title: Novel interleukin-5 inhibitors based on hydroxyethylaminomethyl-4H-chromen-4-one scaffold.
abstract: Hydroxyethylaminomethyl-4H-chromenones were previously discovered as fairly strong IL-5 inhibitor. For determination of detail structure activity relationship, N-substituted hydroxyethylaminomethylchromenones 4a-n were prepared and evaluated for their IL-5 inhibitory activity. Shifting the hydrophobic group to nitrogen from 1-position of hydroxyethylamino moiety of hydroxyethylaminomethyl-4H-chromenones enhances the activity. The increment in bulkiness or hydrophobicity of alkyl side chain at amino group increases the activity. The same level of activity of 5-(cyclohexylmethoxy)-3-(N-benzyl-2-hydroxyethylaminomethyl)-4H-chromenone analogs regardless of hydrophobic or hydrophilic substituents at 4th position of phenyl ring might infer the existence of tunnel structure in the putative receptor for accepting these side chains.
authors.affiliation: College of Pharmacy and Institute of Drug Research and Development, Chungnam National University, Daejeon 305-764, Republic of Korea.
authors.forename: Cheonik
authors.initials: C
authors.lastname: Joo
authors.forename: Eeda
authors.initials: E
authors.lastname: Venkateswararao
authors.forename: Ki-Cheul
authors.initials: KC
authors.lastname: Lee
authors.forename: Vinay K
authors.initials: VK
authors.lastname: Sharma
authors.forename: Min-Sik
authors.initials: MS
authors.lastname: Kyung
authors.forename: Youngsoo
authors.initials: Y
authors.lastname: Kim
authors.forename: Sang-Hun
authors.initials: SH
authors.lastname: Jung
mesh_terms: D001249:Asthma / Q000188:drug therapy; D001578:Benzopyrans / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D015848:Interleukin-5 / Q000037:antagonists & inhibitors*; D008958:Models, Molecular; D013329:Structure-Activity Relationship
chemical_list: D001578:Benzopyrans; D015848:Interleukin-5