- Novel synthesis of 4-or 6-substituted indirubin derivatives
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A simple and convenient route for synthesis of a series of 4-or 6-substituted indirubin derivatives by oxidation and subsequent condensation of indoxyl and isatin is described. Acidic reaction conditions are crucial to the condensation of 4-substituted derivatives, whereas for the condensation of 6-substituted derivatives, both acidic and basic conditions work well. Copyright Taylor & Francis Group, LLC.
- Zhang, Aiying,Yu, Mingfeng,Lan, Tian,Liu, Zenglu,Mao, Zhenmin
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experimental part
p. 3125 - 3134
(2010/12/24)
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- Oxindole derivative
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An oxindole of Formula 1 or a prodrug thereof, or a pharmaceutically acceptable salt thereof is useful for growth hormone releaser: wherein R1, R2, R3and R4are independently hydrogen, optionally substituted alkyl etc; R5is optionally substituted aryl or optionally substituted heteroaryl; Z is —O— or —NH—; one of W1and W2is hydrogen, alkyl or —Y—CON(R10)R11; the other of W1and W2is n is 1, 2 or 3; m is 0, 1, 2 or 3; Y is single bond or C1-C3alkylene; R6and R7are independently hydrogen, optionally substituted alkyl etc; R8and R9are independently hydrogen, optionally substituted alkyl etc; R10and R11are independently hydrogen, alkyl etc.
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- Pyridazinedione compounds useful in treating neurological disorders
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The present invention relates to pyridazino[4,5-b]quinolines, and pharmaceutically useful salts thereof, which are excitatory amino acid antagonists and which are useful when such antagonism is desired such as in the treatment of neurological disorders. The invention further provides pharmaceutical compositions containing pyridazino[4,5-b]quinolines as active ingredient, and methods for the treatment of neurological disorders.
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- Condensed heterocyclic systems containing bridgehead nitrogen atom: Synthesis and bioactivity of thiazolo[3′,2′:2,3][1,2,4]triazino[5,6-b]indole and isomeric thiazolo[2′,3′:3,4][1,2,4]triazin[5,6-b]indole
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9-Trifluoromethyl-5H-2,3-dihydro[1,2,4]triazino[5,6-b]indole-3-thione (2) on condensation with p-chlorophenacylbromide gives 5H-3-p-chlorophenacylmercapto-9-trifluoromethyl[1,2,4]triazino-[5,6-b] indole hydrobromide (3) which on cyclization yields 3-p-chlorophenyl-6-trifluoromethyl-thiazolo[3′,2′:2,3][1,2,4] triazino[5,6-b]indole (4) and not the angular isomeric 1-(p-chlorophenyl)-6-trifluoromethylthiazolo[2′,3′:3,4][1,2,4] triazino[5,6-b]indole (6). The unequivocal synthesis of 6 has also been accomplished. The antibacterial and antifungal activity of 4 and 6 have been evaluated.
- Mohan, Jag,Kataria, Sangeeta
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p. 456 - 458
(2007/10/03)
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- Antimicrobial activity of fluorinated 1,2-benzisothiazol-3(2H)-ones and 2,2'-dithiobis(benzamides)
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Fluoro and trifluoromethyl derivatives of 1,2-benzisothiazol-3(2H)-ones and the 2,2'-dithiobis(benzamides) have been prepared and their antifungal and antibacterial activity evaluated. Several compounds were found highly active against fungi and Gram-positive microorganisms and a few derivatives displayed some activity against Gram-negative strains. Structure-activity relationships are proposed.
- Carmellino,Pagani,Pregnolato,Terreni,Pastoni
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p. 743 - 751
(2007/10/02)
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