Synthesis and Biological Evaluation of Thieno[3,2-d]- pyrimidinones, Thieno[3,2-d]pyrimidines and Quinazolinones: Conformationally Restricted 17β-Hydroxysteroid Dehydrogenase Type 2 (17β-HSD2) Inhibitors

Molecules

Enrico Perspicace¹  Sandrine Marchais-Oberwinkler¹ 

[1] Pharmaceutical and Medicinal Chemistry, Saarland University, Campus C23, D-66123 Saarbrücken, Germany; E-Mails:

关键词: thieno[3;    2-d]pyrimidinones;    thieno[3;    2-d]pyrimidines;    quinazolinones;    conformationally restricted analogues;    enzyme inhibitors;    17β-hydroxysteroid dehydrogenase type 2;    osteoporosis;   

DOI  :  10.3390/molecules18044487

来源: mdpi

【 摘 要 】

In this study, a series of conformationally restricted thieno[3,2-d]pyrimidinones, thieno[3,2-d]pyrimidines and quinazolinones was designed and synthesized with the goal of improving the biological activity as 17β-hydroxysteroid dehydrogenase type 2 inhibitors of the corresponding amidothiophene derivatives. Two moderately active compounds were discovered and this allowed the identification of the biologically active open conformer as well as the extension of the enzyme binding site characterisation.

【 授权许可】

CC BY   
© 2013 by the authors; licensee MDPI, Basel, Switzerland.