59367-09-8Relevant articles and documents
Multivalent Thiosialosides and Their Synergistic Interaction with Pathogenic Sialidases
Brissonnet, Yoan,Assailly, Coralie,Saumonneau, Amélie,Bouckaert, Julie,Maillasson, Mike,Petitot, Clémence,Roubinet, Benoit,Didak, Blanka,Landemarre, Ludovic,Bridot, Clarisse,Blossey, Ralf,Deniaud, David,Yan, Xibo,Bernard, Julien,Tellier, Charles,Grandjean, Cyrille,Daligault, Franck,Gouin, Sébastien G.
supporting information, p. 2358 - 2365 (2019/01/16)
Sialidases (SAs) hydrolyze sialyl residues from glycoconjugates of the eukaryotic cell surface and are virulence factors expressed by pathogenic bacteria, viruses, and parasites. The catalytic domains of SAs are often flanked with carbohydrate-binding module(s) previously shown to bind sialosides and to enhance enzymatic catalytic efficiency. Herein, non-hydrolyzable multivalent thiosialosides were designed as probes and inhibitors of V. cholerae, T. cruzi, and S. pneumoniae (NanA) sialidases. NanA was truncated from the catalytic and lectinic domains (NanA-L and NanA-C) to probe their respective roles upon interacting with sialylated surfaces and the synthetically designed di- and polymeric thiosialosides. The NanA-L domain was shown to fully drive NanA binding, improving affinity for the thiosialylated surface and compounds by more than two orders of magnitude. Importantly, each thiosialoside grafted onto the polymer was also shown to reduce NanA and NanA-C catalytic activity with efficiency that was 3000-fold higher than that of the monovalent thiosialoside reference. These results extend the concept of multivalency for designing potent bacterial and parasitic sialidase inhibitors.
Neuramindase Inhibitor
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Page/Page column 11, (2008/12/05)
There are provided a novel compound having irreversible inhibitory activity against neuraminidase, a therapeutic agent and a detection agent for a disease involving neuraminidase. A compound represented by the following formula (I) and a salt thereof, a production method thereof, and an application method thereof, wherein: A1 represents an aryl group optionally having a substituent group or a heteroaryl group optionally having a substituent group;A2 represents —CX2R6 or —CHXR6 wherein X represents —F, —Cl, —Br, or —I;R1 represents a hydrogen atom or an alkyl group optionally having a substituent group;R2, R3, R4, and R5 represent each independently —OC(═O)R6, —OR6, —N(R6)2, —N3, —NHC(═NH)NHR6, —NHCOR6, —OSO3R6, —OPO3(R6)2, F, Cl, Br, or I; andR6 represents each independently a hydrogen atom, an alkyl group optionally having a substituent group, an aryl group optionally having a substituent group, or an optionally substituted heteroaryl group.
Syntheses of alkenylated carbohydrate derivatives toward the preparation of monolayers on silicon surfaces
De Smet, Louis C.P.M.,Pukin, Aliaksei V.,Stork, Gerrit A.,De Vos, C.H. Ric,Visser, Gerben M.,Zuilhof, Han,Sudh?lter, Ernst J.R.
, p. 2599 - 2605 (2007/10/03)
This note describes the synthesis of different alkenylated carbohydrate derivatives suitable for direct attachment to hydrogen-terminated silicon surfaces. The derivatives were alkenylated at the C-1 position, while the remaining hydroxyl groups were protected. The development of such new carbohydrate-based sensing elements opens the access to new classes of biosensors.
