479080-20-1Relevant articles and documents
Exploring Heteroaromatic Rings as a Replacement for the Labile Amide of Antiplasmodial Pantothenamides
Guan, Jinming,Spry, Christina,Tjhin, Erick T.,Yang, Penghui,Kittikool, Tanakorn,Howieson, Vanessa M.,Ling, Harriet,Starrs, Lora,Duncan, Dustin,Burgio, Gaetan,Saliba, Kevin J.,Auclair, Karine
, p. 4478 - 4497 (2021/05/04)
Malaria-causing Plasmodium parasites are developing resistance to antimalarial drugs, providing the impetus for new antiplasmodials. Although pantothenamides show potent antiplasmodial activity, hydrolysis by pantetheinases/vanins present in blood rapidly inactivates them. We herein report the facile synthesis and biological activity of a small library of pantothenamide analogues in which the labile amide group is replaced with a heteroaromatic ring. Several of these analogues display nanomolar antiplasmodial activity against Plasmodium falciparum and/or Plasmodium knowlesi, and are stable in the presence of pantetheinase. Both a known triazole and a novel isoxazole derivative were further characterized and found to possess high selectivity indices, medium or high Caco-2 permeability, and medium or low microsomal clearance in vitro. Although they fail to suppress Plasmodium berghei proliferation in vivo, the pharmacokinetic and contact time data presented provide a benchmark for the compound profile likely required to achieve antiplasmodial activity in mice and should facilitate lead optimization.
Design, synthesis and cytotoxic evaluation of a library of oxadiazole-containing hybrids
Camacho, Cristián M.,Pizzio, Marianela G.,Roces, David L.,Boggián, Dora B.,Mata, Ernesto G.,Bellizzi, Yanina,Barrionuevo, Elizabeth,Blank, Viviana C.,Roguin, Leonor P.
, p. 29741 - 29751 (2021/10/07)
The development of hybrid compounds led to the discovery of new pharmacologically active agents for some of the most critical diseases, including cancer. Herein, we describe a new series of oxadiazole-containing structures designed by a molecular hybridiz
Preparation method and intermediate of benzodiazepine compound
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Paragraph 0075-0077, (2020/09/16)
The invention discloses a preparation method of a benzodiazepine compound and an intermediate compound K. The compound K disclosed by the invention can be used for preparing the compound shown as theformula I in one step at high yield. The preparation met
Five-membered heterocycle substitutive N-alkenamides WNT pathway inhibitor
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Paragraph 0076; 0077; 0078; 0079, (2017/08/29)
The present invention discloses a five-membered heterocycle substitutive N-alkenamides WNT pathway inhibitor, belonging to a compound capable of adjusting the activity of a Wnt single pathway; and the present invention also provides a preparation method of the compound, and application of the compound in preparation of a drug antagonizing the Wnt single pathway. The five-membered heterocycle substitutive N-alkenamides WNT pathway inhibitor provided by the present invention is based on a reasonable drug design of a target, is obvious in antineoplastic activity, can be used for developing a new-generation Wnt pathway inhibitor, has an excellent clinical application value and is considerable in market potential.
OXADIAZOLE COMPOUNDS WHICH INHIBIT BETA-SECRETASE ACTIVITY AND METHODS OF USE THEREOF
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Page/Page column 83, (2012/05/05)
The invention provides novel beta-secretase inhibitors and methods for their including methods of treating Alzheimer's disease.
Tetrahydroquinoline Derivatives And Their Pharmaceutical Use
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Page/Page column 32, (2012/08/28)
Tetrahydroquinoline compounds of formula (I) and salts thereof, pharmaceutical compositions containing such compounds and their use in therapy.
INDAZOLE DERIVATIVES AND THEIR USE FOR BLOCKADING VOLTAGE DEPENDENT SODIUM CHANNELS
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Page/Page column 24, (2011/06/19)
The invention provides an indazole derivative of formula (1), or a pharmaceutically acceptable salt or N-oxide thereof, wherein R1, R2, R3 and R4 are as defined herein. The indazole derivatives are capable of bl
COMPOUNDS CONTAINING FUSED RINGS WHICH INHIBIT BETA-SECRETASE ACTIVITY AND METHODS OF USE THEREOF
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Page/Page column 82, (2011/11/01)
The invention provides novel beta-secretase inhibitors and methods for their use, including methods of treating Alzheimer's disease.
TETRAHYDROQUINOLINE DERIVATIVES AND THEIR PHARMACEUTICAL USE
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Page/Page column 72-73, (2011/06/11)
Tetrahydroquinoline compounds of Formula (I) and salts thereof, pharmaceutical compositions containing such compounds and their use in therapy.
Oxadiazolylindazole sodium channel modulators are neuroprotective toward hippocampal neurones
Clutterbuck, Lisa A.,Posada, Cristina Garcia,Visintin, Cristina,Riddall, Dieter R.,Lancaster, Barrie,Gane, Paul J.,Garthwaite, John,Selwood, David L.
experimental part, p. 2694 - 2707 (2010/03/03)
We report the discovery of a new class of neuroprotective voltage-dependent sodium channel modulators exemplified by (5-(1-benzyl-1H-indazol-3-yl)-1,2,4- oxadiazol-3-yl)methanamine 11 (CFM1178). The compounds were inhibitors of [ 14C]guanidiniu