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Identification of nicotinamide phosphoribosyltransferase (NAMPT) inhibitors with no evidence of CYP3A4 time-dependent inhibition and improved aqueous solubility.

Abstract：

:Herein we report the optimization efforts to ameliorate the potent CYP3A4 time-dependent inhibition (TDI) and low aqueous solubility exhibited by a previously identified lead compound from our NAMPT inhibitor program (1, GNE-617). Metabolite identification studies pinpointed the imidazopyridine moiety present in 1 as the likely source of the TDI signal, and replacement with other bicyclic systems was found to reduce or eliminate the TDI finding. A strategy of reducing the number of aromatic rings and/or lowering cLogD7.4 was then employed to significantly improve aqueous solubility. These efforts culminated in the discovery of 42, a compound with no evidence of TDI, improved aqueous solubility, and robust efficacy in tumor xenograft studies.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Zak M,Liederer BM,Sampath D,Yuen PW,Bair KW,Baumeister T,Buckmelter AJ,Clodfelter KH,Cheng E,Crocker L,Fu B,Han B,Li G,Ho YC,Lin J,Liu X,Ly J,O'Brien T,Reynolds DJ,Skelton N,Smith CC,Tay S,Wang W,Wang Z,Xi

doi

10.1016/j.bmcl.2014.12.026

subject

Has Abstract

pub_date

2015-02-01 00:00:00

pages

529-41

issue

3

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(14)01323-7

journal_volume

25

pub_type

杂志文章

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