114368-05-7Relevant articles and documents
1-benzyl-2- [...] -4-amide compound and its preparation method and application
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, (2016/10/31)
The invention discloses 1-benzyl-2-pyrroline ketone-4-amide compounds represented by the general formula. According to independent R1, R2, R3, R4, R5, R6, R7, R8, R9 or R10, 1-3 C1-4 alkyl groups substituted by substituent groups are selected from a non-substituent C1-4 alkyl group, a non-substituent C1-3 alkoxy group, halogen, an amine sulfonyl group, a nitryl group and hydrogen or from halogen, a nitryl group, a C1-3 alkyl group and a C1-2 alkoxy group, or 1-3 C1-3 alkoxy groups substituted by substituent groups are selected from halogen, a nitryl group, a C1-3 alkyl group and a C1-2 alkyl group. The halogen is fluorine, chlorine or bromine. The invention further discloses a preparing method and application of the compounds. The compounds can restrain tyrosine kinase signal transduction and unhealthy cell hyperplasia and angiogenesis, and obvious curative effect is achieved on diseases such as tumors especially.
Synthesis and structure-activity relationships of 7-[3-(1- aminoalkyl)pyrrolidinyl]- and 7-[3-1-aminocycloalkyl)pyrrolidinyl]-quinolone antibacterials
Kimura,Atarashi,Takahashi,Hayakawa
, p. 1442 - 1454 (2007/10/02)
A series of 7-[3-(1-aminoalkyl and 1-aminocycloalkyl)-1- pyrrolidinyl]quinolones have been prepared and their biological properties evaluated. Among them, 1-(S)-aminoalkyl derivatives exhibited potent antibacterial activities against gram-positive and gram-negative organisms. They had moderate lipophilicity and high aqueous solubility compared to their aminomethyl counterparts; e.g., the 3-(1-aminoethyl)-1-pyrrolidinyl compound (83) showed superior pharmacokinetic properties to its aminomethyl counterpart (6).