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Structure-activity relationships in a series of NPY Y5 antagonists: 3-amido-9-ethylcarbazoles, core-modified analogues and amide isosteres.

Abstract：

:Beginning with carbazole 1a, the amide and alkyl substituents were optimized to maintain potency while adding solubilizing groups. Efforts to replace the 3-amino-9-ethylcarbazole core, a known carcinogen, used the SAR generated in the carbazole series for guidance and led to the synthesis of a number of core-modified analogues. In addition, an isosteric series, in which the amide was replaced with an imidazole, was prepared. Two potent new series lacking the putative toxicophore were identified from these endeavors.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Hammond M,Elliott RL,Gillaspy ML,Hager DC,Hank RF,LaFlamme JA,Oliver RM,DaSilva-Jardine PA,Stevenson RW,Mack CM,Cassella JV

doi

10.1016/s0960-894x(03)00329-9

subject

Has Abstract

pub_date

2003-06-16 00:00:00

pages

1989-92

issue

12

eissn

0960-894X

issn

1464-3405

pii

S0960894X03003299

journal_volume

13

pub_type

杂志文章

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