60867-91-6Relevant academic research and scientific papers
Simplified heterocyclic analogues of fluoxetine inhibit inducible nitric oxide production in lipopolysaccharide-induced BV2 cells
Park, Ju-Young,Kim, Seung-Woo,Lee, Ja-Kyeong,Im, Weon Bin,Jin, Byung Kwan,Yoon, Sung-Hwa
experimental part, p. 538 - 544 (2012/02/15)
A series of fluoxetine, where the N-methylamino group was replaced and then simplified, were synthesized and their inhibitory effect was tested for nitric oxide (NO) production and inducible NO synthase (iNOS) expression in lipopolysaccharide (LPS)-induced BV2 cells. Although the synthesized compounds generally revealed weaker activity or greater cytotoxicity than fluoxetine, compound 10a, in which the N-methylamino group in fluoxetine was replaced by morpholine, and the trifluoromethylphenyl ring was substituted with simple oxo group, suppressed NO production dose-dependently at 10, 20 and 40 μM concentrations with less cytotoxicity than fluoxetine, and inhibited iNOS mRNA and protein expression at the same concentrations in LPS-induced BV2 cells. The results suggested that the trifluoromethylphenyl ring moiety in fluoxetine is not necessary for the suppression of NO production and that 10a has the potential as a potent inhibitor of NO production.
Synthesis of benzenepropanamine analogues as non-detergent spermicides with antitrichomonas and anticandida activities
Kiran Kumar,Sharma, Vishnu Lal,Kumar, Manish,Shukla, Praveen Kumar,Tiwari, Pratibha,Jain, Rajeev Kumar,Maikhuri, Jagdamba Prasad,Singh, Divya,Gupta, Gopal,Singh, Man Mohan
, p. 6593 - 6600 (2007/10/03)
Fifteen analogues of benzenepropanamine were synthesized and evaluated for their spermicidal as well as microbicidal activities against Trichomonas vaginalis and Candida spp. Several compounds showed appreciable dual activities. Compound 12 exhibited good
Propanolamine derivatives, their preparation and use
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, (2008/06/13)
Compounds of formula I wherein, X is phenyl unsubstituted or optionally substituted with one or more cyano, halogeno, halogenoalkyl, C1-6-alkoxy, C1-6-alkyl, C1-5-alkanoyl, C3-5-alkenyl, aryloxy, aralkoxy, amino, C1-6-alkyl mono or disubstituted amino, C1-4-alkanoylamino, carbamoyl, C1-4-alkyl N-mono or disubstituted carbamoyl, C1-4-alkyl substituted with amino, C1-2-alkyl mono or disubstituted amino, N02, morpholino or imidazolyl; and, R is 3,4-methylenedioxyphenyl, aryl or heteroaryl all of which can be optionally substituted with one or more cyano, halogeno, C1-6-alkyl, C1-6-alkoxy, C2-6-alkenyl, trifluoromethyl, C3-5-alkylene, aryloxy, aralkoxy or C1-6-alkylthio; and, R1 and R2 are C1-10-alkyl, C3-7-cycloalkyl, C2-10-alkenyl, C3-6-cycloalkyl-C1-5-alkyl, all of which can be unsubstituted or substituted with C1-5-alkyl, C1-5-alkoxy or cyano; or, R1 and R2 together form a 5, 6 or 7 membered ring containing at least one nitrogen atom, or which optionally contains two nitrogen atoms, one or two oxygen atom(s) or one or two sulphur atom(s) or a combination thereof, which ring is unsubstituted or optionally substituted with C1-4-alkyl, C1-4-alkoxy or aryl; and, R3, R4, R5, R6, and R7 independently are hydrogen, C1-4-alkyl or phenyl; or, R4 and X together form a carbocyclic ring containing 5 or 6 atoms, or a salt thereof with a pharmaceutically acceptable acid; provided however that R1 and R2 are not C3-7-cycloalkyl, C1-10-alkyl or C2-10-alkenyl which may be straight, branched or cyclic, unsubstituted or substituted with C1-4-alkoxy, aryloxy or cycloalkyl, cyano or cycloalkylalkyl, when X is phenyl substituted with cyano, halogen, halogenalkyl, C1-6-alkoxy, C1-6-alkyl, C1-5-alkanoyl, C3-5-alkylene, aryloxy or aralkoxy, are useful in the treatment of anoxia, traumatic injury, ischemia, migraine, epilepsy, Parkinson's disease, Alzheimer's disease and other neurodegenerative diseases.
1-PIPERAZINES AND SOME RELATED COMPOUNDS
Valenta, Vladimir,Bartosova, Marie,Protiva, Miroslav
, p. 1280 - 1287 (2007/10/02)
Amino alcohols VIIIa-c, prepared by reduction of the Mannich bases VIa-c, were transformed by treatment with thionyl chloride to the chloro derivatives IXa-c which were subjected to substituttion reactions with the sodium salts of guaiacol, 2-ethoxyphenol and 2-benzyloxyphenol giving the title compounds IIIb,c, IVb,c and Va-c.N,N-Dimethyl-3-(2-benzyloxyphenoxy)-3-phenylpropylamine (Va) was partially demethylated by treatment with ethyl chloroformate and by the following alkaline hydrolysis to the secondary amine XI.Amines III-V and XI in high doses exhibit centralexcitation but do not show antireserpine activity; they have several structurally less specific effects (hypotensive, local anaesthetic, spasmolytic).
