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To develop new drugs for treatment of Alzheimer's disease, a group of N'-2-(4-Benzylpiperidin-/piperazin-1-yl)acylhydrazones was designed, synthesized and tested for their ability to inhibit acetylcholinesterase, butyrylcholinesterase and aggregation of amyloid beta peptides (1-40, 1-42 and 1-40_1-42). The enzyme inhibition assay results indicated that… (More)
In this study, new isoxazolo[4,5-d]pyridazin-4(5H)-one derivatives having an N-acylhydrazone moiety were synthesized. The compounds were tested for their COX inhibitory activities using NS-398 and indomethacine as reference compounds. Although the compounds had an inhibitory profile against both COX-1 and COX-2, most were found to be more selective against… (More)
Some new thiazolo[3,2-a]pyrimidine derivatives were prepared refluxing 2-thioxo-1,2,3,4-tetrahydropyrimidine derivatives with phenacyl bromide in glacial acetic acid. Calcium antagonistic activities of these compounds were evaluated in K(+)-depolarized rat aorta, using nifedipine as reference compound.
In this study, twenty-five new 6-methyl-4,5-dihydropyridazin-3(2H)-one derivatives having N-acylhydrazone and thiosemicarbazide moieties were synthesized. The target compounds were tested for their antimycobacterial activity in vitro against Mycobacterium tuberculosis H37Rv using the agar dilution method. Among the synthesized compounds,… (More)
Some thiazolo[4,5-d]pyrimidine-7(6H)-one derivatives were evaluated in vivo for their analgesic and anti-inflammatory activities. The results were compared with that of acetyl salicylic acid and phenylbutazone. Compounds 3b and 3h were the most active in the anti-inflammatory paw edema inhibition test. In terms of the analgesic activity (acetic acid… (More)
In this study, compounds with a 7-[2-(dihydro-5-substituted 6-thioxo-2H-1,3,5-thiadiazine-3[4H]-yl)-2-phenyl]acetamido-3 -methyl-3- cephem-4-carboxylic acid structure were synthesized by reacting cephalexin monohydrate with formaldehyde and dithiocarbamic acid salts prepared from some primary amines. The structure of the compounds was confirmed by spectral… (More)
This study describes the synthesis, pharmacological evaluation, including acetylcholinesterase (AChE)/butyrylcholinesterase (BChE) inhibition, amyloid beta (Aβ) antiaggregation, and neuroprotective effects, as well as molecular modeling of novel 2-(4-substituted phenyl)-1H-benzimidazole derivatives. These derivatives were synthesized by cyclization of… (More)
The synthesis of a series of thiazolo[3,2-a]pyrimidine derivatives were described. The structures of the compounds were elucidated by IR, 1H-NMR, 13C and elementary analysis. The compounds were evaluated for their calcium antagonistic activities using nifedipine as standard compound. All of the compounds were found to be less potent than nifedipine.
In this study, by starting from ethyl 4-amino-2,3-dihydro-3-methyl-2-thioxothiazole-5-carboxylate (1), the compounds having 2,3-dihydro-3-methyl-5-mercapto-6-methyl/ethyl-2- thioxothiazolo[4,5-d]pyrimidin-7(6H)-one (2a, 2b) structure and their 5-(4'-nonsubstituted/-substituted benzoylmethyl)thio derivatives (3a-h) were synthesized. The chemical structures… (More)
Eleven new 7-[2-(dihydro-5-substituted-6-thioxo-2H-1,3,5-thiadiazine-3( 4H)-yl)-2- (4-hydroxyphenyl)acetamido]-3-methyl-3-cephem-4-carboxylic acid derivatives were synthesized by the reaction of cefadroxil monohydrate, formaldehyde and substituted potassium dithiocarbamate. Their structures have been elucidated by spectral data and elementary analysis. The… (More)