- Design, synthesis and cytotoxic evaluation of a library of oxadiazole-containing hybrids
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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
- 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.
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p. 29741 - 29751
(2021/10/07)
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- Exploring Heteroaromatic Rings as a Replacement for the Labile Amide of Antiplasmodial Pantothenamides
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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.
- 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
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p. 4478 - 4497
(2021/05/04)
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- Preparation method and intermediate of benzodiazepine compound
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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
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- Five-membered heterocycle substitutive N-alkenamides WNT pathway inhibitor
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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.
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Paragraph 0076; 0077; 0078; 0079
(2017/08/29)
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- OXADIAZOLE COMPOUNDS WHICH INHIBIT BETA-SECRETASE ACTIVITY AND METHODS OF USE THEREOF
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The invention provides novel beta-secretase inhibitors and methods for their including methods of treating Alzheimer's disease.
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Page/Page column 83
(2012/05/05)
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- Tetrahydroquinoline Derivatives And Their Pharmaceutical Use
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Tetrahydroquinoline compounds of formula (I) and salts thereof, pharmaceutical compositions containing such compounds and their use in therapy.
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Page/Page column 32
(2012/08/28)
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- COMPOUNDS CONTAINING FUSED RINGS WHICH INHIBIT BETA-SECRETASE ACTIVITY AND METHODS OF USE THEREOF
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The invention provides novel beta-secretase inhibitors and methods for their use, including methods of treating Alzheimer's disease.
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Page/Page column 82
(2011/11/01)
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- TETRAHYDROQUINOLINE DERIVATIVES AND THEIR PHARMACEUTICAL USE
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Tetrahydroquinoline compounds of Formula (I) and salts thereof, pharmaceutical compositions containing such compounds and their use in therapy.
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Page/Page column 72-73
(2011/06/11)
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- INDAZOLE DERIVATIVES AND THEIR USE FOR BLOCKADING VOLTAGE DEPENDENT SODIUM CHANNELS
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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
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Page/Page column 24
(2011/06/19)
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- (3-HYDROXY-4-AMINO-BUTAN-2-YL) -3- (2-THIAZOL-2-YL-PYRROLIDINE-1-CARBONYL) BENZAMIDE DERIVATIVES AND RELATED COMPOUNDS AS BETA-SECRETASE INHIBITORS FOR TREATING
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The present invention provides novel beta-secretase inhibitors and methods for their use, including methods of treating of Alzheimer's disease. (Formula)
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Page/Page column 97
(2009/05/29)
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- Oxadiazolylindazole sodium channel modulators are neuroprotective toward hippocampal neurones
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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
- Clutterbuck, Lisa A.,Posada, Cristina Garcia,Visintin, Cristina,Riddall, Dieter R.,Lancaster, Barrie,Gane, Paul J.,Garthwaite, John,Selwood, David L.
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experimental part
p. 2694 - 2707
(2010/03/03)
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- NOVEL HETEROARYL CARBOXAMIDES
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The invention is concerned with novel heteroaryl carboxamides of formula (I) wherein A, R1, R2, X, Y, Z and m are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit the coagulation factor Xa and can be used for the treatment or prevention of thrombotic disorders.
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Page/Page column 7
(2008/06/13)
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- PYRIDINONYL PDK1 INHIBITORS
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The present invention provides pyridinonyl PDKl inhibitors and methods of treating cancer using the same.
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Page/Page column 78
(2008/06/13)
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- Synthesis of 1,2,4-oxadiazole-linked orthogonally urethane-protected dipeptide mimetics
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The synthesis of a new class of 1,2,4-oxadiazole-linked orthogonally urethane-protected dipeptide mimetics is described. The protocol employs a reaction between an N-protected amino acyl fluoride and an amino acid-derived amidoxime. All the three commonly
- Sureshbabu, Vommina V.,Hemantha, Hosahalli P.,Naik, Shankar A.
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p. 5133 - 5136
(2008/12/20)
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- NOVEL COMPOUNDS
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Compounds of formula (I) wherein: R1 represents substituted or unsubstituted heteroaryl; Y represents -(CRnaRnb)n-; Rna and Rnb are each independently hydrogen or C1-6alkyl; n is an integer from 0 to 5;R2 represents unsubstituted or substituted aryl or un
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Page/Page column 47
(2008/06/13)
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