Identification of inhibitors for mycobacterial protein tyrosine phosphatase B (MptpB) by biology-oriented synthesis (BIOS).
In: Chemistry : An Asian Journal, Jg. 2 (2007), Heft 9, S. 1109 - 1126
Titel:
Identification of inhibitors for mycobacterial protein tyrosine phosphatase B (MptpB) by biology-oriented synthesis (BIOS).
Autor*in:
Corrêa, Ivan R.;Nören-Müller, Andrea;Ambrosi, Horst-Dieter;Jakupovic, Sven;Saxena, Krishna;Schwalbe, Harald;Kaiser, MarkusUDE
- LSF ID
- 52590
- ORCID
- 0000-0002-6540-8520
- Sonstiges
- der Hochschule zugeordnete*r Autor*in
Erscheinungsjahr:
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.