- The total large-scale synthesis of argiopine
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The total large-scale synthesis of a natural toxin argiopine, a polymethylenepolyamine derivative, was developed. It consisted of 26 stages and included three key block schemes. Most of the stages proceeded quantitatively, which excluded the necessity of using the chromatographic separation of intermediates.
- Formanovsky,Popova,Mikhura
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experimental part
p. 752 - 758
(2010/07/15)
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- Substituted phenyl compounds
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Compounds of formula (I) are described wherein R1is hydrogen, -(lower alkyl)q(CO2R6or OH), —CN, —C(R7)═NOR8, NO2, —O(lower alkyl)R9, —C≡C—R10, —CR11═C(R12)(R13), —C(═O)CH2C(═O)CO2H, —CO(R14), alkylthio, alkylsulphinyl, alkylsulphonyl, carbamoyl, thiocarbamoyl, substituted carbamoyl, substituted thiocarbamoyl, sulphamoyl or an optionally substituted nitrogen-containing ring, m, n, o and p are independently zero or 1 and R2, R3, R4and R5are various groups; and physiologically acceptable salts, N-oxides and prodrugs thereof. The compounds have endothelin antagonist activity and are useful as pharmaceuticals.
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- Selective endothelin A receptor ligands. 1. Discovery and structure-activity of 2,4-disubstituted benzoic acid derivatives
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This paper describes the discovery of a new non-peptide endothelin A (ET(A)) selective ligand, 2,4-dibenzyloxybenzoic acid 3, which inhibits the binding of [125I]ET-1 to ET(A) receptors with an IC50 of 9 μM (ET-1 = endothelin-1). Optimisation of 3 resulted in compound 52 which had an IC50 of 1 μM. One of the analogues of 3, compound 15, was examined in a functional assay and shown to antagonise ET-1-induced contraction of rat aorta. The identification of 3 was made through the application of ChemDBS-3D searching of our corporate database. The 3D query, using an aromatic ring to a carboxylic acid group separated by 10.2 ± 1.1 A, was derived from an examination of common pharmacophoric distances found in the low energy conformations of two known ET(A) antagonists, the cyclic pentapeptide BQ 123 1 and myriceron caffeoyl ester 2.
- Astles,Brown,Handscombe,Harper,Harris,Lewis,Lockey,McCarthy,McLay,Porter,Roach,Smith,Walsh
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p. 409 - 423
(2007/10/03)
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- An efficient synthesis of JSTX-3, a potent neurotoxin of Joro spider (Nephila clavata)
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JSTX-3 (Joro spider toxin-3) (1), a potent neurotoxin isolated from Joro spider (Nephila clavata), has been efficiently synthesized starting from 5-azido-1-N-Boc-pentylamine (11) via the convergent synthetic strategy in which the characteristic polyamine
- Matsushita, Masayuki,Kanemura, Takanori,Hatakeyama, Susumi,Irie, Hiroshi,Toki, Takashi,Miyashita, Masaaki
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p. 10687 - 10698
(2007/10/02)
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- Amide compounds, their production and use
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A compound is provided which has the formula STR1 wherein m is an integer of 1 to 3; n is an integer of 1 or 2; p is an integer of 1 or 2; q is an integer of 1 to 6; x is an integer of 2 to 6; Ph is phenylene or a pharmceutically acceptable salt thereof. Also provided is a method for glutamate receptor inhibition which comprises administering to a mammal in need thereof an effective amount of said compound or a pharmaceutically acceptable salt thereof. Compositions for glutamate receptor inhibition are provided which contain an effective amount of said compound to provide a glutamate receptor inhibition effect, together with at least one pharmaceutically acceptable carrier, dilient or excipient therefor.
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- SYNTHESIS OF SPIDER TOXIN (JSTX-3) AND ITS ANALOGS
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One of the active principles isolated from spider venom, JSTX-3, and its analogs of the polyamine part were synthesized.
- Hashimoto, Yuichi,Endo, Yasuyuki,Shudo, Koichi,Aramaki, Yoshio,Kawai, Nobufumi,Nakajima, Terumi
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p. 3511 - 3514
(2007/10/02)
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