Abstract
Equation Presented Vinylogous amides 5 and 6 have been synthesized from L-propargyl glycine and tested against diaminopimelate (DAP) enzymes involved in bacterial lysine biosynthesis. Both are reversible inhibitors of DAP D-dehydrogenase and DAP epimerase with IC50 values in the 500 μM range. Compound 5 shows competitive inhibition against the L-dihydrodipicolinate (DHDP) reductase with a Ki value of 32 μM, which is comparable to the planar dipicolinate 16 (Ki = 26 μM), the best known inhibitor of the enzyme.
Original language | English (US) |
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Pages (from-to) | 3857-3860 |
Number of pages | 4 |
Journal | Organic Letters |
Volume | 2 |
Issue number | 24 |
DOIs | |
State | Published - Nov 30 2000 |
ASJC Scopus subject areas
- Biochemistry
- Physical and Theoretical Chemistry
- Organic Chemistry