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Items: 1 to 20 of 73

1.

Synthesis of New Series of 2-C-(β-D-glucopyranosyl)-Pyrimidines and Their Evaluation as Inhibitors of Some Glycoenzymes.

Szennyes E, Gyémánt G, Somsák L, Bokor É.

Molecules. 2020 Feb 6;25(3). pii: E701. doi: 10.3390/molecules25030701.

2.

Stereoselective Synthesis of Carbon-Sulfur-Bridged Glycomimetics by Photoinitiated Thiol-Ene Coupling Reactions.

Csávás M, Eszenyi D, Mező E, Lázár L, Debreczeni N, Tóth M, Somsák L, Borbás A.

Int J Mol Sci. 2020 Jan 16;21(2). pii: E573. doi: 10.3390/ijms21020573.

3.

Glucose-based spiro-oxathiazoles as in vivo anti-hyperglycemic agents through glycogen phosphorylase inhibition.

Goyard D, Kónya B, Czifrák K, Larini P, Demontrond F, Leroy J, Balzarin S, Tournier M, Tousch D, Petit P, Duret C, Maurel P, Docsa T, Gergely P, Somsák L, Praly JP, Azay-Milhau J, Vidal S.

Org Biomol Chem. 2020 Feb 7;18(5):931-940. doi: 10.1039/c9ob01190k. Epub 2020 Jan 10.

PMID:
31922157
4.

The architecture of hydrogen and sulfur σ-hole interactions explain differences in the inhibitory potency of C-β-d-glucopyranosyl thiazoles, imidazoles and an N-β-d glucopyranosyl tetrazole for human liver glycogen phosphorylase and offer new insights to structure-based design.

Kyriakis E, Karra AG, Papaioannou O, Solovou T, Skamnaki VT, Liggri PGV, Zographos SE, Szennyes E, Bokor É, Kun S, Psarra AG, Somsák L, Leonidas DD.

Bioorg Med Chem. 2020 Jan 1;28(1):115196. doi: 10.1016/j.bmc.2019.115196. Epub 2019 Nov 14.

PMID:
31767404
5.

Glucopyranosylidene-spiro-imidazolinones, a New Ring System: Synthesis and Evaluation as Glycogen Phosphorylase Inhibitors by Enzyme Kinetics and X-ray Crystallography.

Szabó KE, Kyriakis E, Psarra AG, Karra AG, Sipos Á, Docsa T, Stravodimos GA, Katsidou E, Skamnaki VT, Liggri PGV, Zographos SE, Mándi A, Király SB, Kurtán T, Leonidas DD, Somsák L.

J Med Chem. 2019 Jul 11;62(13):6116-6136. doi: 10.1021/acs.jmedchem.9b00356. Epub 2019 Jun 28.

PMID:
31251604
6.

Identification of C-β-d-Glucopyranosyl Azole-Type Inhibitors of Glycogen Phosphorylase That Reduce Glycogenolysis in Hepatocytes: In Silico Design, Synthesis, in Vitro Kinetics, and ex Vivo Studies.

Barr D, Szennyes E, Bokor É, Al-Oanzi ZH, Moffatt C, Kun S, Docsa T, Sipos Á, Davies MP, Mathomes RT, Snape TJ, Agius L, Somsák L, Hayes JM.

ACS Chem Biol. 2019 Jul 19;14(7):1460-1470. doi: 10.1021/acschembio.9b00172. Epub 2019 Jun 19.

PMID:
31243960
7.

Glucopyranosylidene-spiro-benzo[ b][1,4]oxazinones and -benzo[ b][1,4]thiazinones: Synthesis and Investigation of Their Effects on Glycogen Phosphorylase and Plant Growth Inhibition.

Kun S, Kánya N, Galó N, Páhi A, Mándi A, Kurtán T, Makleit P, Veres S, Sipos Á, Docsa T, Somsák L.

J Agric Food Chem. 2019 Jun 19;67(24):6884-6891. doi: 10.1021/acs.jafc.9b00443. Epub 2019 Jun 10.

PMID:
31135156
8.

Synthesis of C-β-d-glucopyranosyl derivatives of some fused azoles for the inhibition of glycogen phosphorylase.

Szennyes E, Bokor É, Docsa T, Sipos Á, Somsák L.

Carbohydr Res. 2019 Jan 15;472:33-41. doi: 10.1016/j.carres.2018.11.003. Epub 2018 Nov 7.

PMID:
30453096
9.

Synthesis of thiomaltooligosaccharides by a thio-click approach.

Lázár L, Borbás A, Somsák L.

Carbohydr Res. 2018 Dec;470:8-12. doi: 10.1016/j.carres.2018.09.005. Epub 2018 Sep 27.

PMID:
30286336
10.

Synthesis of New C- and N-β-d-Glucopyranosyl Derivatives of Imidazole, 1,2,3-Triazole and Tetrazole, and Their Evaluation as Inhibitors of Glycogen Phosphorylase.

Kun S, Bokor É, Sipos Á, Docsa T, Somsák L.

Molecules. 2018 Mar 15;23(3). pii: E666. doi: 10.3390/molecules23030666.

11.

