Synthesis of some novel analogues of 4-[l-pyrrolidinyl] piperidine and their effect on plasma glucose level

In the present study some compounds of 4-[1-Pyrrolidinyl] Piperidine [I] have been synthesized. Structures of compounds were confirmed by using HNMR, IR, Mass and UV spectrophotometer techniques. All the derivatives [II, III, IV and V] and the parent compound [I] at the dose of 100 mg/kg were evaluated for their effect on plasma glucose level. Compound [II] was the only derivative which showed effect on plasma glucose level

Synthesis and evaluation of novel phenacyl based carboxamide derivatives of piperidine as antihypertensive agents

The research in the field of piperidine has generally been related to the synthesis of useful medicinal drugs. In view of the pharmacological and medicinal importance of piperidine derivatives in different disciplines of medicines the present study has been carried out. A series of newly synthesized N-substituted phenacyl piperidine derivatives [II-VII and XIII-XIV] has been evaluated for hypotensive activity in normotensive anesthetized rats at the doses of 0.5 micro g/kg taking acetylcholine and noradrenaline [1 micro g/kg] as control. Mean arterial blood pressure and heart rate were compared to its respective control values obtained immediately before the administration of test compounds and expressed as percent change. The compounds II, III and XIV showed mild hypertensive activity while compound V, VII and XIII were found inactive at that dose level. However, compound IV showed more hypotensive effect than the starting molecule [I]. None of these derivatives affected the heart rate at the same dose. It was also revealed that the carboxamide group has no considerable effects on arterial blood pressure and plays no important role in the increase or decrease of blood pressure

Neurochemical estimations of some new quaternary phenacyl- bromopiperidinium compounds

Considering the fact that N-alkyl substituted quaternary ammonium salts of piperidinium bromide induce brain catecholamine and indoleamine metabolism, we thought it may he valuable to investigate the effects of three selected phenacyl derivatives [I, V and VIII] of piperidine on brain monoamines metabolism in mice [100mg/kg body weight] assuming that these derivatives might alter the brain indoleamine and catecholamine levels differently. Studies are carried out by using HPLC technique. It was found that compound VIII possessed greater neuroleptic activity as compared to compounds I and V

Antibacterial activity of 1-methyl-7-methoxy-B-carboline and its phenacyl and coumarine analogues

Antibacterial activity of 1-methyl-7-methoxy-pound]-carboline [harmaline] and its phenacyl and coumarine analogues 1-[3-nitro-phenyl]-[2-[7-Methoxy-1-methyl-1,3,4,9-tetrahydro-pound]-carbolin-2-yl]-ethanone[II], 1-[3,4-Dihydroxy-phe-nyl]-2-[7-methoxy-1-methyl-1,3,4,9-tetrahydro-pound]-carbolin-2-yl]-ethanone[III] 7-[methoxy-pound]-carboline],15-24, de-hydro[19,20-dimethoxy]coumarine [IV], 7-[methoxy-pound]-carboline]15-24,dehydro[20-methoxy]coumarine [V] were studied by disc diffusion method. All compounds were tested against three Gram positive and four Gram-negative bacteria. Parent compound showed good activity. All compounds revealed better results against Gram positive as compared to Gram-negative bacteria. 1-[3,4-dihydroxy-phenyl]-2-[7-methoxy-1-methyl-1,3,4,9-tetrahydro-pound]-carbolin-2-yl]-ethanone [III] was found most potent compound showing broad spectrum activity when compared with all synthesized analogues. Coumarine analogues showed more or less same activity indicating that number and position of methoxy groups are not important regarding antimicrobial activity

Effect of diazepam on the CNS excitation and behavioural changes induced by harmdline and its newly synthesized analogues

The neuropharmacologic profile of harmala alkaloids has been studied and found to have central effects like convulsions, catalepsy, or altered startle response. In number of studies the effects of diazepam, on harmaline and other beta carboline containing compounds-induced tremors were investigated. The present study was undertaken to examine the effect of diazepam on pretreated animals with harmaline and its synthesized phenacyl and coumarine analogues. Diazepam successfully inhibited the tremor and convulsions and attenuated the other behavioural response produced by Harmaline and its derivatives

New azaindole derivatives as analgesic agent

The indole class of analgesics continues to be exposed to the pharmaceutical community. The synthesis and analgesic properties of these agents have been the subject of ongoing investigations. During the course of present research, efforts were made to evaluate the possible analgesic activity of various quaternary ammonium salts of 7 - azaindole to see whether one more nitrogen in the indole nucleus also responsible for analgesic activity

Structure activity relationship of some new phenethylamine analogues

Discovery of L-dopa, isoprenaline, ephedrine and other catecholamines as effective therapeutic agents in cardiac and respiratory diseases initiated our interest to synthesize similar types of compounds possessing potentiating effect and lesser side effects and toxicity. The research, therefore carried out consisted of the synthesis, spectroscopic and biological studies of some new phenethylamine analogues. Some of these products exhibited significant cardiac activity on the heart of frog on the basis of which certain speculations were made regarding their structure activity relationships