Synthesis, antibacterial and anticonvulsant evaluations of some cyclic enaminones.
Several cyclic enaminone esters were synthesized, characterized, and evaluated for anticonvulsant and antibacterial activities using standardized tests. A series of enaminones were mainly phenyl analogs of anticonvulsant enaminones, while a second series comprised of compounds bearing the oxazolidinone pharmacophoric moiety found in the synthetic antibacterial linezolid. The enaminone ester bearing an unsubstituted anilino analog showed class 2 anticonvulsant activity. This represents a first report of an unsubstituted anilino enaminone with anticonvulsant activity. The enaminone esters gave interesting UV data, and four analogs displayed potent anticonvulsant activities, while another four compounds showed moderate anticonvulsant activities. Surprisingly, none of the enaminone esters had any significant antibacterial activity.
Edafiogho
Ivan O
IO
Faculty of Pharmacy, Kuwait University, P.O. Box 24923, Safat 13110, Kuwait. ivanoe@hsc.edu.kw
Phillips
Oludotun A
OA
Udo
Edet E
EE
Samuel
Santosh
S
Rethish
Beigy
B
D000588:Amines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000927:Anticonvulsants / Q000138:chemical synthesis* / Q000494:pharmacology*; D009682:Magnetic Resonance Spectroscopy; D013056:Spectrophotometry, Ultraviolet; D013329:Structure-Activity Relationship
D000588:Amines; D000900:Anti-Bacterial Agents; D000927:Anticonvulsants