Substituted propanolamines and alkylamines derived from fluoxetine as potent appetite suppressants.
A series of propanolamine and alkylamine analogues of fluoxetine (7-26, 28-31) were synthesized and assessed for their anorexigenic and antidepressant activities. Effect of various substituents at C-4 aryl position of fluoxetine has also been studied. Most of the propanolamine analogues (7-13, 16-26) displayed significant anorexigenic activity but interestingly they were devoid of antidepressant activity whereas anorexigenic as well as antidepressant activity was retained in the alkylamine series (28-31). Compounds 10 and 26 emerged as the most active compound and anorexigenic activity was better (83.67% and 82.45%) compared to fluoxetine (81.25%).
Bhandari
Kalpana
K
Medicinal and Process Chemistry Division, Central Drug Research Institute, Lucknow 226 001, India. bhandarikalpana@rediffmail.com
Srivastava
Shipra
S
Shanker
Girija
G
Nath
Chandishwar
C
D000818:Animals; D001067:Appetite Depressants / Q000737:chemistry / Q000494:pharmacology*; D005260:Female; D005473:Fluoxetine / Q000737:chemistry / Q000494:pharmacology*; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D051379:Mice; D011412:Propanolamines / Q000737:chemistry / Q000494:pharmacology*; D016339:Spectrometry, Mass, Fast Atom Bombardment; D013055:Spectrophotometry, Infrared
D001067:Appetite Depressants; D011412:Propanolamines; D005473:Fluoxetine