1,4-Thioarialkylation and/or amination of E-3- [4-bromebenzoyl] acrylic acid and some studies with the products

Recently[1], it was reported that 3-[4-bromobenzoyl] acrylic acid has antibacterial activity towards Staphilococcus aureus, Escherichia coli and Kllebsiella, this was ascribed to the presence of the highly conjugated benzoylacrylic system, which may react with biologically essential-SH groups. This prompted us to investigate the behaviour of 3[4-bromobenzoyl] acrylic acid [1] towards compounds bearing the sulphhydryl group. Thus, when compound [1], was allowed to react with thiophenol and/or thioglycolic acid in dry benzene in the presence of few drops of piperidine is a catalyst[2], it afforded 2-phenyhmercapto-3-[4-bromobenzoyl] propionic acid, and 2-carboxymethyl mercapto-3-[4-bromobenzoyl] propionic acid [2 a and b], respectively. The structure of the acids 2 was proved from their infrared spectra, which show absorptions at 1674, 1683 cm[-1] [V[C=O] of ketone], 1700 and 1725 cm[-1] [V[c=o] of carboxylic acid] and broad basin peak centered at 3300 cm[-1]1 [V[OH] of acids] the electron impact fragmentation of compound 2a exhibits m/e =348[M[+]-18]. The [1]H-NMR spectrum of compound 2b in DMSO exhibits signals at 2.3 [S, 2H, S-CH[2]-COO], 3.1 [octet, 2H, C-CH[2]-] nonequivalent diasterotopic methylene protons, 4[quartet, -CH, methane proton], 7.7-7.9 [m, 4H, Ar-H], 12.79 [broad singlet, OH protons which disappear in D[2]O]

use of midazolam for attenuation of hypertensive response to endotracheal intubation in severe preeclampsia and its relation to neonatal condition at birth

The pressor response to intubation is known to be exaggerated in patients with severe preeclampsia. Twenty-Five women with severe preeclampsia who were scheduled to undergo caesarean section under general anesthesia were randomly assigned to either a midazolam pretreatment group [n = 15] and a control group [n = 10] who did not receive any antihypertensive therapy before the induction of anaesthesia. Patients in the mediazolam group received 0.1 mg kg[-1] intravenous midazolam 5 minutes before induction of anesthesia. Other control group received placebo intravenously. Blood pressure and heart rate were recorded at various time intervals. There was significant decrease in mean arterial blood pressure [MAP] after pretreatment with midazlam [P < 0.01]. The increase in MAP during laryngoscopy and intubation was significantly higher in the control group compared with midazolm; pretreatment group [P < 0.01]. During laryngoscopy and intubation; MAP is decreased by 5 mmHg in the midazolam pretreatment group while there was an increase of 18 mmHg in the control group. Heart rate is significantly increased in both groups during laryngoscopy and tracheal intubation [P <0.01], but the increase was higher in the midazolam group. The neonatal Apgar scores were similar in two groups

Therapeutic efficacy and tissue distribution of kitasamycin in normal and e coli-infected chickens

The therapeutic efficacy of kitasamycin following oral administration of 300 or 600 mg/kg. b. wt. for five successive days against experimental E.coli infection in broiler Hubbard chicken was studied. Effect on body weight gain and feed conversion from 3 weeks were of age till the end of 6 weeks also investigated. Moreover, tissue distribution of kitasamycin in normal and E.coli-infected chicks were recorded. Results achieved showed that administration of kitasamycin at the same time of infection, reduced morbidity, mortality and development of lesions more effectively than its administration after the appearance of symptoms in therapeutic or double the therapeutic doses. Kitasamycn improved significantly body weight gain and feed conversion, especially when given at the same time of E.coli infection. Kitasamycin [300 mg/kg. b. wt.] Was detected in serum of E.coli-infected chickens as early as 5 minutes and after 10 minutes in serum of normal birds following administration. It reached peak concentration one hour after administration and its level was slightly higher [7.4 +/- 0.78 micro g/ml] in serum of infected chickens versus normal birds [6.2 +/- 0.37 micro g/ml]. The concentration of the drug was high he in bile, ceacum, intestine, gizzard and lung than in muscles, fat and spleen. Kitasamycin could not be detected in brain at any interval following administration

Pharmacokinetics and bioavailability of gentamycin in goats

Gentamicin [2 mg/kg] was given both intravenously and intramuscularly to five healthy goats. Following intravenous injection, the blood concentration curve was biexponential. The dimination half- lives after both routes were similar i.e.2.30 +/- 0.11 and 2.47 +/- 0.12 hours. The apparent specific volume of distribution was 0.3 L/kg. The body clearance after i.v. administration was 1.61 +/- 0.04 ml/kg/min. the interval between doses was significantly different i.e. 7.57 +/- 2.08 and 12.59 +/- 0.62 hour after i.v. and i.m. injections, respectively. The bioavailability of gentamicin after i.m injection amounted to 88.12 +/- 3.36% with a maximum serum concentration [C[max]] of 4.20 +/- 0.18 micro g ml, about one hour after administration