Sign in to use this feature.

Years

Between: -

Subjects

remove_circle_outline
remove_circle_outline

Journals

Article Types

Countries / Regions

Search Results (1)

Search Parameters:
Keywords = Terahydro-beta-carboline

Order results
Result details
Results per page
Select all
Export citation of selected articles as:
19 pages, 3478 KB  
Article
Structure-Based Design of Novel Tetrahydro-Beta-Carboline Derivatives with a Hydrophilic Side Chain as Potential Phosphodiesterase Inhibitors
by Ahmed K. Elhady, Sara C. Sigler, Nazih Noureldin, Joshua C. Canzoneri, Nermin S. Ahmed, Gary A. Piazza and Ashraf H. Abadi
Sci. Pharm. 2016, 84(3), 428-446; https://doi.org/10.3390/scipharm84030428 - 26 Sep 2015
Cited by 7 | Viewed by 4276
Abstract
Tadalafil is a clinically approved phosphodiesterase-5 inhibitor for the treatment of erectile dysfunction and pulmonary arterial hypertension. It contains two chiral carbons, and the marketed isomer is the 6R, 12aR isomer with a methyl substituent on the terminal nitrogen of the piperazinedione [...] Read more.
Tadalafil is a clinically approved phosphodiesterase-5 inhibitor for the treatment of erectile dysfunction and pulmonary arterial hypertension. It contains two chiral carbons, and the marketed isomer is the 6R, 12aR isomer with a methyl substituent on the terminal nitrogen of the piperazinedione ring. In this report, tadalafil analogues with an extended hydrophilic side chain on the piperazine nitrogen were designed to interact with particular hydrophilic residues in the binding pocket. This leads to analogues with moderate inhibitory activity on phosphodiesterase-5, even for isomers in which chiral carbons are of the S configuration. Full article
Show Figures

Figure 1

Back to TopTop