Synthesis of some substituted 4 [3H] Quinazo-linones ofdiverse biological activities

The synthesis of 3-[[3-hydroxy-4-methoxyphenyl] and 3-[4-hydroxy-2-methylphenyl]-4[3H]-quinazolinone and their nitroanalogs 2 and 3 is described. Reaction of 2 and 3 with alkyl halides gave the alkoxy derivatives 4 and 7, reaction with alkyl or aryl isocyanates afforded the alkyl or aryl carbamoyloxy derivatives 5 and 8, while reaction with aldehydes yielded the 2-styryl derivatives 6 and 9. Refluxing 3 with secondary amines and formaldehyde produced mannich bases 10. Reaction of 3 with ethyl chloroacetate gave the ethyl phenoxyacetate 11 which upon refluxing with hydrazine hydrate yielded the acid hydrazide 12. Further reaction of 12 with aldehydes or isothiocyanates afforded the hydrazones 13 or the thiosemicarbazides 14, respectively. Cyclization of the latter with chloroacetic acid produced the thiazolidinones 15. Fifteen of the newly synthesized compounds were screened for tranquillizing, anticonvulsant and analgesic activities. Twelve of the tested compounds showed marked activities

Synthesis and antidepressant activity of some novel fluoxetine derivatives

The present work involves the synthesis of three series of novel fluoxetine derivatives in order to evaluate their potential as antidepr ess ants. The first series consists of 1 -methyl- 1-[3-phenyl-3-[4-trifluoromethylphenoxy]propyl]-3-substituted ureas 2a-c and thioureas as their bioisosters 3a-m which were prepared by reacting fluoxetine 1a with different isocyanates and isothiocyanates respectively. The second series N-acyl/aroyl-N-methyl-3-phenyl-3-[4-trifluoromethylphenoxy]-propylamines 4a-d were synthesized by refluxing 1a with acyl/aroyl chloride and trifluoroacetic anhydride. The third one, N-chloroacyl-fluoxetine 5a-c was obtained via the reaction of la with chloroacyl chloride. In addition to a propionitrile derivative 8 which was achieved by refluxing 1a with acrylonitrile. The twenty four final compounds were biologically screened throughout the work for their potential as serotonin reuptake inhibitors by measuring potentiation of 5-HTP induced neurotoxity and some as norepinephrine reuptake inhibitor by measuring yohimbine-induced mortality in mice to calculates-HTP/NE ratio as a parameter for selectivity to inhibit serotonin reuptake. Four compounds [3e, 3h, 3i, 5b] were found to be as potent as fluoxetine

Synthesis of some 1,3,4-oxadizolines and thiazolidinones of expected anti-bacterial activity

Reaction of the acid hydrazide [3] with different carbonyl compounds gave the corresponding hydrazones [4]. The oxadiazolines [5] were obtained by refluxing [4] with acetic anhydride. The thiazolidinones [6] were achieved by the cyclocondensation of [4] with mercaptoacetic acid. The antimicrobial activity was determined for eight representative compounds and some of them were active

Synthesis of certain 1,3,4-oxadiazole derivatives of expected anti-inflammatory activity

The synthesis of certain diclofenac acid hydrazones 2a-k is described. The delta 2-1,3,4-oxadiazoline-5-thione 4 is prepared by reacting diclofenac acid hydrazide 1 with carbon disulfide in ethanolic potassium hydroxide. Some thio ethers 5a-f and Mannich bases 6a-f are prepared from the 1,3,4-oxadiazole derivative 4 and tested for their analgetic antipyretic and antiinflammatory activities. The given structures are confirmed by microanalyses and spectral data

Synthesis and biological activity of certain antipyrine derivatives

4-hydroxyantipyrine 2 reacted with different 2-chloroacetonilides to give the corresponding antipyrinyl ethers 3. Also, 4-chloro acetylaminoantipyrin 4 treated with the potassium salt of some nonsteroidal antiinflammatory acids, the potassium salt of certain ureido acids and some hydroxylated compounds afforded compounds 5, 7 and 9, respectively. The structure of the products was confirmed by microanalysis and spectral data. Preliminary pharmacological testing showed that some of these new products have demonstrated analgetic antiinflammatory effects

Synthesis and anti-inflammatory activity of analogs of diclofenac

The synthesis of ester and amide derivarives of diclofenac is described. The structure of products was confirmed by elemental analyses and spectral data. As a preliminary report, representative members of these compounds have demonstrated marked analgesic, antipyretic and anti-inflammatory activities compared to diclofenac