129604-54-2Relevant articles and documents
The second aryl piperazine compounds and their pharmaceutical use (by machine translation)
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Paragraph 0145, (2017/07/26)
The invention relates to the general formula I indicated by the two aryl piperazine compound, solvate, stereoisomer or a pharmaceutically acceptable salt thereof, pharmaceutical compositions containing them, and the compounds for the preparation for preventing or treating post-surgical pain, migraine, visceral pain, neuropathic pain such as the pain and analgesics such as by analgesic drug addiction and tolerance caused by the use of disease. (by machine translation)
Design, synthesis and evaluation of new GEQ derivatives as inhibitors of InhA enzyme and Mycobacterium tuberculosis growth
Chollet, Aurélien,Mori, Giorgia,Menendez, Christophe,Rodriguez, Frédéric,Fabing, Isabelle,Pasca, Maria Rosalia,Madacki, Jan,Korduláková, Jana,Constant, Patricia,Quémard, Anna?k,Bernardes-Génisson, Vania,Lherbet, Christian,Baltas, Michel
, p. 218 - 235 (2015/07/07)
A series of fluorene-based derivatives was synthesized and evaluated for inhibiting both InhA and Mycobacterium tuberculosis growth. These compounds were inspired by the previously reported Genz-10850 molecule, a good InhA inhibitor, but with a poor activity against M. tuberculosis growth. Structure-activity relationships were performed by introducing the following chemical modifications: 1) the piperazine ring; 2) the amide group; 3) the aryl moiety; and 4) the fluorene moiety. Among these new derivatives, one of them was more effective against both the InhA activity and mycobacterial growth, compared to the hit compound. Docking studies were also performed to rationalize activities of these derivatives. Furthermore, we showed for the first time that efflux pump inhibitors potentiated the efficacy of Genz-10850 (GEQ) derivatives against M. tuberculosis growth, demonstrating that these compounds could be substrates of some efflux pumps.
PLASMINOGEN ACTIVATOR INHIBITOR-1 INHIBITOR
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Page/Page column 51, (2009/05/28)
The present invention relates to an inhibitor of plasminogen activator inhibitor-1. The present invention further relates to a pharmaceutical composition that has an inhibitory action on PAI-1 activity and is useful in the prevention and treatment of various diseases whose onset is associated with PAI-1 activity. Furthermore, the present invention relates to a novel compound having PAI-1 inhibitory activity represented by the following general formula (I), and a salt thereof. Each symbol is defined as those in the specification.
Pyrrolidine carboxamides as a novel class of inhibitors of enoyl acyl carrier protein reductase from Mycobacterium tuberculosis
He, Xin,Alian, Akram,Stroud, Robert,Ortiz De Montellano, Paul R.
, p. 6308 - 6323 (2007/10/03)
In view of the worldwide spread of multidrug resistance of Mycobacterium tuberculosis, there is an urgent need to discover antituberculosis agent with novel structures. InhA, the enoyl acyl carrier protein reductase (ENR) from M. tuberculosis, is one of t
Amino acid derivative having anti-CCK activity
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, (2008/06/13)
A compound represented by the formula (1): STR1 wherein, m is an integer of 1 to 3; n is an integer 0 or 1; A represents CH or N atom, and forms together with the N atom bonded to the carbonyl group a piperidine ring or a piperazine ring; R1 independently represents a straight or branched chain alkyl group having 1 to 4 carbon atoms; a cycloalkyl group having 3 to 8 carbon atoms; a phenyl group, unsubstituted or substituted with a halogen atom or with an alkoxy group having 1 to 4 carbon atoms; or a pyridyl group; or two R1, together with the group >CH-- to which they bind, form a dibenzo cycloheptenyl group or a fluorenyl group; R2 represents a phenyl group substituted with a carboxyl or substituted carboxyl group; a pyridyl group substituted with a carboxyl or substituted carboxyl group, a pyrazyl group substituted with a carboxyl or substituted carboxyl group, an oxazolyl substituted with a carboxyl or substituted carboxyl group, a triazolyl substituted with one or two carboxyl or substituted carboxyl groups, or a phosphonopyridyl group; and R3 represents an indolyl group unsubstituted or substituted with a substituent selected from the group consisting of a halogen atom, a hydroxy group, an alkoxy group having 1 to 4 carbon atoms and methoxycarbonyl ethyl group and the pharmaceutically acceptable salts thereof.
Structure-activity relationship of newly synthesized quinoline derivatives for reversal of multidrug resistance in cancer
Suzuki, Tsuneji,Fukazawa, Nobuyuki,San-nohe, Kunio,Sato, Wakao,Yano, Osamu,Tsuruo, Takashi
, p. 2047 - 2052 (2007/10/03)
The effect of 24 newly synthesized quinoline derivatives on tumor cell multidrug resistance (MDR) was examined in vitro. At low concentrations, these compounds enhanced the accumulation of [3H]vincristine in K562/ADM cells and reversed tumor cell MDR. The results of the structure-activity relationship analysis indicate that in highly active compounds the two aryl rings in the hydrophobic moiety deviate from a common plane, so they are capable of interacting with hydrogen bond donors of P-170 glycoprotein (P- gp) via π-hydrogen-π interactions. Other major structural features which influence the MDR-reversing activities of these compounds are a quinoline nitrogen atom and a basic nitrogen atom in piperazine. Furthermore, in highly active compounds, the distance between the hydrophobic moiety and the basic nitrogen atom (an atom connected to 2-hydroxypropoxyquinoline) must be at least 5 A?. Several compounds were found to reverse vincristine resistance in K562/ADM cells in vitro, and compound 16 (MS-209) was selected for clinical studies.
Bis-benzo, cyclohepta piperidylidene, piperidine and piperazine compounds, compositions and methods of use
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, (2008/06/13)
Bis-benzo cyclohepta piperidine, piperidylidene and piperazine compounds of the general formula, STR1 and pharmaceutically acceptable salts thereof are disclosed, which possess anti-allergic and/or anti-inflammatory activity. Methods for preparing and using the compounds are also described.
Bis-benzo or benzopyrido cyclohepta piperidene, piperidylidene and piperazine compounds, compositions and methods of use
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, (2008/06/13)
Bis-benzo or benzopyrido piperidene, piperidylidene and piperazine compounds of the formula: STR1 and pharmaceutically acceptable salts thereof are disclosed, wherein Z represents --(C(Ra)2)m --Y--(C(Ra)2)n -- or STR2 The compounds of Formula I possess anti-allergic and anti-inflammatory activity. Methods for preparing and using the compounds are also described.