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Selection, synthesis, and structure–activity relationship of tetrahydropyrido[4,3-d]pyrimidine-2,4-diones as human GnRH receptor antagonists by Marion C. Lanier; Miklos Feher; Neil J. Ashweek; Colin J. Loweth; Jaimie K. Rueter; Deborah H. Slee; John P. Williams; Yun-Fei Zhu; Susan K. Sullivan; Michael S. Brown is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.

What is Selection, synthesis, and structure–activity relationship of tetrahydropyrido[4,3-d]pyrimidine-2,4-diones as human GnRH receptor antagonists about?

The present article describes a selection of a new class of small molecule antagonists for the h-GnRH receptor, their preparation, and evaluation in vitro. Three computational methods were combined into a consensus score, to rank order virtual templates. The top 5% of templates were further evaluated in silico and assessed for novelty and synthetic accessibility. The tetrahydropyrido [4,3-d]pyrimidine-2,4-dione core was selected for synthesis and evaluated in vitro. Using an array approach for analog design and synthesis, we were able to drive the binding below 10 nM for the h-GnRH receptor after two rounds of optimization.

Who reads Selection, synthesis, and structure–activity relationship of tetrahydropyrido[4,3-d]pyrimidine-2,4-diones as human GnRH receptor antagonists?

Author

Marion C. Lanier; Miklos Feher; Neil J. Ashweek; Colin J. Loweth; Jaimie K. Rueter; Deborah H. Slee; John P. Williams; Yun-Fei Zhu; Susan K. Sullivan; Michael S. Brown

Publisher

Elsevier Science; Elsevier ; Elsevier Ltd.; Elsevier BV (ISSN 0968-0896)

Published

2007

Language

EN

Field

Biochemistry, Genetics and Molecular Biology (Life Sciences)