91600-21-4Relevant articles and documents
Synthesis and Antimicrobial Evaluation of Novel Chiral 2-Amino-4,5,6,7-tetrahydrothieno[2,3-c]pyridine Derivatives
Rossetti, Arianna,Bono, Nina,Candiani, Gabriele,Meneghetti, Fiorella,Roda, Gabriella,Sacchetti, Alessandro
, (2019/05/15)
New N-substituted-2-amino-4,5,6,7-tetrahydrothieno[2,3-c]pyridine derivatives were synthesized employing a convenient one-pot three-component method and their structures were characterized by 1H-NMR and single crystal X-ray diffraction analysis. All the synthesized compounds were in vitro screened for antimicrobial activity against Gram-positive (Sarcina lutea) and Gram-negative bacteria (Escherichia coli). In this work, we introduced a chiral residue on the tetrahydropyridine nitrogen, the hitherto the less investigated position on this pharmacophore in order to explore the effect. The antibacterial results showed that the synthesized compounds were active only against Gram-positive bacteria and the (R)-enantiomers displayed a greater antimicrobial potency than their (S)-counterparts. The structure–activity relationship here investigated may provide some interesting clues for future development of tetrahydrothienopyridine derivatives with higher antimicrobial activity.
PIPERIDIN-4-YLPIPERAZINE COMPOUNDS FOR THE TREATMENT OF HCV INFECTION
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Page/Page column 36, (2010/08/08)
The invention relates to new piperazine-pieridine compounds having anti-viral activity and particularly anti-HCV activity. The invention further relates to pharmaceutical compositions comprising compounds according to the invention.
6, 9-disubstituted 2-[trans-(4-aminocyclohexyl)amino] purines
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, (2008/06/13)
The present invention provides novel compounds of the formula (I) wherein R is selected from the group consisting of R2, R2NH—, or R3R4N—R5- wherein R2 is selected from the group consisting of C9-C12alkyl, Z is selected from the group consisting of phenyl, heterocycle, cycloalkyl, and naphthanlene; and M is selected from the group consisting of hydrogen, C1-C4alkyl, and wherein each C9-C12alkyl or Z is optionally substituted with 1 to 3 substituents, which may be the same or different, and which are selected from the group consisting of D, E, wherein each D is independently selected from the group consisting of trifluoromethyl, trifluoromethoxy, and C1-C4alkoxy; each E is independently selected from the group consisting of Hal, OH, and C1-C8alkyl; R3 and R4 are selected from the group consisting of hydrogen, C1-C4alkyl and (CH2)y-phenyl, wherein y is an integer 0-8, with the proviso that R3 and R4 not both be hydrogen; R5 is C1-C8alkylene; and R1 is selected from the group consisting of cyclopentyl, cyclopentenyl and isopropyl, and the pharmaceutically acceptable salts, optical isomers, and hydrates thereof, with the proviso that when R2 is the group wherein n is 1 or greater; R1 is isopropyl or cyclopentyl; R6 is hydrogen, C1-C4alkyl, or (CH2)m-phenyl; and Z is phenyl, heterocycle, or cycloalkyl, that Z is substituted with 1 to 3 substituents, which may be the same or different, and which are selected from the group consisting of In addition, the present invention provides a method of inhibiting cyclin dependent kinases, particularly cdk-2. The present invention also provides a method of preventing apoptosis in neuronal cells and a method of inhibiting the development of neoplasms.