title: Synthesis of imidazopyridines and purines as potent inhibitors of leukotriene A4 hydrolase.
abstract: The synthesis and biological evaluation of a series of heterocyclic analogues of the previously reported LTA(4) hydrolase inhibitor 1b are described. Imidazopyridine and purine analogues are specifically highlighted with several demonstrating excellent potency in our in vitro assays, as well as good oral activity in a mouse ex vivo assay.
authors.affiliation: Department of Medicinal Chemistry, Pharmacia Corporation, 4901 Searle Parkway, Skokie, IL 60077, USA. thomas.d.penning@pharmacia.com
authors.forename: Thomas D
authors.initials: TD
authors.lastname: Penning
authors.forename: Nizal S
authors.initials: NS
authors.lastname: Chandrakumar
authors.forename: Bipin N
authors.initials: BN
authors.lastname: Desai
authors.forename: Stevan W
authors.initials: SW
authors.lastname: Djuric
authors.forename: Alan F
authors.initials: AF
authors.lastname: Gasiecki
authors.forename: James W
authors.initials: JW
authors.lastname: Malecha
authors.forename: Julie M
authors.initials: JM
authors.lastname: Miyashiro
authors.forename: Mark A
authors.initials: MA
authors.lastname: Russell
authors.forename: Leslie J
authors.initials: LJ
authors.lastname: Askonas
authors.forename: James K
authors.initials: JK
authors.lastname: Gierse
authors.forename: Elizabeth I
authors.initials: EI
authors.lastname: Harding
authors.forename: Maureen K
authors.initials: MK
authors.lastname: Highkin
authors.forename: James F
authors.initials: JF
authors.lastname: Kachur
authors.forename: Suzanne H
authors.initials: SH
authors.lastname: Kim
authors.forename: Doreen
authors.initials: D
authors.lastname: Villani-Price
authors.forename: E Yvonne
authors.initials: EY
authors.lastname: Pyla
authors.forename: Nayereh S
authors.initials: NS
authors.lastname: Ghoreishi-Haack
authors.forename: Walter G
authors.initials: WG
authors.lastname: Smith
mesh_terms: D000818:Animals; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D004851:Epoxide Hydrolases / Q000037:antagonists & inhibitors* / Q000097:blood; D006571:Heterocyclic Compounds / Q000138:chemical synthesis / Q000494:pharmacology; D006801:Humans; D066298:In Vitro Techniques; D007202:Indicators and Reagents; D051379:Mice; D011687:Purines / Q000138:chemical synthesis* / Q000494:pharmacology*; D011725:Pyridines / Q000138:chemical synthesis* / Q000494:pharmacology*; D011994:Recombinant Proteins / Q000037:antagonists & inhibitors; D013329:Structure-Activity Relationship
chemical_list: D004791:Enzyme Inhibitors; D006571:Heterocyclic Compounds; D007202:Indicators and Reagents; D011687:Purines; D011725:Pyridines; D011994:Recombinant Proteins; D004851:Epoxide Hydrolases; C043134:leukotriene A4 hydrolase