THE STRUCTURAL MODIFICATION CAUSES THE ENHANCEMENT OF ANALGESIC ACTIVITY OF 4-(4′ CHLORO –PHENYL)-4- HYDROXY PIPERIDINE

Objective- The outstanding  position of piperidine analogues  has proven them an important core in the structures of pharmaceutically active molecules, naturally occurring alkaloids, pharmaceuticals and as synthetic intermediates with interesting biological, physical and pharmacological behaviors. The  piperidine ring containing compound like pethidine having strong opiod analgesic activity, more potent than codein and controls the pain of smooth muscle spasm. Because of having similarity in structure the present study was aimed to estimate the analgesic activity of synthesized derivatives of 4-(4′-Chlorophenyl)-4-hydroxy piperidine.Method- The present study was conducted in animal model, mice by using Pethidine as standard drug. For which the Eddy's hot plate method was adopted and analgesia ( mean increase in latency)  was observed.Result- The result showed the more prominent response of substituted compound than the parent one 4-(4′-Chlorophenyl)-4-hydroxy piperidine†and it was studied that alteration in the molecule structure is accountable for  a better analgesic response.Conclusion- The studies proved the positive pharmacological responsiveness of the combination of 4-(4′-Chlorophenyl)-4-hydroxy piperidine with phencyl halides. These synthesized derivatives will establish as potent analgesics.KEY WORDS:AlkaloidsOpiodAnalgesicPiperidin

Synthesis and cytotoxic activity of some derivatives of alkyl piperidine

Abstract: 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

Tyrosinase inhibition: conformational analysis based studies on molecular dynamics calculations of bipiperidine based inhibitors.

Two series of variably N-substituted biperidines were synthesized by condensing various acid chlorides, alkyl halides and anhydrides with 1,4-bipiperidine. The new compounds were tested as tyrosinase inhibitors and a structure-activity relationship (SAR) study was carried out. Potent inhibition was observed in the case of the 4'-methylbenzyl substitution on this atom (IC50 = 1.72 microM) with this compound being a lead for future drug design. Additionally, calculations of the important QSAR molecular descriptors were done on the biperidine analogues after their 2 ps molecular dynamics (MD) simulations using molecular mechanics force field (MMFF) approaches. Using MD simulations potential and total energies were calculated for the energy minimized models of bipiperidine and the most active analogs 2, 3, 4, 6, 8 and 10