49609-03-2Relevant academic research and scientific papers
Trk inhibitor, preparation method and applications thereof
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Paragraph 0159-0163, (2020/03/12)
The invention belongs to the field of medicine, and particularly relates to a Trk inhibitor, a preparation method and applications thereof, mainly to compounds represented by a formula A1, a formula A2, a formula A3 or a formula A4, pharmaceutically accep
7-Aminoquinolines. A novel class of agents active against herpesviruses
Nasr,Drach,Smith,Shipman Jr.,Burckhalter
, p. 1347 - 1351 (2007/10/02)
A series of 7-aminoquinoline derivatives was synthesized and evaluated for their capacity to produce cytotoxicity in KB cells and to inhibit the replication of herpes simplex virus (HSV) type 1. All compounds tested inhibited the replication of HSV-1 with 50% inhibitory concentrations in the range of 2-50 μg/mL. The antiviral activity of many compounds, however, was separated from cytotoxicity to replicating uninfected cells by only two- to fivefold higher than those required for antiviral activity. Nonetheless, six compounds (10, 28, 29, 32, 34, and 36) were identified in which the separation was greater than fivefold. All compounds examined were more potent inhibitors of viral DNA synthesis than the cellular DNA synthesis.
NUCLEOPHILIC HETEROAROMATIC SUBSTITUTIONS. XXXIX. THE REACTION OF α- AND γ-- AND α- AND γ--7-NITROQUINOLINE WITH PIPERIDINE IN BENZONITRILE: BASE CATALYSIS AND O vs S REACTIVITY
Cidda, Claudio,Sleiter, Giancarlo
, p. 155 - 162 (2007/10/02)
The reactivity of the title compounds with piperidine has been examined.Product analysis showed that substitution is accompanied by other processes, the extent of which depends on the reactivity of the substrates towards nucleophilic substitution and is greatest in the case of the γ-arylthio derivative, which does not undergo substitution at all.Accordingly, a kinetic analysis of the reaction could be performed only for the two aryloxy and the α-arylthio derivatives.Second-order rate coefficients for the reactions of the α-substituted quinolines were found to be independent of amine concentration and the α-aryloxy derivative was found to be only ca 4 times as reactive as the α-arylthio compound.In contrast, the reaction of the γ-aryloxy derivative followed third-order kinetics and turned out to be base-catalysed because it was accelerated by added quinuclidine.The reaction mechanisms are discussed in the light of these observations and other, previously reported, facts.
