- Discovery of carbazole carboxamides as novel RORγt inverse agonists
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A novel series of carbazole carboxamides was discovered as potent RORγt inverse agonists using a scaffold hybridization strategy. Structure-activity relationship exploration on the amide linker, carbazole ring and arylsulfone moiety of the hybrid amide 3a led to identification of potent RORγt inverse agonists. Compound 6c was found to have a good RORγt activity with an IC50 of 58.5 nM in FRET assay, and reasonable inhibitory activity in mouse Th17 cell differentiation assay (58.8% inhibition at 0.3 μM). The binding mode of carbazole carboxamides in RORγt ligand binding domain was discussed.
- Huang, Yafei,Yu, Mingcheng,Sun, Nannan,Tang, Ting,Yu, Fazhi,Song, Xiaoxia,Xie, Qiong,Fu, Wei,Shao, Liming,Wang, Yonghui
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p. 465 - 476
(2018/02/28)
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- Copper(II) catalyzed aromatization of tetrahydrocarbazole: An unprecedented protocol and its utility towards the synthesis of carbazole alkaloids
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An efficient protocol for the aromatization of tetrahydrocarbazole is described by using catalytic copper(II) chloride dihydrate in DMSO. This newly established methodology has utilized towards the synthesis of naturally occurring carbazole alkaloids, namely 3-methylcarbazole, 3-formyl carbazole, glycozoline, glycozolicine and clauszoline-K. In addition, the protocol is generalized for the aromatization of N-substituted tetrahydrocarbazole, 1,2,3,4-tetrahydroquinoline, 1,2,3,4-tetrahydroisoquinoline and 1,2,3,4-tetrahydro β-carboline to give the corresponding heteroaromatic compounds from very good to excellent yield. Moreover, this method has been proven to be tolerant to a broad range of functional groups with excellent yields.
- Dalvi, Bhakti A.,Lokhande, Pradeep D.
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supporting information
p. 2145 - 2149
(2018/05/08)
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- FUNCTIONALISED AND SUBSTITUTED CARBAZOLES AS ANTI-CANCER AGENTS
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The present invention relates to anti-tropomyosin compounds, processes for their preparation, and methods for treating or preventing a disease or disorder, such as a proliferative disease (preferably cancer), using compounds of the invention.
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Page/Page column 31; 32
(2016/02/26)
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- Iodine-catalyzed aromatization of tetrahydrocarbazoles and its utility in the synthesis of glycozoline and murrayafoline A: A combined experimental and computational investigation
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A new protocol for the aromatization of tetrahydrocarbazoles has been achieved using a catalytic amount of iodine, giving high yields. The role of iodine in the aromatization has been explained by DFT, and its wide scope is extended to the total synthesis of glycozoline and murrayafoline A. This method has proven to be tolerant of a broad range of functional groups. This journal is the Partner Organisations 2014.
- Humne, Vivek,Dangat, Yuvraj,Vanka, Kumar,Lokhande, Pradeep
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supporting information
p. 4832 - 4836
(2014/07/07)
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- Discovery of ITX 4520: A highly potent orally bioavailable hepatitis C virus entry inhibitor
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The manuscript reports an identification of a highly potent, orally bioavailable hepatitis C virus entry inhibitor through optimization of a previously reported class of molecules (1) that were not stable in the rat plasma. Compound 39 (ITX 4520) exhibited an excellent PK profile in both rats and dogs with good oral exposure, half-life and oral bioavailability. The compound is also well-tolerated in the preliminary in vivo toxicity studies and has been selected as a pre-clinical candidate for our HCV clinical pipeline.
- Mittapalli, Gopi Kumar,Zhao, Fang,Jackson, Andrew,Gao, Hongfeng,Lee, Haekyung,Chow, Stephine,Kaur, Maninder Pal,Nguyen, Natalie,Zamboni, Robert,McKelvy, Jeffrey,Wong-Staal, Flossie,MacDonald, James E.
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scheme or table
p. 4955 - 4961
(2012/09/07)
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- Discovery of highly potent small molecule Hepatitis C Virus entry inhibitors
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Novel, highly potent small molecule HCV entry inhibitors are reported. The SAR exploration of a hit molecule identified from screening of a compound library led to the identification of highly potent compounds with IC 50 values of 5 nM in the tissue culture HCV infectious assay.
