1.
Bioorg Med Chem Lett
; 30(15): 127279, 2020 08 01.
Article
in English
| MEDLINE
| ID: mdl-32527459
ABSTRACT
The synthesis and structure activity relationship development of a pyrimidine series of heterocyclic Factor IXa inhibitors is described. Increased selectivity over Factor Xa inhibition was achieved through SAR expansion of the P1 element. Select compounds were evaluated in vivo to assess their plasma levels in rat.
Subject(s)
Drug Discovery , Factor IXa/antagonists & inhibitors , Factor Xa Inhibitors/pharmacology , Pyrimidines/pharmacology , Dose-Response Relationship, Drug , Factor IXa/metabolism , Factor Xa Inhibitors/chemical synthesis , Factor Xa Inhibitors/chemistry , Humans , Molecular Structure , Pyrimidines/chemical synthesis , Pyrimidines/chemistry , Structure-Activity Relationship
2.
Tetrahedron
; 69(29): 5829-5840, 2013 Jul 22.
Article
in English
| MEDLINE
| ID: mdl-23894213
ABSTRACT
The preparation of an indole appended vinamidinium salt, an indole appended vinylogous amide and an indole appended chloroenal are described. The subsequent regiospecific conversion of these indole containing building blocks to functionalized pyrazoles and pyrroles is detailed.