Analgesic activity of alkyl piperidine derivatives

Piperidine is the most significant scaffold which reveals therapeutic potential because of its conformationally flexible nature. During the course of present investigations synthetic quaternary salts of alkyl piperidine with various phenacyl bromides were explored for their possible analgesic activity. Compounds I analogs [1a-1f] and compound II analogs [IIa-IIf] showed varying degree of analgesic activity when compared with pethidine as standard and its duration by tail immersion method

Antimicrobial and antioxidant screening of N'-substituted sulphonyl and benzoyl derivatives of 4-Pyridine carboxylic acid hydrazide

In this research program, the antibacterial, antifungal and antioxidant activities of six N_-substituted sulfonyl and benzoyl derivatives of lead molecule PCH were reported. Out of these compounds, sulphonyl derivatives 2,3 and benzoyl derivative 5 showed moderate to good activity against different strains of gram-positive and gram-negative bacteria including B. cereus, B. subtilis, B. thruingiensis and S. pyogenes, S. fecalis and E. coli ATCC 8739. Moreover, upon antifungal screening, the compound, N?-[[2,4,6-trimethylbenzene] sulfonyl]pyridine-4-carbohydrazide possessed good antifungal activity against Candida species, a causative agent of systemic fungal infections. Antioxidant study demonstrated more than 50% inhibition in DPPH assay for sulphonyl derivative 2 indicating its potential as antioxidant while the other derivatives expressed low level of radical scavenging property

Synthesis of novel derivatives of 4-Pyridine carboxylic acid hydrazide and their activity on central nervous system

Six novel derivatives [2-7] of 4-Pyridine carboxylic acid hydrazide [PCH] were synthesized by treating this lead molecule with substituted arylsulphonyl and benzoyl chlorides

The molecular structures of the newly derived products were characterized by the help of UV Visible, IR, FAB, 1HNMR spectroscopy and CHN analysis

During the preliminary pharmacological screening, it was observed that the synthesized compounds induced noticeable changes on motor activity of the animals

Interesting structure activity relationship was also observed among the synthesized molecules. Because of the interesting affect on motor activity, the newly synthesized derivatives can further be evaluated for their effects on CNS

Synthesis and cytotoxic activity of some derivatives of alkyl piperidine

Synthesis of novel phenacyl derivatives of alkyl piperidine as cytotoxic agents via simple and single step reaction procedure is going to be reported here. Twelve new compounds were successfully synthesized in moderate yield and in solid form. Their synthesis was confirmed by TLC, melting point, CHN analysis and through different spectral studies such as UV, IR, Mass and proton NMR. The advantages of this synthetic route are simple operation, mild reaction conditions and good yields. These newly synthesized derivatives were extensively explored for their cytotoxicity by brine shrimp lethality assay

Behavioral and neurochemical profile of some novel phenacyl based isonipecotamide derivatives

Study of natural products led to the development of new molecules of potential biological activity. Piperidine nucleus constitutes one of the components of various alkaloids and drugs. During the course of our project regarding the synthesis of derivatives of piperidine carboxamide to study the effects of these compounds as anti-depressive agents, some of the compounds exhibited significant effects at all three doses, through open field activity thus establishing a direct relationship between dose and locomotion. Moreover, these compounds have also shown the decreased level of 5-HT alone with increased level of dopamine as an indication of their antagonism towards 5-HT receptor

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