97074-59-4Relevant academic research and scientific papers
NOVEL CANNABINOID RECEPTOR 2 (CB2) INVERSE AGONISTS AND THERAPEUTIC POTENTIAL FOR MULTIPLE MYELOMA AND OSTEOPOROSIS BONE DISEASES
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Paragraph 0152; 0153, (2013/07/19)
Cannabionid receptor-2 inverse antagonists include compounds represented by Formula IV, or a pharmaceutically acceptable salt thereof: wherein: R1 and R2 are independently H, alkyl, or alkenyl; R3 is alkyl, alkenyl, aryl, aralkyl, aralkenyl, heterocyclyl, heterocyclylalkyl, heteroaryl, heteroarylalkyl; R4 and R5 are independently a bond, alkylenyl, or alkenylenyl; each R6 and R7 is independently selected from the group consisting of OH, F, Cl, Br, I, (C1-C6)alkyl, alkoxy, amino, COOH, CONH2, SO3H, PO3H2, CN, SH, NO2 and CF3; and p and q are independently 0, 1, 2, 3, 4, or 5. Such compounds may be used to treat osteoporosis or multiple myeloma.
Lead discovery, chemistry optimization, and biological evaluation studies of novel biamide derivatives as CB2 receptor inverse agonists and osteoclast inhibitors
Yang, Peng,Myint, Kyaw-Zeyar,Tong, Qin,Feng, Rentian,Cao, Haiping,Almehizia, Abdulrahman A.,Alqarni, Mohammed Hamed,Wang, Lirong,Bartlow, Patrick,Gao, Yingdai,Gertsch, Jürg,Teramachi, Jumpei,Kurihara, Noriyoshi,Roodman, Garson David,Cheng, Tao,Xie, Xiang-Qun
, p. 9973 - 9987 (2013/01/16)
N,N′-((4-(Dimethylamino)phenyl)methylene)bis(2-phenylacetamide) was discovered by using 3D pharmacophore database searches and was biologically confirmed as a new class of CB2 inverse agonists. Subsequently, 52 derivatives were designed and synthesized through lead chemistry optimization by modifying the rings A-C and the core structure in further SAR studies. Five compounds were developed and also confirmed as CB2 inverse agonists with the highest CB2 binding affinity (CB2Ki of 22-85 nM, EC50 of 4-28 nM) and best selectivity (CB 1/CB2 of 235- to 909-fold). Furthermore, osteoclastogenesis bioassay indicated that PAM compounds showed great inhibition of osteoclast formation. Especially, compound 26 showed 72% inhibition activity even at the low concentration of 0.1 μM. The cytotoxicity assay suggested that the inhibition of PAM compounds on osteoclastogenesis did not result from its cytotoxicity. Therefore, these PAM derivatives could be used as potential leads for the development of a new type of antiosteoporosis agent.
On the conformation of 1-aryl-1,4-dihydro-3(2H)-isoquinolinones
Mokrosz,Cegla,Szneler
, p. 241 - 245 (2007/10/02)
1H- and 13C-NMR spectra of the 1-aryl-1,4-dihydro-3(2H)-isoquinolinones 2a-1 were examined. It was found that the 1-aryl group assumes a roughly axial position on the boat conformation of the heterocyclic ring in meta- and para-subst
