Afabicin dephosphono

Synonym(s): Debio 1452  |  Debio1452  |  AFN-1252  |  Afabicin

Class: Fatty acid synthesis inhibitor (FabI inhibitor)

Spectrum of activity:	Gram-positive
Details of activity:	Inhibits FabI, which determines the completing of each cycle of elongation in the fatty acid synthesis. Active against Staphylococcus only.
Propensity to select resistant mutants:	Yes
Institute where first reported:	Debiopharm Group, Switzerland
Year first mentioned:	2014
Highest developmental phase:	Phase 2 (NCT03723551)
Development status:	Active

Chemical structure(s):
Canonical SMILES:	CC1=C(CN(C)C(=O)/C=C/C2=CN=C3C(=C2)CCC(=O)N3)OC4=C1C=CC=C4
Isomeric SMILES:	CC1=C(OC2=CC=CC=C12)CN(C)C(=O)/C=C/C3=CC4=C(NC(=O)CC4)N=C3
InChI:	InChI=1S/C22H21N3O3/c1-14-17-5-3-4-6-18(17)28-19(14)13-25(2)21(27)10-7-15-11-16-8-9-20(26)24-22(16)23-12-15/h3-7,10-12H,8-9,13H2,1-2H3,(H,23,24,26)/b10-7+
InChI Key:	QXTWSUQCXCWEHF-JXMROGBWSA-N
Structure link:	https://pubchem.ncbi.nlm.nih.gov/compound/10407120

External links:
Guide to Pharmacology:	DEBIO 1452
Main Source:	https://www.debiopharm.com/debiopharm-international/pipeline/debio1450-bone-joint-infections/
Citations:	http://aac.asm.org/content/59/5/2583.long https://www.debiopharm.com/our-business/pipeline/item/3548-debiopharm-international-sa-initiates-clinical-phase-ii-study-evaluating-debio-1450-in-staphylococcal-skin-infections.html https://www.ncbi.nlm.nih.gov/pubmed/25691627