1373398-74-3Relevant academic research and scientific papers
Synthesis, characterization and drug-likeness predictions of 1,3-thiazole and benzothiazole derivatives
Naqvi, Arshi
, p. 3134 - 3139 (2018)
Heterocyclic compounds bearing nitrogen and sulphur in the main skeleton are reported to be a bioactive group. Thiazole and benzothiazole moieties are biologically significant class of this group. This research focus on the synthesis and characterization of 1,3-thiazole and benzothiazole derivatives. Drug likeness predictions were also undertaken for these newly synthesized compounds.
Synthesis and pharmacological screening of novel (2-(4-Methyl-2-oxo-2H- chromen-7-yloxy)-N-(benzo[d]thiazol-2-yl))acetamide derivatives
Gawai, Ashish,Das, Sanjib,Nemade, Mahesh,Wathore, Sandeep
experimental part, p. 3969 - 3974 (2012/01/13)
A new series of 2-(4-methyl-2-oxo-2H-chromen-7-yloxy)-N-(benzo[d]thiazol-2- yl)acetamide derivatives (4a-k) was synthesized and evaluated for their D 2 and 5HT2 antagonistic activity as a measure of atypical antipsychotic property. Compounds (4a-k) were synthesized by refluxing various N-(benzothiazol-2-yl)-2-chloroacetamides substituted derivatives (3a-k) with 7-hydroxy-4 methyl-2H-chromen-2-one (1) in acetonitrile and anhydrous K 2CO3. N-(Benzothiazol-2-yl)-2-chloroacetamides substituted derivatives (3a-k) were prepared from the chloroacetyl chloride with various 2-amino benzothiazole substituted derivatives (2a-k). The synthesized compounds were characterized with the help of spectral and analytical data. Most of these compounds showed dopamine D2 receptor antagonistic activity from moderate to high affinity along with serotonin 5-HT2 receptor blockage activity: a property that has been suggested as necessary for atypicality. The D 2 and 5-HT2 receptor blockage activity was evaluated by inhibition of apomorphine-induced climbing behaviour and 5HTP induced head twitches in mice, respectively.
