The Experts below are selected from a list of 33 Experts worldwide ranked by ideXlab platform
Zohreh Kheilkordi - One of the best experts on this subject based on the ideXlab platform.
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recent progress towards synthesis of the indolizidine alkaloid 195b
Current Organic Synthesis, 2020Co-Authors: Ghodsi Mohammadi Ziarani, Fatemeh Mohajer, Zohreh KheilkordiAbstract:BACKGROUND Natural products have been received attention due to their importance in human life as those are biologically active. In this review, there are some reports through different methods related to the synthesis of the indolizidine 195B which was extracted from Poisonous Frog; however, due to respect nature, the synthesis of natural compounds such as indolizidine has been attracted much attention among scientists and researchers. OBJECTIVE This review discloses the procedures and methods to provide indolizidine 195B from 1989 to 2018 due to their importance as a natural product. CONCLUSION There are several methods to give rise to the indolizidine 195B as a natural product that is highly active from the biological perspective in pharmaceutical chemistry. In summary, many protocols for the preparations of indolizidine 195B from various substrates, several reagents, and conditions have been reported from different aromatic and aliphatic.
Floris P. J. T. Rutjes - One of the best experts on this subject based on the ideXlab platform.
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Amidopalladation of alkoxyallenes applied in the synthesis of an enantiopure 1-ethylquinolizidine Frog alkaloid.
Journal of the American Chemical Society, 2004Co-Authors: Sape S. Kinderman, René De Gelder, Jan H. Van Maarseveen, Hans E. Schoemaker, Henk Hiemstra, Floris P. J. T. RutjesAbstract:A palladium-catalyzed amidation of alkoxyallenes has been developed for the construction of linear allylic N,O-acetals under basic conditions involving (cyclic) amides, sulfonamides, carbamates, and amidophosphates. Application of the methodology provided access to the enantiopure 1-ethylquinolizidine structural motif, which is a key synthon in the synthesis of the naturally occurring Poisonous Frog quinolizidine 233A and derivatives such as the 1-epi-isomer of quinolizidine 207I.
Stephen Robert Fletcher - One of the best experts on this subject based on the ideXlab platform.
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Antinociceptive and toxic effects of (+)-epibatidine oxalate attributable to nicotinic agonist activity
British Journal of Pharmacology, 1994Co-Authors: Nadia M. J. Rupniak, Rosemarie Marwood, Jackie Elliott, Shil Patel, John R Traynor, J K Webb, Stephen B Freedman, Stephen Robert FletcherAbstract:1. Epibatidine is an analgesic substance, isolated from the skin of the Poisonous Frog Epipedobates tricolor, for which the mechanism of action was previously unknown. 2. The IC50 of synthetic (+)-epibatidine oxalate (the naturally occurring isomer) for [3H]-nicotine binding to rat whole-brain membranes was 0.1 nM. The (-)-isomer also exhibited high affinity (IC50 = 0.2 nM). 3. (+)- and (-)-Epibatidine exhibited much lower affinity for displacement of the muscarinic ligand [3H]-N-methylscopolamine binding to rat cortical membranes (Kapp = 6.9 microM and 16.0 microM respectively). The (+)-enantiomer of epibatidine had an antagonist/agonist (NMS/oxo-M) binding ratio of 4.2 This is consistent with a muscarinic antagonist profile. 4. (+)-Epibatidine oxalate (10 microM) did not cause significant (> 30%) displacement of radioligand binding to opioid, excitatory amino acid, benzodiazepine, 5-HT, dopamine, adrenaline or peptide receptors. 5. (+)- and (-)-Epibatidine (5-20 micrograms kg-1 s.c.) doubled response latency in the mouse hot-plate test. Antinociception and behavioural depression induced by (+)-epibatidine (5 micrograms kg-1) was fully blocked by the nicotinic antagonists mecamylamine (2 mg kg-1 s.c.) or dihydro-beta-erythroidine (2 mg kg-1 s.c.). The muscarinic antagonist scopolamine (0.4 and 10 mg kg-1 s.c.) caused partial reversal of antinociception induced by (+)-epibatidine in mice, but not in rats. 6. These findings demonstrate that (+)-epibatidine oxalate salt is a highly selective and potent nicotinic analgesic agent.
Ghodsi Mohammadi Ziarani - One of the best experts on this subject based on the ideXlab platform.
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recent progress towards synthesis of the indolizidine alkaloid 195b
Current Organic Synthesis, 2020Co-Authors: Ghodsi Mohammadi Ziarani, Fatemeh Mohajer, Zohreh KheilkordiAbstract:BACKGROUND Natural products have been received attention due to their importance in human life as those are biologically active. In this review, there are some reports through different methods related to the synthesis of the indolizidine 195B which was extracted from Poisonous Frog; however, due to respect nature, the synthesis of natural compounds such as indolizidine has been attracted much attention among scientists and researchers. OBJECTIVE This review discloses the procedures and methods to provide indolizidine 195B from 1989 to 2018 due to their importance as a natural product. CONCLUSION There are several methods to give rise to the indolizidine 195B as a natural product that is highly active from the biological perspective in pharmaceutical chemistry. In summary, many protocols for the preparations of indolizidine 195B from various substrates, several reagents, and conditions have been reported from different aromatic and aliphatic.
Sape S. Kinderman - One of the best experts on this subject based on the ideXlab platform.
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Amidopalladation of alkoxyallenes applied in the synthesis of an enantiopure 1-ethylquinolizidine Frog alkaloid.
Journal of the American Chemical Society, 2004Co-Authors: Sape S. Kinderman, René De Gelder, Jan H. Van Maarseveen, Hans E. Schoemaker, Henk Hiemstra, Floris P. J. T. RutjesAbstract:A palladium-catalyzed amidation of alkoxyallenes has been developed for the construction of linear allylic N,O-acetals under basic conditions involving (cyclic) amides, sulfonamides, carbamates, and amidophosphates. Application of the methodology provided access to the enantiopure 1-ethylquinolizidine structural motif, which is a key synthon in the synthesis of the naturally occurring Poisonous Frog quinolizidine 233A and derivatives such as the 1-epi-isomer of quinolizidine 207I.