title: Novel 1-alkynyl substituted 1,2-dihydroquinoline derivatives from nimesulide (and their 2-oxo analogues): a new strategy to identify inhibitors of PDE4B.
abstract: A number of novel 1-(3-arylprop-2-ynyl) substituted 1,2-dihydroquinoline derivatives related to nimesulide and their 2-oxo analogues have been designed as potential inhibitors of PDE4. All these compounds were synthesized by using Sonogashira coupling as a key step. In vitro PDE4B inhibitory properties and molecular modeling studies of some of the compounds synthesized are presented.
authors.affiliation: Department of Chemistry, MNR Degree and PG College, Kukatpally, Hyderabad, India. sarbani277@yahoo.com
authors.forename: Sarbani
authors.initials: S
authors.lastname: Pal
authors.forename: Shylaprasad
authors.initials: S
authors.lastname: Durgadas
authors.forename: Suresh Babu
authors.initials: SB
authors.lastname: Nallapati
authors.forename: Khagga
authors.initials: K
authors.lastname: Mukkanti
authors.forename: Ravikumar
authors.initials: R
authors.lastname: Kapavarapu
authors.forename: Chandana Lakshmi T
authors.initials: CL
authors.lastname: Meda
authors.forename: Kishore V L
authors.initials: KV
authors.lastname: Parsa
authors.forename: Manojit
authors.initials: M
authors.lastname: Pal
mesh_terms: D020134:Catalytic Domain; D054703:Cyclic Nucleotide Phosphodiesterases, Type 4 / Q000737:chemistry / Q000187:drug effects*; D008958:Models, Molecular; D058988:Phosphodiesterase 4 Inhibitors / Q000494:pharmacology*; D011804:Quinolines / Q000737:chemistry / Q000494:pharmacology*; D013449:Sulfonamides / Q000737:chemistry*
chemical_list: D058988:Phosphodiesterase 4 Inhibitors; D011804:Quinolines; D013449:Sulfonamides; D054703:Cyclic Nucleotide Phosphodiesterases, Type 4; C517360:PDE4B protein, human; C012655:nimesulide