N'-3-3-(piperidinomethyl)phenoxypropylureas were synthesized and evaluated for histamine H2-receptor antagonistic, gastric ...antisecretory, and gastric mucosal protective activities. A QSAR study showed that the most favorable N-substituents were electron-donating straight-chain alkyl groups of short length such as ethyl group from the viewpoint of dual action, i.e., gastric antisecretory and mucosal protective actions. Among the ureas studied, compounds 4, 5, and 8-10 were selected as candidates for further study.
The antibacterial activity of the extracts prepared from 181 species (75 families) of tropical and subtropical plants was screened against various types of pathogenic bacteria. Among the 505 extracts ...tested, 53 of them inhibited the growth of methicillin-resistant Staphylococcus aureus (MRSA). The active extracts obtained from barks of Shorea hemsleyana and roots of Cyphostemma bainessi were separated to their components, some of which greatly reduced the viable cell number of MRSA. These active compounds were all identified as stilbene derivatives. Hemsleyanol d, one of the stilbene tetramer isolated from S. hemsleyana, was the most effective compound and had MIC of 2 μg/ml.
Extracts of Garcinia mangostana (Guttiferae) showing inhibitory effects against the growth of S. aureus NIHJ 209p were fractionated according to guidance obtained from bioassay and some of the ...components with activity against methicillin‐resistant Staphylococcus aureus (MRSA) were characterized.
One active isolate, α‐mangostin, a xanthone derivative, had a minimum inhibitory concentration (MIC) of 1.57−12.5 μg mL−1. Other related xanthones were also examined to determine their anti‐MRSA activity. Rubraxanthone, which was isolated from Garcinia dioica and has a structure similar to that of α‐mangostin, had the highest activity against staphylococcal strains (MIC = 0.31−1.25 μg mL−1), an activity which was greater than that of the antibiotic vancomycin (3.13−6.25 μg mL−1). The inhibitory effect against strains of MRSA of two of the compounds when used in conjunction with other antibiotics was also studied. The anti‐MRSA activity of α‐mangostin was clearly increased by the presence of vancomycin; this behaviour was not observed for rubraxanthone.
The strong in‐vitro antibacterial activity of xanthone derivatives against both methicillin‐resistant and methicillin‐sensitive Staphylococcus aureus suggests the compounds might find wide pharmaceutical use.
From the aerial parts of
Pepermia obtusifolia, five phenolic compounds bearing a methyl, an isoprenyl and a geranyl group on a benzene ring core have been isolated. The structures were determined by ...the spectroscopic analysis including 2D NMR techniques and synthesis.
Benzophenone derivatives, garcinol (1) and isogarcinol (2) isolated from the pericarps of Garcinia purpurea (Guttiferae), and xanthochymol (3) and a mixture of isoxanthochymol (4) cycloxanthochymol ...(5) from the pericarps of G. subelliptica were evaluated for their antibacterial activity against methicillin-resistant Staphylococcus aureus. Among them, 3 showed the lowest minimum inhibitory concentration at 3.1-12.5μg/ml. This concentration is nearly equal to that of the antibiotic, vancomycin.
We performed a randomized study to evaluate the differences between upper midline incision and transverse incision for gastrectomy.
Patients undergoing distal gastrectomy or total gastrectomy for ...gastric cancer were randomly allocated to have either an upper midline incision or a transverse incision. The times taken to open and close the abdominal cavity, the number of doses of postoperative analgesics, and the incidence of postoperative pneumonia, wound infection, and intestinal obstruction were compared between the patients having the two incisions.
Times for both opening and closing the abdominal cavity were longer with a transverse incision, in both the distal gastrectomy group and total gastrectomy group. In the patients in whom continuous epidural analgesia was used postoperatively, the number of additional doses of analgesics was smaller in the transverse-incision group after distal gastrectomy. The incidence of postoperative pneumonia was lower in the transverse-incision group after distal gastrectomy. The number of patients with postoperative intestinal obstruction was smaller in the transverse-incision group than in the midline-incision group after distal gastrectomy. In contrast to distal gastrectomy, there was no significant difference in the number of doses of postoperative analgesics, incidence of postoperative pneumonia, or incidence of postoperative intestinal obstruction between the two study groups after total gastrectomy.
A transverse incision for distal gastrectomy may be more beneficial than an upper midline incision in attenuating postoperative wound pain, decreasing the incidence of postoperative pneumonia, and preventing postoperative intestinal obstruction.
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