Výsledky vyhledávání - "Amelia Bitant"

Direct Comparison of (N)-Methanocarba and Ribose-Containing 2-Arylalkynyladenosine Derivatives as A3 Receptor Agonists

Autor: Harsha Rao, Veronica Salmaso, Amelia Bitant, Ryan G. Campbell, Zhan-Guo Gao, Dilip K. Tosh, John A. Auchampach, Kenneth A. Jacobson

Publikováno v: ACS Medicinal Chemistry Letters. 11:1935-1941

A side-by-side pharmacological comparison of ribose and (N)-methanocarba (bicyclo[3.1.0]hexane) nucleosides as A3AR agonists indicated that the bicyclic pseudoribose ring constraint provided higher affinity/selectivity at human and mouse A3AR. The me

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b74aaba4f484fd38ac7019484b68d0a0
https://doi.org/10.1021/acsmedchemlett.9b00637

Zobrazit plný text záznamu

Autor: Dilip K, Tosh, Veronica, Salmaso, Ryan G, Campbell, Harsha, Rao, Amelia, Bitant, Eline, Pottie, Christophe P, Stove, Naili, Liu, Oksana, Gavrilova, Zhan-Guo, Gao, John A, Auchampach, Kenneth A, Jacobson

Publikováno v: Eur J Med Chem

Following our study of 4′-truncated (N)-methanocarba-adenosine derivatives that displayed unusually high mouse (m) A(3)AR affinity, we incorporated dopamine-related N(6) substituents in the full agonist 5′-methylamide series. N(6)-(2-(4-Hydroxy-3

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::161420a7ac6615c0ab479813bf211958
https://pubmed.ncbi.nlm.nih.gov/34844790

Zobrazit plný text záznamu

Design and in Vivo Characterization of A1 Adenosine Receptor Agonists in the Native Ribose and Conformationally Constrained (N)-Methanocarba Series

Autor: Amy C. Rothwell, Zhan-Guo Gao, Julie A. Mattison, Philip Z. Mannes, Zhenzhong Cui, Harsha Rao, Marc L. Reitman, Oksana Gavrilova, Antonella Ciancetta, Amelia Bitant, Kelli L. Vaughan, Veronica Salmaso, Kenneth A. Jacobson, Dilip K. Tosh, John A. Auchampach, David I. Lieberman, Naili Liu

Publikováno v: Journal of Medicinal Chemistry. 62:1502-1522

(N)-Methanocarba ([3.1.0]bicyclohexyl) adenosines and corresponding ribosides were synthesized to identify novel A1 adenosine receptor (A1AR) agonists for CNS or peripheral applications. Human and mouse AR binding was determined to assess the constra

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::63b059795412fd1ec341a36c21121381
https://doi.org/10.1021/acs.jmedchem.8b01662

Zobrazit plný text záznamu

Truncated (N)-Methanocarba Nucleosides as Partial Agonists at Mouse and Human A

Autor: Dilip K, Tosh, Veronica, Salmaso, Harsha, Rao, Amelia, Bitant, Courtney L, Fisher, David I, Lieberman, Helmut, Vorbrüggen, Marc L, Reitman, Oksana, Gavrilova, Zhan-Guo, Gao, John A, Auchampach, Kenneth A, Jacobson

Publikováno v: J Med Chem

Dopamine-derived N(6)-substituents, compared to N(6)-(2-phenylethyl), in truncated (N)-methanocarba (bicyclo[3.1.0]hexyl) adenosines favored high A(3) adenosine receptor (AR) affinity/selectivity, e.g. C2-phenylethynyl analogue 15 (MRS7591, K(i) 10.9

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::39ab3dda627bedc9c650d51ef492d63a
https://pubmed.ncbi.nlm.nih.gov/32271569

Zobrazit plný text záznamu

A3 adenosine receptor agonists containing dopamine moieties for enhanced interspecies affinity

Autor: Zhan-Guo Gao, Naili Liu, Christophe P. Stove, Veronica Salmaso, Amelia Bitant, Eline Pottie, Oksana Gavrilova, Dilip K. Tosh, Kenneth A. Jacobson, Ryan G. Campbell, John A. Auchampach, Harsha Rao

Publikováno v: European Journal of Medicinal Chemistry. 228:113983

Following our study of 4′-truncated (N)-methanocarba-adenosine derivatives that displayed unusually high mouse (m) A3AR affinity, we incorporated dopamine-related N6 substituents in the full agonist 5′-methylamide series. N6-(2-(4-Hydroxy-3-metho

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f5169808804b245984ebdb92161b19e9
https://doi.org/10.1016/j.ejmech.2021.113983

Zobrazit plný text záznamu

Direct Comparison of (N)-Methanocarba and Ribose-Containing 2-Arylalkynyladenosine Derivatives as A

Autor: Dilip K, Tosh, Veronica, Salmaso, Harsha, Rao, Ryan, Campbell, Amelia, Bitant, Zhan-Guo, Gao, John A, Auchampach, Kenneth A, Jacobson

Publikováno v: ACS Med Chem Lett

[Image: see text] A side-by-side pharmacological comparison of ribose and (N)-methanocarba (bicyclo[3.1.0]hexane) nucleosides as A(3)AR agonists indicated that the bicyclic pseudoribose ring constraint provided higher affinity/selectivity at human an

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::66649d32e4a4340d609273e79ba12596
https://pubmed.ncbi.nlm.nih.gov/33062176

Zobrazit plný text záznamu

Structure activity relationship of 2-arylalkynyl-adenine derivatives as human A3 adenosine receptor antagonists

Autor: Kenneth A. Jacobson, John A. Auchampach, Jinha Yu, Young-Hwan Jung, Amelia Bitant, Antonella Ciancetta, Zhan-Guo Gao, Philip Z. Mannes, Sami S. Khaznadar, David I. Lieberman

Publikováno v: MedChemComm. 9:1920-1932

Recognition of nucleosides at adenosine receptors (ARs) is supported by multiple X-ray structures, but the structure of an adenine complex is unknown. We examined the selectivity of predicted A(1)AR and A(3)AR adenine antagonists that incorporated kn

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::83073a9376facca8e5f394008844a8f9
https://doi.org/10.1039/c8md00317c

Zobrazit plný text záznamu

Design and in Vivo Characterization of A

Autor: Dilip K, Tosh, Harsha, Rao, Amelia, Bitant, Veronica, Salmaso, Philip, Mannes, David I, Lieberman, Kelli L, Vaughan, Julie A, Mattison, Amy C, Rothwell, John A, Auchampach, Antonella, Ciancetta, Naili, Liu, Zhenzhong, Cui, Zhan-Guo, Gao, Marc L, Reitman, Oksana, Gavrilova, Kenneth A, Jacobson

Publikováno v: Journal of medicinal chemistry. 62(3)

(N)-Methanocarba ([3.1.0]bicyclohexyl) adenosines and corresponding ribosides were synthesized to identify novel A(1) adenosine receptor (A(1)AR) agonists for CNS or peripheral applications. Human and mouse AR binding was determined to assess the con

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::dd7ba6edbfd4ee5a129147461a67cdb6
https://pubmed.ncbi.nlm.nih.gov/30605331

Zobrazit plný text záznamu

Vyhledávací nástroje:

Upřesnit hledání