title: Synthesis and different biological activities of novel benzoxazoles.
abstract: A series of 2-[4-(4-substitutedbenzamido/phenylacetamido/butanamido)phenyl]-5-ethylsulphonyl-benzoxazole derivatives were synthesized and biologically evaluated as possible antimicrobial agents and inhibitors of tyrosinase, acetylcholinesterase (AChE), and butyrylcholinesterase (BChE). The results demonstrated that the synthesized compounds exhibited a broad spectrum of activity with minimum inhibitory concentration (MIC) values of 128-16 μg/ml against some Gram-positive, Gram-negative bacteria as well as Candida albicans and C. krusei. The compound 10 displayed higher activity in this series against methicilline resistant Staphylococcus aureus (MRSA) with a MIC value of 16 μg/ml than the compared control drugs ampicillin and ceftriaxone. Compound 14 showed moderate tyrosinase inhibition, however, none of the compounds showed effect as inhibitor of AChE and BChE.
authors.affiliation: Department of Pharmaceutical Chemistry, Ankara University, Ankara, Turkey. temiz@pharmacy.ankara.edu.tr
authors.forename: O
authors.initials: O
authors.lastname: Temiz-Arpaci
authors.forename: B
authors.initials: B
authors.lastname: Eylem Cifcioglu Goztepe
authors.forename: Fatma
authors.initials: F
authors.lastname: Kaynak-Onurdag
authors.forename: Selda
authors.initials: S
authors.lastname: Ozgen
authors.forename: Fatma Sezer
authors.initials: FS
authors.lastname: Senol
authors.forename: I
authors.initials: I
authors.lastname: Erdogan Orhan
mesh_terms: D000110:Acetylcholinesterase / Q000378:metabolism; D000890:Anti-Infective Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D001426:Bacterial Proteins / Q000037:antagonists & inhibitors / Q000378:metabolism; D001583:Benzoxazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D002091:Butyrylcholinesterase / Q000378:metabolism; D002176:Candida albicans / Q000254:growth & development*; D002800:Cholinesterase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D005656:Fungal Proteins / Q000037:antagonists & inhibitors / Q000378:metabolism; D006090:Gram-Negative Bacteria / Q000254:growth & development*; D055624:Methicillin-Resistant Staphylococcus aureus / Q000254:growth & development*
chemical_list: D000890:Anti-Infective Agents; D001426:Bacterial Proteins; D001583:Benzoxazoles; D002800:Cholinesterase Inhibitors; D005656:Fungal Proteins; D000110:Acetylcholinesterase; D002091:Butyrylcholinesterase