Details
| Original language | English |
|---|---|
| Article number | st-2015-b0058-l |
| Pages (from-to) | 1175-1178 |
| Number of pages | 4 |
| Journal | Synlett |
| Volume | 26 |
| Issue number | 9 |
| Publication status | Published - 2 Jun 2015 |
Abstract
Abstract The first total synthesis of cystobactamid 507, a member of a class of new natural products with strong inhibitory activity towards bacterial topoisomerases, is reported. Synthetic key challenges are the central tetrasubstitued arene and the low chemical reactivity of anilines and ortho-phenolic and isopropoxy-substituted benzoic acids. Biological evaluations demonstrate that cystobactamid 507 inhibits several Gram-positive pathogens but at significantly lower concentrations than described for the larger members of this natural product family.
Keywords
- amides, antibiotics, medicinal chemistry, natural products, total synthesis
ASJC Scopus subject areas
- Chemistry(all)
- Organic Chemistry
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In: Synlett, Vol. 26, No. 9, st-2015-b0058-l, 02.06.2015, p. 1175-1178.
Research output: Contribution to journal › Article › Research › peer review
}
TY - JOUR
T1 - Synthesis and biological evaluation of cystobactamid 507
T2 - A bacterial topoisomerase inhibitor from Cystobacter sp.
AU - Moreno, María
AU - Elgaher, Walid A.M.
AU - Herrmann, Jennifer
AU - Schläger, Nadin
AU - Hamed, Mostafa M.
AU - Baumann, Sascha
AU - Müller, Rolf
AU - Hartmann, Rolf W.
AU - Kirschning, Andreas
PY - 2015/6/2
Y1 - 2015/6/2
N2 - Abstract The first total synthesis of cystobactamid 507, a member of a class of new natural products with strong inhibitory activity towards bacterial topoisomerases, is reported. Synthetic key challenges are the central tetrasubstitued arene and the low chemical reactivity of anilines and ortho-phenolic and isopropoxy-substituted benzoic acids. Biological evaluations demonstrate that cystobactamid 507 inhibits several Gram-positive pathogens but at significantly lower concentrations than described for the larger members of this natural product family.
AB - Abstract The first total synthesis of cystobactamid 507, a member of a class of new natural products with strong inhibitory activity towards bacterial topoisomerases, is reported. Synthetic key challenges are the central tetrasubstitued arene and the low chemical reactivity of anilines and ortho-phenolic and isopropoxy-substituted benzoic acids. Biological evaluations demonstrate that cystobactamid 507 inhibits several Gram-positive pathogens but at significantly lower concentrations than described for the larger members of this natural product family.
KW - amides
KW - antibiotics
KW - medicinal chemistry
KW - natural products
KW - total synthesis
UR - http://www.scopus.com/inward/record.url?scp=84929944325&partnerID=8YFLogxK
U2 - 10.1055/s-0034-1380509
DO - 10.1055/s-0034-1380509
M3 - Article
AN - SCOPUS:84929944325
VL - 26
SP - 1175
EP - 1178
JO - Synlett
JF - Synlett
SN - 0936-5214
IS - 9
M1 - st-2015-b0058-l
ER -