Pd-catalyzed coupling reactions of anhydro-aldose tosylhydrazones with aryl bromides to produce substituted exo-glycals.

Kaszás T, Ivanov A, Tóth M, Ehlers P, Langer P, Somsák L.

Carbohydr Res. 2018 Aug;466:30-38. doi: 10.1016/j.carres.2018.02.010. Epub 2018 Feb 19.

PMID:
29499901
12.

Probing the β-pocket of the active site of human liver glycogen phosphorylase with 3-(C-β-d-glucopyranosyl)-5-(4-substituted-phenyl)-1, 2, 4-triazole inhibitors.

Kyriakis E, Solovou TGA, Kun S, Czifrák K, Szőcs B, Juhász L, Bokor É, Stravodimos GA, Kantsadi AL, Chatzileontiadou DSM, Skamnaki VT, Somsák L, Leonidas DD.

Bioorg Chem. 2018 Apr;77:485-493. doi: 10.1016/j.bioorg.2018.02.008. Epub 2018 Feb 12.

PMID:
29454281
13.

A multidisciplinary study of 3-(β-d-glucopyranosyl)-5-substituted-1,2,4-triazole derivatives as glycogen phosphorylase inhibitors: Computation, synthesis, crystallography and kinetics reveal new potent inhibitors.

Kun S, Begum J, Kyriakis E, Stamati ECV, Barkas TA, Szennyes E, Bokor É, Szabó KE, Stravodimos GA, Sipos Á, Docsa T, Gergely P, Moffatt C, Patraskaki MS, Kokolaki MC, Gkerdi A, Skamnaki VT, Leonidas DD, Somsák L, Hayes JM.

Eur J Med Chem. 2018 Mar 10;147:266-278. doi: 10.1016/j.ejmech.2018.01.095. Epub 2018 Feb 2.

PMID:
29453094
14.

Glucopyranosylidene-Spiro-Thiazolinones: Synthetic Studies and Determination of Absolute Configuration by TDDFT-ECD Calculations.

Szabó KE, Kun S, Mándi A, Kurtán T, Somsák L.

Molecules. 2017 Oct 19;22(10). pii: E1760. doi: 10.3390/molecules22101760.

15.

Nanomolar Inhibitors of Glycogen Phosphorylase Based on β-d-Glucosaminyl Heterocycles: A Combined Synthetic, Enzyme Kinetic, and Protein Crystallography Study.

Bokor É, Kyriakis E, Solovou TGA, Koppány C, Kantsadi AL, Szabó KE, Szakács A, Stravodimos GA, Docsa T, Skamnaki VT, Zographos SE, Gergely P, Leonidas DD, Somsák L.

J Med Chem. 2017 Nov 22;60(22):9251-9262. doi: 10.1021/acs.jmedchem.7b01056. Epub 2017 Oct 3.

PMID:
28925695
16.

van der Waals interactions govern C-β-d-glucopyranosyl triazoles' nM inhibitory potency in human liver glycogen phosphorylase.

Kantsadi AL, Stravodimos GA, Kyriakis E, Chatzileontiadou DSM, Solovou TGA, Kun S, Bokor É, Somsák L, Leonidas DD.

J Struct Biol. 2017 Jul;199(1):57-67. doi: 10.1016/j.jsb.2017.05.001. Epub 2017 May 5.

PMID:
28483603
17.

Glycogen phosphorylase inhibition improves beta cell function.

Nagy L, Márton J, Vida A, Kis G, Bokor É, Kun S, Gönczi M, Docsa T, Tóth A, Antal M, Gergely P, Csóka B, Pacher P, Somsák L, Bai P.

Br J Pharmacol. 2018 Jan;175(2):301-319. doi: 10.1111/bph.13819. Epub 2017 Jun 18.

18.

C-Glycopyranosyl Arenes and Hetarenes: Synthetic Methods and Bioactivity Focused on Antidiabetic Potential.

Bokor É, Kun S, Goyard D, Tóth M, Praly JP, Vidal S, Somsák L.

Chem Rev. 2017 Feb 8;117(3):1687-1764. doi: 10.1021/acs.chemrev.6b00475. Epub 2017 Jan 25. Review.

PMID:
28121130
19.

Synthetic, enzyme kinetic, and protein crystallographic studies of C-β-d-glucopyranosyl pyrroles and imidazoles reveal and explain low nanomolar inhibition of human liver glycogen phosphorylase.

Kantsadi AL, Bokor É, Kun S, Stravodimos GA, Chatzileontiadou DSM, Leonidas DD, Juhász-Tóth É, Szakács A, Batta G, Docsa T, Gergely P, Somsák L.

Eur J Med Chem. 2016 Nov 10;123:737-745. doi: 10.1016/j.ejmech.2016.06.049. Epub 2016 Jul 12.

PMID:
27522507
20.

C-Glucopyranosyl-1,2,4-triazol-5-ones: synthesis and inhibition of glycogen phosphorylase.

Bokor É, Széles Z, Docsa T, Gergely P, Somsák L.

Carbohydr Res. 2016 Jun 24;429:128-34. doi: 10.1016/j.carres.2015.12.005. Epub 2015 Dec 24.

PMID:
26818133

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