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

1email, 1email and 1,2,* email
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)
Download PDF [418 KB, uploaded 18 June 2014]
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
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

Export to BibTeX |
EndNote


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