The Experts below are selected from a list of 210 Experts worldwide ranked by ideXlab platform
E Neokosmidis - One of the best experts on this subject based on the ideXlab platform.
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formal synthesis of the Piperidine Alkaloid prosophylline using polymer supported dihydro 2h pyridin 3 one
Tetrahedron Letters, 2007Co-Authors: Elias A Couladouros, Alexandros T Strongilos, E NeokosmidisAbstract:Abstract The use of polymer-supported 2,6-disubstituted-dihydro-2 H -pyridin-3-one, as the ‘polymorphic’ core molecule for the formal synthesis of the Piperidine Alkaloid (±)-prosophylline is presented.
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Formal synthesis of the Piperidine Alkaloid (±)-prosophylline using polymer-supported dihydro-2H-pyridin-3-one
Tetrahedron Letters, 2007Co-Authors: Elias A Couladouros, Alexandros T Strongilos, E NeokosmidisAbstract:Abstract The use of polymer-supported 2,6-disubstituted-dihydro-2 H -pyridin-3-one, as the ‘polymorphic’ core molecule for the formal synthesis of the Piperidine Alkaloid (±)-prosophylline is presented.
Abimael D Rodriguez - One of the best experts on this subject based on the ideXlab platform.
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neopetrosiamine a biologically active bis Piperidine Alkaloid from the caribbean sea sponge neopetrosia proxima
ChemInform, 2011Co-Authors: Karinel Nieves, Abimael D RodriguezAbstract:Neopetrosiamine A (I) displays strong in vitro activities against a panel of cancer cell lines.
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neopetrosiamine a biologically active bis Piperidine Alkaloid from the caribbean sea sponge neopetrosia proxima
Bioorganic & Medicinal Chemistry Letters, 2010Co-Authors: Karinel Nieves, Abimael D RodriguezAbstract:Abstract A new tetracyclic bis-Piperidine Alkaloid, neopetrosiamine A (1), has been extracted from the marine sponge Neopetrosia proxima collected off the west coast of Puerto Rico. The structure of compound 1 was elucidated by analysis of spectroscopic data coupled with careful comparisons of its 1H and 13C NMR data with those of a well-known 3-alkylbis-Piperidine Alkaloid model. The new Alkaloid displayed strong in vitro cytotoxic activity against a panel of cancer cell lines as well as in vitro inhibitory activity against the pathogenic microbes Mycobacterium tuberculosis and Plasmodium falciparum.
Elias A Couladouros - One of the best experts on this subject based on the ideXlab platform.
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formal synthesis of the Piperidine Alkaloid prosophylline using polymer supported dihydro 2h pyridin 3 one
Tetrahedron Letters, 2007Co-Authors: Elias A Couladouros, Alexandros T Strongilos, E NeokosmidisAbstract:Abstract The use of polymer-supported 2,6-disubstituted-dihydro-2 H -pyridin-3-one, as the ‘polymorphic’ core molecule for the formal synthesis of the Piperidine Alkaloid (±)-prosophylline is presented.
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Formal synthesis of the Piperidine Alkaloid (±)-prosophylline using polymer-supported dihydro-2H-pyridin-3-one
Tetrahedron Letters, 2007Co-Authors: Elias A Couladouros, Alexandros T Strongilos, E NeokosmidisAbstract:Abstract The use of polymer-supported 2,6-disubstituted-dihydro-2 H -pyridin-3-one, as the ‘polymorphic’ core molecule for the formal synthesis of the Piperidine Alkaloid (±)-prosophylline is presented.
K E Panter - One of the best experts on this subject based on the ideXlab platform.
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fetal muscle type nicotinic acetylcholine receptor activation in te 671 cells and inhibition of fetal movement in a day 40 pregnant goat model by optical isomers of the Piperidine Alkaloid coniine
Journal of Pharmacology and Experimental Therapeutics, 2013Co-Authors: Benedict T Green, Kevin D Welch, James A Pfister, K E PanterAbstract:Coniine is an optically active toxic Piperidine Alkaloid and nicotinic acetylcholine receptor (nAChR) agonist found in poison hemlock ( Conium maculatum L. ). Coniine teratogenicity is hypothesized to be attributable to the binding, activation, and prolonged desensitization of fetal muscle-type nAChR, which results in the complete inhibition of fetal movement. However, pharmacological evidence of coniine actions at fetal muscle-type nAChR is lacking. The present study compared (−)-coniine, (+)-coniine, and nicotine for the ability to inhibit fetal movement in a day 40 pregnant goat model and in TE-671 cells that express fetal muscle-type nAChR. Furthermore, α-conotoxins (CTx) EI and GI were used to antagonize the actions of (+)- and (−)-coniine in TE-671 cells. (−)-Coniine was more effective at eliciting electrical changes in TE-671 cells and inhibiting fetal movement than was (+)-coniine, suggesting stereoselectivity by the receptor. The pyridine Alkaloid nicotine did not inhibit fetal movement in a day 40 pregnant goat model, suggesting agonist specificity for the inhibition of fetal movement. Low concentrations of both CTxs potentiated the TE-671 cell response and higher concentrations of CTx EI, and GI antagonized the actions of both coniine enantiomers demonstrating concentration-dependent coagonism and selective antagonism. These results provide pharmacological evidence that the Piperidine Alkaloid coniine is acting at fetal muscle-type nAChR in a concentration-dependent manner.
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actions of Piperidine Alkaloid teratogens at fetal nicotinic acetylcholine receptors
Neurotoxicology and Teratology, 2010Co-Authors: Benedict T Green, K E Panter, Kevin D Welch, Daniel Cook, James A PfisterAbstract:Abstract Teratogenic Alkaloids are found in many species of plants including Conium maculatum L., Nicotiana glauca, Nicotiana tabaccum, and multiple Lupinus spp. Fetal musculoskeletal defects produced by Alkaloids from these plants include arthrogyropisis, scoliosis, torticollis, kyposis, lordosis, and cleft palate. A pharmacodynamic comparison of the Alkaloids ammodendrine, anabasine, anabaseine, anagyrine, and coniine in SH-SY5Y cells and TE-671 cells was made. These Alkaloids and their enantiomers were more effective in depolarizing TE-671 cells which express the human fetal-muscle type nicotinic acetylcholine receptor (nAChR) relative to SH-SY5Y cells which predominately express autonomic nAChRs. The rank order of potency in TE-671 cells was: anabaseine > (+)-anabasine > (−)-anabasine > (±)-anabasine > anagyrine > (−)-coniine > (±)-coniine > (+)-coniine > (±)-ammodendrine > (+)-ammodendrine. The rank order potency in SH-SY5Y cells was: anabaseine > (+)-anabasine > (−)-coniine > (+)-coniine > (+)-ammodendrine > anagyrine > (−)-anabasine > (±)-coniine > (±)-anabasine > (−)-ammodendrine. The actions of these Alkaloids at nAChRs in both cell lines could be distinguished by their maximum effects in depolarizing cell membrane potential. The teratogenic action of these compounds may be related to their ability to activate and subsequently desensitize nAChRs.
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quinolizidine and Piperidine Alkaloid teratogens from poisonous plants and their mechanism of action in animals
Veterinary Clinics of North America-food Animal Practice, 1993Co-Authors: K E Panter, Richard F KeelerAbstract:Quinolizidine and Piperidine Alkaloid teratogens from Lupinus,Conium, and Nicotiana genera have been identified as causes ofbirth defects in livestock induced by poisonous plants. Manydefects now known to be related to poisonous plant ingestionwere once thought to have a genetic origin. This suppositiondelayed diagnosis, reporting, and understanding of such birthdefects, because breeders and producers feared the news wouldmake it difficult to sell breeding stock. Defects caused by quinolizidineand Piperidine teratogens include cleft palate andcontracture-type skeletal defects such as arthrogryposis, scoliosis,torticollis, and kyphosis. Teratogens have been identified,differences in susceptibility to teratogenic compounds amonglivestock species have been elucidated, periods of gestation whenspecific types of birth defects occur have been determined, andinformation about mechanism of action has been developed.
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multiple congenital contractures mcc and cleft palate induced in goats by ingestion reduction in fetal movement as the probable cause of Piperidine Alkaloid containing plants
1990Co-Authors: K E Panter, R F Keeler, T D Bunch, D V Sisson, R J CallanAbstract:Fetal movement, observed by ultrasound imaging, was significantly reduced (P 5 0.001) in pregnant goats gavaged with Conium seed and Nicofiunu gZaucu and temporarily reduced with fresh Conium plant. Conium seed and Nicofiunu gZuucu induced cleft palate and multiple congenital contractures in 100% of the kids born to pregnant goats gavaged with these plants. Multiple congenital contractures included torticollis, scoliosis, lordosis, arthrogryposis, rib cage anomalies, over extension, and flexure and rigidity of the joints. However, in goats gavaged with fresh Conium plant, fetal movement was inhibited for only about 5 hours after each individual dosage and gradually returned to control levels 12 hours after dosing. Fetal malformations in this group were limited from modest to moderate contractures of the front limbs, which resolved by 8-10 weeks post partum. No cleft palates were induced. Fetal movement was not inhibited in goats fed Lupinus cuudutus and no cleft palates or multiple congenital contractures were induced in their offspring. The duration of the reduction in fetal movement appears to be an important factor in the severity and permanence of the deformities, particularly with cleft palate, spinal column defects, and severe joint deviation and fixation.
Kunio Ogasawara - One of the best experts on this subject based on the ideXlab platform.
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A Diastereocontrolled Synthesis of (+)-Febrifugine: A Potent Antimalarial Piperidine Alkaloid
Organic Letters, 2000Co-Authors: Takahiko Taniguchi, Kunio OgasawaraAbstract:A diastereocontrolled synthesis of (+)-febrifugine, a potent antimalarial Piperidine Alkaloid, has been achieved using a chiral block having a bicyclo[3.2.1]octane framework which exhibits inherent convex-face selectivity.
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a diastereocontrolled synthesis of febrifugine a potent antimalarial Piperidine Alkaloid
Organic Letters, 2000Co-Authors: Takahiko Taniguchi, Kunio OgasawaraAbstract:A diastereocontrolled synthesis of (+)-febrifugine, a potent antimalarial Piperidine Alkaloid, has been achieved using a chiral block having a bicyclo[3.2.1]octane framework which exhibits inherent convex-face selectivity.