- INHIBITORS OF VAP-1
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Provided herein are compounds and methods of use thereof for the modulation of VAP-1 activity.
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Paragraph 0439
(2020/05/12)
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- Formal asymmetric synthesis of a 7-methoxyaziridinomitosene
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The conversion of (-)-2,3-O-isopropylidene-D-erythronolactone (14) and 2-benzyloxy-6-bromo-4-methoxy-3-methylaniline (18) into {(1R,2R)-(-)-1-azido-2, 3,5,8-tetrahydro-7-methoxy-6-methyl-2-methanesulfonyloxy-5,8-dioxo-1H-pyrrolo- [1,2-a]indol-9-yl}methyl phenyl carbonate (39) has been accomplished in 17 steps by way of the enaminone 26. Key steps included the preparation of 26 by a Reformatsky reaction on a thiolactam precursor 25, and intramolecular Heck reaction of 26 to form the indole ring. The preparation of 39 constitutes a formal synthesis of the fully functionalised 7-methoxyaziridinomitosene 12, only the second such synthesis to have been accomplished. Georg Thieme Verlag Stuttgart.
- Michael, Joseph P.,De Koning, Charles B.,Mudzunga, Theophilus T.,Petersen, Riaan L.
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p. 3284 - 3288
(2008/09/17)
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- Novel series of O-substituted 8-quinolines and 4-benzothiazoles as potent antagonists of the bradykinin B2 receptors
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The synthesis and the SAR study of novel O-substituted 8-quinolines and 4-benzothiazoles as highly potent non-peptide bradykinin B2 receptor antagonists are described. Several members of this series of antagonists efficiently inhibited the BK-induced vasoconstriction on different isolated organ preparations.
- Heitsch, Holger,Wagner, Adalbert,Schoelkens, Bernward A.,Wirth, Klaus
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p. 327 - 332
(2007/10/03)
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- Resorufin derivatives
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The present invention provides resorufin derivatives of the general formulae: STR1 wherein R1, R2, R3, R4 and R5, which can be the same or different, are hydrogen, halogen, carboxyl, carboxamido, lower alkoxycarbonyl, cyano or nitro groups or lower alkyl or lower alkoxy radicals, which can be substituted by carboxyl, carboxamido, lower alkoxycarbonyl, cyano or nitro groups, and wherein R4 and R5 can together also represent an anellated aromatic residue, Z is a bridge member, A is the residue of a ligand and n is a whole number of from 1 to 200. The present invention also provides processes for the preparation of these resorufin derivatives, as well as intermediates for the preparation thereof.
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- Synthesis of Indolin-2-ones (Oxindoles) Related to Mitomycin A
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Oxindoles (indolin-2-ones) containing the functionality of the first two rings of the mytomicin A structure have been synthesized.Attempts to employ the oxindole grouping to construct the third ring were unsuccessful because of the resistance of the oxindole group or its derivatives towards nucleophilic attack.An unusual methylation of 3-methyl-5-nitrobenzene-1,2,4-triol to give the (E)-3,6-dihydroxy-2-methyl-1,4-benzoquinone 4-methoxyimine N-oxide is noted.A novel indole formation is described.
- Raphael, Ralph A.,Ravenscroft, Paul
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p. 1823 - 1828
(2007/10/02)
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