Thiazole and thiadiazole analogues as a novel class of adenosine receptor antagonists

Autor: de Groote M, Visser S, van Muijlwijk-Koezen Je, Adriaan P. IJzerman, Frijtag von Drabbe Künzel J, R C Vollinga, Henk Timmerman

Publikováno v: van Muijlwijk-Koezen, J E, Timmerman, H, Vollinga, R C, Frijtag von Drabbe Kunzel, F, de Groote, M, Visser, S & AP., IJ 2001, ' Thiazole and thiadiazole analogues as a novel class of adenosine receptor antagonists ', Journal of Medicinal Chemistry, vol. 44, pp. 749-762 . https://doi.org/10.1021/jm0003945
Journal of Medicinal Chemistry, 44, 749-762. American Chemical Society

Novel classes of heterocyclic compounds as adenosine antagonists were developed based on a template approach. Structure-affinity relationships revealed insights for extended knowledge of the receptor-ligand interaction. We replaced the bicyclic heter

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ded3174ba221a40d0913a49eb74277f2
https://doi.org/10.1021/jm0003945

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The Role of Water Networks in Phosphodiesterase Inhibitor Dissociation and Kinetic Selectivity.

Autor: Blaazer AR; Division of Medicinal Chemistry, Amsterdam Institute of Molecular and Life Sciences (AIMMS), Vrije Universiteit Amsterdam, De Boelelaan 1108, 1081 HZ, Amsterdam, The Netherlands.; Division of Innovations in Human Health & Life Sciences (iH2LS), Amsterdam Institute of Molecular and Life Sciences (AIMMS), Vrije Universiteit Amsterdam, De Boelelaan 1108, 1081 HZ, Amsterdam, The Netherlands., Singh AK; School of Biosciences, University of Kent, CT2 7NJ, Canterbury, UK.; Current address A.K.S.: Mahatma Gandhi Medical Advanced Research Institute (MGMARI), Sri Balaji Vidyapeeth (Deemed to be University), Puducherry, 607 402, India., Zara L; Division of Medicinal Chemistry, Amsterdam Institute of Molecular and Life Sciences (AIMMS), Vrije Universiteit Amsterdam, De Boelelaan 1108, 1081 HZ, Amsterdam, The Netherlands., Boronat P; Division of Medicinal Chemistry, Amsterdam Institute of Molecular and Life Sciences (AIMMS), Vrije Universiteit Amsterdam, De Boelelaan 1108, 1081 HZ, Amsterdam, The Netherlands., Bautista LJ; Division of Medicinal Chemistry, Amsterdam Institute of Molecular and Life Sciences (AIMMS), Vrije Universiteit Amsterdam, De Boelelaan 1108, 1081 HZ, Amsterdam, The Netherlands., Irving S; Charles River, Ingram Building, Parkwood Road, CT2 7NH, Canterbury, UK., Majewski M; Institut de Biomedicina de la Universitat de Barcelona (IBUB), University of Barcelona, Av. Joan XXIII 27, 08028, Barcelona, Spain., Barril X; Institut de Biomedicina de la Universitat de Barcelona (IBUB), University of Barcelona, Av. Joan XXIII 27, 08028, Barcelona, Spain.; Catalan Institution for Research and Advanced Studies (ICREA), Passeig Lluís Companys 23, 08010, Barcelona, Spain., Wijtmans M; Division of Medicinal Chemistry, Amsterdam Institute of Molecular and Life Sciences (AIMMS), Vrije Universiteit Amsterdam, De Boelelaan 1108, 1081 HZ, Amsterdam, The Netherlands., Danielson UH; Science for Life Laboratory, Department of Chemistry-BMC, Uppsala University, SE-75123, Uppsala, Sweden., Sterk GJ; Division of Medicinal Chemistry, Amsterdam Institute of Molecular and Life Sciences (AIMMS), Vrije Universiteit Amsterdam, De Boelelaan 1108, 1081 HZ, Amsterdam, The Netherlands., Leurs R; Division of Medicinal Chemistry, Amsterdam Institute of Molecular and Life Sciences (AIMMS), Vrije Universiteit Amsterdam, De Boelelaan 1108, 1081 HZ, Amsterdam, The Netherlands., van Muijlwijk-Koezen JE; Division of Innovations in Human Health & Life Sciences (iH2LS), Amsterdam Institute of Molecular and Life Sciences (AIMMS), Vrije Universiteit Amsterdam, De Boelelaan 1108, 1081 HZ, Amsterdam, The Netherlands., Brown DG; School of Biosciences, University of Kent, CT2 7NJ, Canterbury, UK., de Esch IJP; Division of Medicinal Chemistry, Amsterdam Institute of Molecular and Life Sciences (AIMMS), Vrije Universiteit Amsterdam, De Boelelaan 1108, 1081 HZ, Amsterdam, The Netherlands.

Publikováno v: ChemMedChem [ChemMedChem] 2024 Nov 18; Vol. 19 (22), pp. e202400417. Date of Electronic Publication: 2024 Sep 12.

Progress in Free Energy Perturbation: Options for Evolving Fragments.

Autor: Zara L; Division of Medicinal Chemistry, Amsterdam Institute of Molecular and Life Sciences (AIMMS), Faculty of Science, Vrije Universiteit Amsterdam, De Boelelaan 1108, 1081 HZ Amsterdam, The Netherlands., Efrém NL; Division of Medicinal Chemistry, Amsterdam Institute of Molecular and Life Sciences (AIMMS), Faculty of Science, Vrije Universiteit Amsterdam, De Boelelaan 1108, 1081 HZ Amsterdam, The Netherlands., van Muijlwijk-Koezen JE; Division of Medicinal Chemistry, Amsterdam Institute of Molecular and Life Sciences (AIMMS), Faculty of Science, Vrije Universiteit Amsterdam, De Boelelaan 1108, 1081 HZ Amsterdam, The Netherlands., de Esch IJP; Division of Medicinal Chemistry, Amsterdam Institute of Molecular and Life Sciences (AIMMS), Faculty of Science, Vrije Universiteit Amsterdam, De Boelelaan 1108, 1081 HZ Amsterdam, The Netherlands., Zarzycka B; Division of Medicinal Chemistry, Amsterdam Institute of Molecular and Life Sciences (AIMMS), Faculty of Science, Vrije Universiteit Amsterdam, De Boelelaan 1108, 1081 HZ Amsterdam, The Netherlands.. Electronic address: b.a.zarzycka@vu.nl.

Publikováno v: Drug discovery today. Technologies [Drug Discov Today Technol] 2021 Dec; Vol. 40, pp. 36-42. Date of Electronic Publication: 2021 Nov 18.