112734-21-1Relevant articles and documents
Synthesis and solid-phase purification of anthranilic sulfonamides as CCK-2 ligands
Woods, Craig R.,Hack, Michael D.,Allison, Brett D.,Phuong, Victor K.,Rosen, Mark D.,Morton, Magda F.,Prendergast, Clodagh E.,Barrett, Terrance D.,Shankley, Nigel P.,Rabinowitz, Michael H.
, p. 6905 - 6909 (2007)
A novel strategy for the synthesis of cholecystokinin-2 receptor ligands was developed. The route employs a solution-phase synthesis of a series of anthranilic sulfonamides followed by a resin capture purification strategy to produce multi-milligram quant
Scaffold and Parasite Hopping: Discovery of New Protozoal Proliferation Inhibitors
Ackermann, Jasmin,Bachovchin, Kelly A.,Bag, Seema,Bernatchez, Jean A.,Buskes, Melissa J.,Calvet, Claudia M.,Campbell, Robert F.,Erath, Jessey,Ferrins, Lori,Jalani, Hitesh B.,Klug, Dana M.,Leed, Susan E.,McCall, Laura-Isobel,McKerrow, James,Penn, Erica C.,Pollastri, Michael P.,Rodriguez, Ana,Roncal, Norma E.,Sciotti, Richard J.,Silva, Everton M.,Singh, Baljinder,Siqueira-Neto, Jair L.,Souza, Julia M.,Thomas, Diane
, p. 249 - 257 (2020)
Utilizing a target repurposing and parasite-hopping approach, we tested a previously reported library of compounds that were active against Trypanosoma brucei, plus 31 new compounds, against a variety of protozoan parasites including Trypanosoma cruzi, Leishmania major, Leishmania donovani, and Plasmodium falciparum. This led to the discovery of several compounds with submicromolar activities and improved physicochemical properties that are early leads toward the development of chemotherapeutic agents against kinetoplastid diseases and malaria.
Indole compounds as well as preparation method, pharmaceutical composition and application thereof
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Paragraph 0468; 0470-0472, (2020/06/05)
The invention discloses indole compounds with structural characteristics of a formula (I), metabolites, metabolic precursors, prodrugs, solvates, crystals or pharmaceutically acceptable salts thereof,a preparation method of the indole compounds, and an application of the indole compounds and the metabolites, the metabolic precursors, the prodrugs, the solvates, the crystals or the pharmaceutically acceptable salts thereof as an indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor. Experimental results show that the compound disclosed by the invention has a remarkable inhibition effect on the activity of IDO1; T lymphocyte proliferation can be effectively promoted; the initial T lymphocytes are inhibited from being differentiated into regulatory T cells; the IDO1-mediated immunosuppressive effect is reversed, and the compounds can be used for treating related diseases, including cancers, viral infections, neurodegenerative diseases, cataract, organ transplant rejection, depression, autoimmune diseases and the like, with pathological characteristics of an IDO1-mediated kynurenine metabolic pathway.
2-Aminoquinazolin-4(3H)-one based plasmepsin inhibitors with improved hydrophilicity and selectivity
Rasina, Dace,Stakanovs, Georgijs,Borysov, Oleksandr V.,Pantelejevs, Teodors,Bobrovs, Raitis,Kanepe-Lapsa, Iveta,Tars, Kaspars,Jaudzems, Kristaps,Jirgensons, Aigars
, p. 2488 - 2500 (2018/04/10)
2-Aminoquinazolin-4(3H)-ones were previously discovered as perspective leads for antimalarial drug development targeting the plasmepsins. Here we report the lead optimization studies with the aim to reduce inhibitor lipophilicity and increase selectivity