16382-20-0Relevant academic research and scientific papers
Superior inhibition of influenza virus hemagglutinin-mediated fusion by indole-substituted spirothiazolidinones
Cihan-üstünda?, G?k?e,Zopun, Muhammet,Vanderlinden, Evelien,Ozkirimli, Elif,Persoons, Leentje,?apan, Gültaze,Naesens, Lieve
, (2020)
The influenza virus hemagglutinin (HA) mediates membrane fusion after viral entry by endocytosis. The fusion process requires drastic low pH-induced HA refolding and is prevented by arbidol and tert-butylhydroquinone (TBHQ). We here report a class of supe
CARBOXYLIC ACID, ACYL SULFONAMIDE AND ACYL SULFAMIDE-DERIVATIZED BICYCLIC AZA-HETEROAROMATICS AS SELECTIVE MCL-1 INHIBITORS AND AS DUAL MCL-1/BCL-2 INHIBITORS
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Page/Page column 62, (2020/12/19)
Mcl-1 selective inhibitors, Bcl-2 selective inhibitors, and Mcl-1/Bcl-2 dual inhibitors and methods of using the same for the treatment of disease are disclosed.
N- (ARYLALKYL) - 1H- INDOLE- 2 - SULFONIC ACID AMIDE COMPOUNDS AND THEIR THERAPEUTIC USE AS CANNABINOID ALLOSTERIC MODULATORS
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Page/Page column 100, (2012/09/21)
The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain /V-(arylalkyl)-1 H-indole- 2-sulfonic acid amide compounds that, inter alia, inhibit cannabinoid receptor signalling. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit cannabinoid receptor signalling; to treat disorders that are ameliorated by the inhibition of cannabinoid receptor signalling; to treat metabolic syndrome, type-2 diabetes, dyslipidaemia, obesity, eating disorders, cardiovascular diseases and disorders, and other conditions as described herein.
Indole-2-carboxamides as allosteric modulators of the cannabinoid CB 1 receptor
Piscitelli, Francesco,Ligresti, Alessia,La Regina, Giuseppe,Coluccia, Antonio,Morera, Ludovica,Allarà, Marco,Novellino, Ettore,Di Marzo, Vincenzo,Silvestri, Romano
supporting information; experimental part, p. 5627 - 5631 (2012/08/28)
We synthesized new N-phenylethyl-1H-indole-2-carboxamides as the first SAR study of allosteric modulators of the CB1 receptor. The presence of the carboxamide functionality was required in order to obtain a stimulatory effect. The maximum stimulatory activity on CB1 was exerted by carboxamides 13 (EC50 = 50 nM) and 21 (EC50 = 90 nM) bearing a dimethylamino or piperidinyl group, respectively, at position 4 of the phenethyl moiety and a chlorine atom at position 5 of the indole.
Regiospecific Bromination of 3-Methylindoles with NBS and Its Application to the Concise Synthesis of Optically Active Unusual Tryptophans Present in Marine Cyclic Peptides
Liu, Ruiyan,Zhang, Puwen,Gan, Tong,Cook, James M.
, p. 7447 - 7456 (2007/10/03)
A regiospecific bromination of substituted 3-methylindoles at either the C(3) alkyl moiety or the C(2) position was achieved via a free radical bromination or electrophilic process, respectively. The regiospecificity of the bromination could be controlled by variation of both the substituent and the N(1) protecting group on the indole ring. In addition, enantiospecific syntheses of 5-methoxytryptophan (20) and 5-hydroxy-6-chlorotryptophan (21c) as well as concise syntheses of optically active 2-bromotryptophan ethyl esters 26a,b or their substituted derivatives in three steps from bifunctional dibromoindoles were achieved via the above regiospecific process.
2-SACCHARINYLMETHYL HETEROCYCLIC CARBOXYLATES USEFUL AS PROTEOLYTIC ENZYME INHIBITORS
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, (2008/06/13)
4-R 4-R 5-2-Saccharinylmethyl heterocyclic carboxylates, useful in the treatment of degenerative diseases, are prepared by reacting a 4-R. sup.4-R 5-2-halomethylsaccharin with either a heterocyclic carboxylic acid in the presence of an acid-acceptor or th
Synthesis & Reaction of Indole-1,2-dicarboxaldehydes with Hydrazine & Hydroxylamine
Hiremath, Shivayogi P.,Thakar, Shreeram B.,Purohit, Muralidhar G.
, p. 770 - 774 (2007/10/02)
Indole-1,2-dicarboxaldehydes (2a-g) have been prepared by formylation of 3-methylindole-2-carboxaldehydes (1a-g) with DMF-POCl3 at 140 deg C. 2a-e react with N2H4.H2O to give hydrazones (3a-e and 3g) of 1-formylindole-2-carboxaldehydes instead of the tria
