147497-57-2Relevant articles and documents
THERAPEUTIC COMPOUNDS AND METHODS TO TREAT INFECTION
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Paragraph 0428-0429, (2019/02/13)
Disclosed herein are compounds of formula I: or a salt thereof and compositions comprising a compound of formula I or a pharmaceutically acceptable salt thereof. Also disclosed herein are methods for treating or preventing a bacterial infection in an animal comprising administering to the animal a compound of formula I or a pharmaceutically acceptable salt thereof, alone or in combination with a bacterial efflux pump inhibitor.
Probing structural requirements for human topoisomerase I inhibition by a novel N1-Biphenyl fluoroquinolone
Delgado, Justine L.,Lentz, Sarah R.C.,Kulkarni, Chaitanya A.,Chheda, Pratik R.,Held, Hailey A.,Hiasa, Hiroshi,Kerns, Robert J.
, p. 109 - 130 (2019/04/10)
Fluoroquinolones substituted with N-1 biphenyl and napthyl groups were discovered to act as catalytically inhibitors of human topoisomerases I and II, and to possess anti-proliferative activity in vivo. Structural requirements for these novel quinolones t
Evaluation of Improved Glycogen Synthase Kinase-3α Inhibitors in Models of Acute Myeloid Leukemia
Neumann, Theresa,Benajiba, Lina,G?ring, Stefan,Stegmaier, Kimberly,Schmidt, Boris
, p. 8907 - 8919 (2015/12/09)
The challenge for glycogen synthase kinase-3 (GSK-3) inhibitor design lies in achieving high selectivity for one isoform over the other. The therapy of certain diseases, such as acute myeloid leukemia (AML), may require α-isoform specific targeting. The s
4-Azaindole Derivatives
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, (2015/04/15)
4-Azaindole derivatives which are modulators of muscarinic acetylcholine receptor (mAChR) M1 and which may be effective for the prevention or disease modifying or symptomatic treatment of cognitive deficits associated with neurological disorders such as Alzheimer-type dementia (AD) or dementia with Lewy bodies (DLB), and a pharmaceutical composition comprising a 4-azaindole derivative as an active ingredient.
4-AZAINDOLE DERIVATIVES
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, (2015/04/22)
4-Azaindole derivatives which are modulators of muscarinic acetylcholine receptor (mAChR) M1 and which may be effective for the prevention or disease modifying or symptomatic treatment of cognitive deficits associated with neurological disorders such as Alzheimer-type dementia (AD) or dementia with Lewy bodies (DLB), and a pharmaceutical composition comprising a 4-azaindole derivative as an active ingredient.
Biarylmethoxy isonipecotanilides as potent and selective inhibitors of blood coagulation factor Xa
Lopopolo, Gianfranco,Fiorella, Filomena,De Candia, Modesto,Nicolotti, Orazio,Martel, Sophie,Carrupt, Pierre-Alain,Altomare, Cosimo
, p. 180 - 191 (2012/01/05)
New chloro-substituted biarylmethoxyphenyl piperidine-4-carboxamides were synthesized and assayed in vitro as inhibitors of the blood coagulation enzymes factor Xa (fXa) and thrombin. An investigation of effects of the amidine and isopropyl groups attache
Fluorinated benzyloxyphenyl piperidine-4-carboxamides with dual function against thrombosis: Inhibitors of factor xa and platelet aggregation
De Candia, Modesto,Liantonio, Francesco,Carotti, Andrea,De Cristofaro, Raimondo,Altomare, Cosimo
experimental part, p. 1018 - 1028 (2009/12/24)
A series of benzyloxy anilides of nipecotic (5, 6) and isonipecotic (7, 8) acids were synthesized and assayed in vitro as inhibitors of ADP-induced platelet aggregation and the blood coagulation enzymes factor Xa (FXa) and thrombin (Flla). An exploration of effects of the amidine group attached at the piperidine nitrogen, position and substitution (F, phenyl) of the benzyloxy group, and addition of fluorine/s on the second (distal) phenyl ring, led us to single out some promising isonipecotamide derivatives 7. Addition of meta-F and para-CF3 on the distal phenyl ring resulted in a 6-to-18-fold enhancement of the FXa potency and in 2-to- 4-fold increase of the antiplatelet potency, the last depending to a large extent upon lipophilicity. Two congeners of N-{[3-(1,1′-biphenyl-4-yl)methoxy]phenyljpiperidine-4-carboxamide (7m and 7p) proved to be potent FXa-selective inhibitors (Ki = 130 and 57 nM, respectively) and antiplatelet agents and were identified as leads for developing new dual function antithrombotic drugs.
