Synthesis of some new fluorene-amino acid derivatives of expected biological activity

The synthesis of fluorenone [and 7-nitrofluorenone]-4-carboxamido acids [3a-4e], their methyl esters [5a-6e] and their corresponding hydrazino hydrazide derivatives [7a-8e] was described. In addition, some dipeptide analogues in the form of their methyl esters [9a-10c] and hydrazides [11a-12c] were synthesized. Most of the synthesized nitro derivatives were found to possess an interesting antimicrobial activities against number of microorganisms

Characterization of the adrenergic activity of arbutamine, a novel agent for pharmacological stress testing

Arbutamine is a novel catecholamine designed to be used as a diagnostic agent in patients with coronary artery diseases. The activity of this agent in anesthetized dogs was studied and its interactions with adrenoceptors in vitro were characterized. Arbutamine, 12.5, 25 and 50 ng/kg/min intravenous infusion, significantly increased the left ventricular pressure, cardiac output [CO], and the heart rate [HR]. It also reduced the total peripheral vascular resistance [TPVR]. These effects were compared to those produced by isoproterenol [ISO] and dobutamine [DOB] infused in doses of 3.75, 7.5 and 15 ng/kg/min and 2, 4 and 8 Ug/kg, respectively. The affinity constant [KA] of arbutamine and ISO for cardiac B1-adrenoceptors as determined by competition binding assays was found to be 7.32 and 6.04, respectively. In guinea pig trachea precontracted with histamine, arbutamine and ISO produced a concentration dependent relaxation. Arbutamine contracted isolated rate aortic rings with maximal activity that of norepinephrine [NE]. The interactions of arbutamine and ISO with the atypical B- adrenoceptors [B3] in rat white adipocytes, arbutamine simulated glycerol release were also studied. The order of potency of the agents tested is BRL-37344 > arbutamine > ISO; while in hamster brown adipocytes, the order is arbutamine > ISO > BRL-37344

Comparative study of the effects of natural honey and antacid [aluminium phosphate] on the anti-inflammatory and ulcerogenic activity of indomethacin

The effects of concurrent administration of either honey of aluminium phosphate with indomethacin on the anti-inflammatory activity, ulcerogenic activity and plasma level of indomethacin in rats were investigated in this study. Natural honey [3 mg/kg orally] caused a significant decrease of ulcerogenic activity of indomethacin [30 mg/kg orally] as indicated by the gross lesion score and hitopathological examination This effect induced by honey is comparable to that produced by colloidal aluminium phosphate [3 gm/kg orally] also honey caused a marked decrease of indomethacin-induced gastric acid secretion that was not significantly different from that produced by aluminium phosphate Both indomethacin-honey and indomethacin-aluminium phosphate combinations caused a decrease of anti-inflammatory activity and plasma level of indomethacin but the reduction produced by the first combination was found to be significantly less than that produced by the second combination. These data may justify the use of honey concurrently with indomethacin to suppress its deleterious effect on the gastric mucosa with less disturbance of its plasma level and anti-inflammatory activity than its concomitant use with antacid