Molecules 2013, 18(4), 4487-4509; doi:10.3390/molecules18044487
Article

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

1 Pharmaceutical and Medicinal Chemistry, Saarland University, Campus C23, D-66123 Saarbr├╝cken, Germany 2 Helmholtz Institute for Pharmaceutical Research Saarland (HIPS), Campus C23, D-66123 Saarbr├╝cken, Germany
* Author to whom correspondence should be addressed.
Received: 22 March 2013; in revised form: 8 April 2013 / Accepted: 10 April 2013 / Published: 16 April 2013
(This article belongs to the Section Medicinal Chemistry)
PDF Full-text Download PDF Full-Text [418 KB, uploaded 16 April 2013 10:27 CEST]
Abstract: 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 17b-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.
Keywords: thieno[3,2-d]pyrimidinones; thieno[3,2-d]pyrimidines; quinazolinones; conformationally restricted analogues; enzyme inhibitors; 17b-hydroxysteroid dehydrogenase type 2; osteoporosis

Article Statistics

Load and display the download statistics.

Citations to this Article

Cite This Article

MDPI and ACS Style

Perspicace, E.; Marchais-Oberwinkler, S.; Hartmann, R.W. Synthesis and Biological Evaluation of Thieno[3,2-d]- pyrimidinones, Thieno[3,2-d]pyrimidines and Quinazolinones: Conformationally Restricted 17b-Hydroxysteroid Dehydrogenase Type 2 (17b-HSD2) Inhibitors. Molecules 2013, 18, 4487-4509.

AMA Style

Perspicace E, Marchais-Oberwinkler S, Hartmann RW. Synthesis and Biological Evaluation of Thieno[3,2-d]- pyrimidinones, Thieno[3,2-d]pyrimidines and Quinazolinones: Conformationally Restricted 17b-Hydroxysteroid Dehydrogenase Type 2 (17b-HSD2) Inhibitors. Molecules. 2013; 18(4):4487-4509.

Chicago/Turabian Style

Perspicace, Enrico; Marchais-Oberwinkler, Sandrine; Hartmann, Rolf W. 2013. "Synthesis and Biological Evaluation of Thieno[3,2-d]- pyrimidinones, Thieno[3,2-d]pyrimidines and Quinazolinones: Conformationally Restricted 17b-Hydroxysteroid Dehydrogenase Type 2 (17b-HSD2) Inhibitors." Molecules 18, no. 4: 4487-4509.

Molecules EISSN 1420-3049 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert