36245-26-8Relevant academic research and scientific papers
Synthesis and preliminary screening of derivatives of 2-(4- arylpiperazin-1-ylalkyl)-3-oxoisothiazolo[5,4-b]pyridines as CNS and antimycobacterial agents
Malinka, Habil W.,Sieklucka-Dziuba,Rajtar,Zgodzinski,Kleinrok
, p. 416 - 425 (2007/10/03)
We have synthesized several new isothiazolopyridines possessing a side chain at the isothiazole ring typical, among others, for trazodone or NAN- 195. Representatives of the novel isothiazolopyridines were examined for acute toxicity and in several commonly used CNS tests in mice and for arterial blood pressure in rats. Three of the five compounds tested showed significant analgesic activity. The most active compound (3b) exhibited analgesic action in the 'writhing' test in a dose 1/1280 of LD50 (LD50 = 1135.5 mg/kg) after administration i.p. to mice. Additionally, the compounds described here and related isothiazolopyridines obtained previously were evaluated against Mycobacterium tuberculosis H37Rv at 12.5 μg/ml in in vitro assays. Seven of the nineteen compounds tested showed 100% inhibition of that mycobacterium.
Substituted heterocyclylalkyl esters of 1,4-dihydropyridine-3,5-dicarboxylic acids
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, (2008/06/13)
Dihydropyridine derivatives and acid addition salts thereof which are of use as prophylactic or/and therapeutic drugs for cardiovascular diseases, said dihydropyridine derivatives having the formula STR1 wherein R1, R2 and R3 are the same or different and each is alkyl, cycloalkyl, cycloalkylalkyl or alkoxyalkyl; R4 and R5 are the same or different and each is hydrogen, halogen, nitro, trifluoromethyl, alkyl, cycloalkyl, alkoxy, cyano, alkoxycarbonyl or alkylthio; R6 is hydrogen, alkyl, cycloalkyl, aralkyl, aryl or a pyridyl; X is oxygen, sulfur, vinylene, azomethine or a group of the formula STR2 A is alkylene; Ar is aryl or a pyridyl; m is an integer of 1 to 3; n is an integer of 0 to 2.
N-Aryl-N-phenoxy-alkyl-piperazine compounds useful in decreasing intracranial pressure
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, (2008/06/13)
A piperazine derivative of the formula: STR1 wherein R1 is hydrogen, alkyl (C1-8), alkyl (C1-4)-sulfonyl or an acyl group of the formula: R3 CO--(wherein R3 is hydrogen, alkyl (C1-7), halogenoalkyl (C1-4), alkoxy (C1-4)-carbonyl-alkyl (C1-4), cycloalkyl (C3-6), alkenyl (C2-5), alkoxy (C1-4), amino, alkyl (C1-4)-amino or anilino), R2 is hydrogen, alkyl (C1-4), alkoxy (C1-4)-carbonyl-alkyl (C1-4), carboxy-alkyl (C1-4), alkenyl (C2-5) or alkyl (C1-4)-sulfonyl, or R1 and R2 are combined together to form succinyl group, Ring A is phenyl, alkyl (C1-4)-phenyl or halogenophenyl, and n is an integer of 2 to 6, or a pharmaceutically acceptable acid addition salt thereof. The piperazine derivative (I) has an intracranial pressure-lowering activity. Said derivative also has a depressing effect on central nervous system.
1-Heterocyclic alkyl-1,2,3,4-tetrahydroquinazolinones
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, (2008/06/13)
1-Heterocyclic alkyl-1,2,3,4-tetrahydroquinazolinones, acid addition salts thereof, and intermediate compounds having analgesic properties. A representative quinazolinone compound is 1-[2-(1-phenyl-4-piperazinyl)-ethyl]-2-phenyl-1,2,3,4-tetrahydro-4-quina
1-Heterocyclic alkyl-1,2,3,4-tetrahydroquinazolinones and analgesic intermediates thereof
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, (2008/06/13)
1-heterocyclic alkyl-1,2,3,4-tetrahydroquinazolinones, acid addition salts thereof, and intermediate compounds having analgesic properties. A representative quinazolinone compound is 1-[2-(1-phenyl-4-piperazinyl)-ethyl]-2-phenyl-1,2,3,4-tetrahydro-4-quinazolinone. A representative analgesic intermediate is 2-[2-(4-[1-phenyl]piperazinyl)ethylamino]benzamide.
