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001-es BibID:	BIBFORM083480
035-os BibID:	(cikkazonosító)701 (WoS)000515384800271 (Scopus)85079216601
Első szerző:	Szennyes Eszter (vegyész)
Cím:	Synthesis of New Series of 2-C-(béta-D-glucopyranosyl)-Pyrimidines and Their Evaluation as Inhibitors of Some Glycoenzymes / Eszter Szennyes, Gyöngyi Gyémánt, László Somsák, Éva Bokor
Dátum:	2020
ISSN:	1420-3049
Megjegyzések:	Despite the substantial interest in C-glycosyl heterocycles as mimetics of biologically active native glycans, the appearance of C-glycopyranosyl derivatives of six-membered heterocycles, both in synthetic and biological contexts, is rather scarce. As part of our ongoing research program aimed at preparing hitherto barely known 2-C-glycopyranosyl pyrimidines, the goal of the present study was to synthesize new 5-mono- and multiply substituted derivatives of this compound class. Thus, 2-C-(β-D-glucopyranosyl)-5,6-disubstituted-pyrimidin-4(3H)-ones and 4-amino-2-C-(β-D-glucopyranosyl)-5,6-disubstituted-pyrimidines were prepared by base-mediated cyclocondensations of O-perbenzylated and O-unprotected C-(β-D-glucopyranosyl) formamidine hydrochlorides with methylenemalonic acid derivatives. The 2-C-(β-D-glucopyranosyl)-5-substituted-pyrimidines were obtained from the same amidine precursors upon treatment with vinamidinium salts. The deprotected derivatives of these pyrimidines were tested as inhibitors of some glycoenzymes. None of them showed inhibitory activity towards glycogen phosphorylase and α- and β-glucosidase enzymes, but some members of the sets exhibited moderate inhibition against bovine liver β-galactosidase.
Tárgyszavak:	Természettudományok Kémiai tudományok idegen nyelvű folyóiratközlemény külföldi lapban folyóiratcikk C-Glucopyranosyl derivative pyrimidine amidine glycoenzyme inhibitor
Megjelenés:	Molecules. - 25 : 3 (2020), p. 1-18. -
További szerzők:	Gyémánt Gyöngyi (1960-) (vegyész) Somsák László (1954-) (vegyész) Bokor Éva (1982-) (vegyész)
Pályázati támogatás:	NKFIH FK125067 Egyéb GINOP-2.3.2-15-2016-00008 GINOP GINOP-2.3.3-15-2016-00004 GINOP
Internet cím:	DOI Intézményi repozitóriumban (DEA) tárolt változat
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