78156-04-4Relevant academic research and scientific papers
INHIBITORS OF HIV-1 NEF FOR THE TREATMENT OF HIV DISEASE
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, (2020/05/21)
A compound of formula I, or a stereoisomer, tautomer, or pharmaceutically acceptable salt thereof: Formula I wherein X1 is benzimidazolyl, substituted benzimidazolyl, azabenzimidazolyl, substituted azabenzimidazolyl, pyrazolyl, or substituted pyrazolyl; X2 is aryl, substituted aryl, arylalkyl, substituted arylalkyl, heteroaryl, substituted heteroaryl, heteroarylalkyl, substituted heteroarylalkyl, cycloalkyl, substituted cycloalkyl, (cycloalkyl)alkyl, substituted (cycloalkyl)alkyl, heterocycloalkyl, substituted heterocycloalkyl, (heterocycloalkyl)alkyl, substituted (heterocycloalkyl)alkyl, alkyl, substituted alkyl, alkoxycarbonyl, substituted alkoxycarbonyl, dialkylaminocarbonyl, substituted dialkylaminocarbonyl, (heterocycloalkyl)carbonyl, or substituted (heterocycloalkyl)carbonyl; X3 is alkyl, substituted alkyl, alkenyl, substituted alkenyl, heterocycloalkyl, substituted heterocycloalkyl, (heterocycloalkyl)alkyl, substituted (heterocycloalkyl)alkyl, aryl, substituted aryl, arylalkyl, substituted arylalkyl, heteroaryl, substituted heteroaryl, heteroarylalkyl, substituted heteroarylalkyl, cycloalkyl, substituted cycloalkyl, (cycloalkyl)alkyl, or substituted (cycloalkyl)alkyl; and X4 is hydroxy, amino, alkyl, or hydrogen.
1,3,4-OXADIAZOLE DERIVATIVE COMPOUNDS AS HISTONE DEACETYLASE 6 INHIBITOR, AND THE PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
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, (2020/12/11)
The present invention relates to 1,3,4-oxadiazole derivative compounds having a histone deacetylase 6 (HDAC6) inhibitory activity, stereoisomers thereof or pharmaceutically acceptable salts thereof, a use thereof in preparation of a medicament, a pharmaceutical composition comprising the same, a therapeutic method using the composition, and a method for preparing the same, and the 1,3,4-oxadiazole derivative compounds are represented by a following chemical formula (I).
Design, synthesis and biological evaluation of novel 7-alkylamino substituted benzo[ a[phenazin derivatives as dual topoisomerase I/II inhibitors
Yao, Bing-Lei,Mai, Yan-Wen,Chen, Shuo-Bin,Xie, Hua-Ting,Yao, Pei-Fen,Ou, Tian-Miao,Tan, Jia-Heng,Wang, Hong-Gen,Li, Ding,Huang, Shi-Liang,Gu, Lian-Quan,Huang, Zhi-Shu
, p. 540 - 553 (2015/01/30)
A novel series of benzo[a]phenazin derivatives bearing alkylamino side chains were designed, synthesized and evaluated for their topoisomerases inhibitory activity as well as cytotoxicity against four human cancer cell lines (HL-60, K-562, HeLa, and A549)
TRIAZOLO- AND PYRAZOLOQUINAZOLINE DERIVATIVES AS PDE10A ENZYME INHIBITOR
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, (2012/02/02)
The invention relates to compounds of the formula (I) and their use as pharmaceutical ingredients, in particular for the treatment of CNS related diseases.
Synthesis and structure-activity relationship of new 1,5-dialkyl-1,5- benzodiazepines as cholecystokinin-2 receptor antagonists
Roberts, Karen,Ursini, Antonella,Barnaby, Robert,Cassar, Paolo G.,Corsi, Mauro,Curotto, Giovanni,Donati, Daniele,Feriani, Aldo,Finizia, Gabriella,Marchioro, Carla,Niccolai, Daniela,Oliosi, Beatrice,Polinelli, Stefano,Ratti, Emiliangelo,Reggiani, Angelo,Tedesco, Giovanna,Tranquillini, Maria E.,Trist, David G.,Van Amsterdam, Franciscus T.M.
