Corrêa, Ivan R.; Nören-Müller, Andrea; Ambrosi, Horst-Dieter; Jakupovic, Sven; Saxena, Krishna; Schwalbe, Harald; Kaiser, Markus; Waldmann, Herbert:
Identification of inhibitors for mycobacterial protein tyrosine phosphatase B (MptpB) by biology-oriented synthesis (BIOS).
In: Chemistry : An Asian Journal, Vol. 2 (2007), No. 9, pp. 1109 - 1126
2007article/chapter in journal
Biology
Related: 1 publication(s)
Title:
Identification of inhibitors for mycobacterial protein tyrosine phosphatase B (MptpB) by biology-oriented synthesis (BIOS).
Author:
Corrêa, Ivan R.;Nören-Müller, Andrea;Ambrosi, Horst-Dieter;Jakupovic, Sven;Saxena, Krishna;Schwalbe, Harald;Kaiser, MarkusUDE
LSF ID
52590
ORCID
0000-0002-6540-8520ORCID iD
Other
connected with university
;
Waldmann, Herbert
Year of publication:
2007

Abstract:

Protein phosphatases have recently emerged as important targets for research in chemical biology and medicinal chemistry, and new classes of phosphatase inhibitors are in high demand. BIOS (biology-oriented synthesis) employs the criteria of relevance to nature and biological prevalidation for the design and synthesis of compound collections. In an application of the BIOS principle, an efficient solid-phase synthesis of highly substituted indolo[2,3-a]quinolizidines by using a vinylogous Mannich–Michael reaction in combination with phosgene- or acid-mediated ring closure was developed. Screening of this library for phosphatase inhibitors yielded a new inhibitor class for the Mycobacterium tuberculosis phosphatase MptpB.