91600-21-4Relevant academic research and scientific papers
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.
Novel symmetrical trans-bis-Schiff bases of N-substituted-4- piperidones: Synthesis, characterization, and preliminary antileukemia activity mensurations
Sun, Chuan-Wen,Wang, Hai-Feng,Zhu, Jun,Yang, Ding-Rong,Xing, Jiahua,Jin, Jia
, p. 1374 - 1380 (2014/01/06)
A series of novel symmetrical trans-bis-Schiff bases (11a, 11b, 11c, 11d, 11e, 11f, 11g, 11h, 11i, 11j, 11k, 11l, 11m) were designed and prepared as novel anticancer analogues, with the trans-configuration confirmed by X-ray diffraction. Preliminary inhibitory effects of these compounds on CML K562 cell growth were investigated, and the potential analogue 11e showed an excellent anti-leukemia activity (IC50=6.35 μg/mL), which is higher than that of the clinical drug 5-fluorouracil (IC50=8.48 μg/mL). Complete assignments had been achieved for the title compounds by spectroscopic techniques, and their structure-activity relationships have been studied.
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.
PESTICIDAL SUBSTITUTED PIPERIDINES
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Page/Page column 51; 57, (2008/06/13)
The invention relates to the use of piperidine derivatives encompassed from the general formula (I) for the control of pests, including arthropods and helminths, and a method for the control of pests.
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.
STERIC CONTROL OF THE ASYMMETRIC SYNTHESIS OF N-SUBSTITUTED 2-METHYL-4-PIPERIDONES
Grishina, G. V.,Potapov, V. M.,Abdulganeeva, S. A.,Korchagina, E. Yu.
, p. 1355 - 1362 (2007/10/02)
Transmission of the iodomethylate of 1,2-dimethyl-4-piperidone by (S)-sec-butylamine gives 1-(S-sec-butyl)-2S-methyl-4-piperidone in 33percent optical yield while transamination by (S)-1-methyl-2-phenylethylamine gives a 1:1 diastereomeric mixture of 1-(1-methyl-2-phenylethyl)-2-methyl-4-piperidone.The decrease in the optical yield is related to the facile opening of the piperidone ring at the C-N bond with subsequent recyclization.The 13C NMR data indicate that all the diastereomers of the 4-piperidones obtained are in the chair conformation with predominantly equatorial orientation of the methyl group at C(2).The chi ral optical properties were studied and the absolution configurations of the 4-piperidones were established.