, p. 4257 - 4273 (2011/08/21)
This article deals with the synthesis and the activities of some 1,5-dialkyl-3-arylureido-1,5-benzodiazepin-2,4-diones which were prepared as potential CCK2 antagonists, with the intention to find a possible follow up of our lead compound GV150013, showin
Benzimidazole and imidazole inhibitors of histone deacetylases: Synthesis and biological activity
Bressi, Jerome C.,Jong, Ron de,Wu, Yiqin,Jennings, Andy J.,Brown, Jason W.,O'Connell, Shawn,Tari, Leslie W.,Skene, Robert J.,Vu, Phong,Navre, Marc,Cao, Xiaodong,Gangloff, Anthony R.
scheme or table, p. 3138 - 3141 (2010/09/03)
A series of N-hydroxy-3-[3-(1-substituted-1H-benzoimidazol-2-yl)-phenyl]-acrylamides (5a-5ab) and N-hydroxy-3-[3-(1,4,5-trisubstituted-1H-imidazol-2-yl)-phenyl]-acrylamides (12a-s) were designed, synthesized, and found to be nanomolar inhibitors of human histone deacetylases. Multiple compounds bearing an N1-piperidine demonstrate EC50s of 20-100 nM in human A549, HL60, and PC3 cells, in vitro and in vivo hyperacetylation of histones H3 and H4, and induction of p21waf. Compound 5x displays efficacy in human tumor xenograft models.
BENZIMIDAZOLONE DERIVATIVES
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Page/Page column 28, (2009/12/23)
This invention relates to compounds and methods for the treatment of a condition mediated by CB1 receptor activity in a mammalian subject including a human, which comprises administering to a mammal in need of such treatment a therapeutically effective am
The SAR studies of novel CB2 selective agonists, benzimidazolone derivatives
Omura, Hirofumi,Kawai, Makoto,Shima, Akiko,Iwata, Yasuhiro,Ito, Fumitaka,Masuda, Tsutomu,Ohta, Atsuko,Makita, Naoya,Omoto, Kiyoyuki,Sugimoto, Hiromi,Kikuchi, Akira,Iwata, Hiroshi,Ando, Kazuo
scheme or table, p. 3310 - 3314 (2009/04/05)
Benzimidazolone derivatives were discovered as novel CB2 selective agonists. Structure Activity Relationship (SAR) studies around them were examined to improve metabolic stability. Compound 39 exhibited excellent metabolic stability in human liver microsomes (HLM) and significant attenuation of the chronic colonic allodynia in the TNBS-treated rats by po administration.
BENZIMIDAZOLONE DERIVATIVES AS CB2 RECEPTOR LIGANDS
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Page/Page column 34, (2008/06/13)
This invention relates to compounds of the formula (I): or pharmaceutically acceptable salts thereof, wherein: A, B, R1, R2 and R3 are each as described herein, and compositions containing such compounds and the use of suc
Synthesis and evaluation of 3-anilino-quinoxalinones as glycogen phosphorylase inhibitors
Dudash Jr., Joseph,Zhang, Yongzheng,Moore, John B.,Look, Richard,Liang, Yin,Beavers, Mary Pat,Conway, Bruce R.,Rybczynski, Philip J.,Demarest, Keith T.
, p. 4790 - 4793 (2007/10/03)
A series of 3-anilino-quinoxalinones has been identified as a new class of glycogen phosphorylase inhibitors. The lead compound 1 was identified through high throughput screening as well as through pharmacophore-based electronic screening. Modifications were made to the scaffold of 1 to produce novel analogues, some of which are 25 times more potent than the lead compound.
