Neuroprotective effects of 2-(2-thienyl) benzothiazoline on gross motor skill deficits in rotenone induced rat model of Parkinson's disease.

In elderly aged people, Parkinson's disease is reported as 2nd most prevailing neuro-degenerative disease. Presently benzothiazole derivatives are gaining attention after showing positive results in various animal models for the investigation of different motor-diseases. In Current work, the 2- (2 Thienyl)Benzothiazoline is synthesized and its therapeutic effect was evaluated against rotenone-induced Parkinson's disease. It was expected to obtain the positive results in the treatment because thiophen group has been successfully reported in various literature as effective agent in the treatment of cognitive and locomotory disease. So, we used a Parkinson's inducive compound rotenone and injectedit intraperitoneally. The dose that we were used was 1.5mg/kg and treatment proceeded for 8 days in rats as rotenone inhibit the functioning of mitochondrial complex I. Administration of 2- (2 Thienyl)Benzothiazoline (10mg/kg per day) was already started 15 days prior to rotenone dose injection. The effects of both pre-treatment and without pre-treatment of 2- (2 Thienyl)Benzothiazoline were assessed by the use of various motor parameters of behavior such as pole test and Kondziela's inverted screen test for checking muscular strength, whereas inclined plane test, open field test and Rota rod test for motor coordination. Pre-treatment with drug reversed the gross motor impairments which were produced by rotenone. We conclude that 2- (2 Thienyl)Benzothiazoline, like its other candidate drug also protects against destructive effects of the compound rotenone and itcan be used as beneficial drug against various neurodegenerative diseases.

New carbazole linked 1,2,3-triazoles as highly potent non-sugar α-glucosidase inhibitors.

In the present study, a series of new carbazole linked 1H-1,2,3-triazoles (2-27) were synthesized via click reaction of N-propargyl-9H-carbazole (1) and azides of appropriate acetophenones and heterocycles. Synthesized carbazole triazoles including 7, 9, 10, 19, 20, and 23-26 (IC50=0.8±0.01-100.8±3.6µM), exhibited several folds more potent α-glucosidase inhibitory in vitro activity as compared to standard drug, acarbose. Compounds 2-5, 7-13, and 17-27 did not show any cytotoxicity against 3T3 cell lines, except triazoles 6, and 14-16. Among the series, carbazole triazoles 23 (IC50=1.0±0.057µM) and 25 (IC50=0.8±0.01µM) were found to be most active, and could serve as an attractive building block in the search of new non-sugar derivatives as anti-diabetic agents.