- Mittapalli, Gopi Kumar,Jackson, Andrew,Zhao, Fang,Lee, Haekyung,Chow, Stephine,McKelvy, Jeffrey,Wong-Staal, Flossie,MacDonald, James E.
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scheme or table
p. 6852 - 6855
(2011/12/22)
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- N-Benzyl-indolo carboxylic acids: Design and synthesis of potent and selective adipocyte fatty-acid binding protein (A-FABP) inhibitors
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Small molecule inhibitors of adipocyte fatty-acid binding protein (A-FABP) have gained renewed interest following the recent publication of pharmacologically beneficial effects of such inhibitors. Despite the potential utility of selective A-FABP inhibito
- Barf, Tjeerd,Lehmann, Fredrik,Hammer, Kristin,Haile, Saba,Axen, Eva,Medina, Carmen,Uppenberg, Jonas,Svensson, Stefan,Rondahl, Lena,Lundbaeck, Thomas
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scheme or table
p. 1745 - 1748
(2010/02/28)
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- DERIVATIVES OF SUBSTITUTED FUSED RING CYCLOINDOLES AND METHODS OF THEIR USE
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Disclosed herein are derivatives of substituted fused ring cycloindole useful, inter alia, in combating Hepatitis C infection and entry into cells.
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Page/Page column 29
(2009/10/09)
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- HEPATITIS C VIRUS ENTRY INHIBITORS
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The present invention relates to the use of tricyclic diphenylamine derivative compounds for prevention and/or treatment of Hepatitis C virus (HCV) infection by inhibiting HCV entry into permissive cells.
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Page/Page column 85
(2010/11/30)
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- TRICYCLIC CYTOPROTECTIVE COMPOUNDS
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Compounds of formula (I): in which: X is a group of formula >CR1R2 or >SO2; Y is a group of formula >NH or >CR1R2; Z is a group of formula >C=O or >CH2 or a direct bond; R1 hydrogen and R2 is hydrogen, carboxy or hydroxy; or R1 and R2 together represent an oxo group, a methylenedioxy group or a hydroxyimino group; R3 is hydrogen or lower alkyl; R4 represents two hydrogen atoms, or an oxo or hydroxyimino group; R5 is hydrogen, lower alkyl or halogen; R6 is hydrogen, lower alkoxy or carboxy; R7 and R8 are each hydrogen, lower alkyl or halogen; and pharmaceutically acceptable salts and esters thereof can be used for the treatment or prophylaxis of acute or chronic neurodegenerative diseases or conditions such as Alzheimer’s Disease, Parkinson’s Disease, Huntington’s Chorea, Multiple Sclerosis or the sequelae to acute ischaemic events such as heart attack, stroke or head injury and for protection against ischaemic damage to tissues of peripheral organs.
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Page/Page column 24-25
(2008/06/13)
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- Fused indolecarboxamides: dopamine receptor subtype specific ligands
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Disclosed are compounds of the formula: or the pharmaceutically acceptable acid addition salts thereof wherein: R1and R2are the same or different and represent hydrogen, C1-C6alkyl, halogen, hydroxy, amino, cyano, nitro, trifluoromethyl, trifluoromethoxy, C1-C6alkoxy, —O2CR′, —NHCOR′, —COR′, —SOmR′, where R′ is C1-C6alkyl and wherein m is 0, 1 or2; or R1and R2independently represent —CONR′R″, or —NR′R″ where R′ and R″ independently represent hydrogen or C1-C6alkyl; R3is hydrogen, C1-C6alkyl, or —COR′″ where R′″ is C1-C6alkyl; R4is hydrogen or C1-C6alkyl; and R represents an azacycloalkylalkyl group, which compounds are useful in the treatment of affective disorders such as schizophrenia, depression, Alzheimer's disease, movement disorders such as Parkinsonism and dysronia, and other disorders which respond to dopaminergic blockade such as substance abuse and obsessive compulsive disorders. Further, compounds of this invention are useful in treating the extrapyramidal side effects associated with the use of conventional neuroleptic agents.
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