No abstract

No abstract

<p class="Abstract">Diazotization of substituted anilines with NaNO₂ and concentrated hydro-chloric acid at 0ºC gave the diazonium chlorides. Coupling of substituted aryl diazonium chlorides with ethyl acetoacetate in methanol gave ethyl-2-aryl-hydrazono-3-oxobutyrates (2a-h). Reaction of (2a-h) with naphthoic carbohydrazide (3) gave the title compounds pyrazolone derivatives (4a-h). The newly synthesized compounds were screened for their in vivo anti-depressant activity by tail suspension test and forced swimming test. Some of the tested compounds 4f, 4g showed very good activity when compared to the standard drug imipramine. The newly synthesized compounds were characterized by physical parameters and the structures were elucidated by spectral data.</p><p><strong>Video Clips</strong></p><p><a href="https://www.youtube.com/v/TZtb2a5u4CU">Forced swimming test</a>: 12 min 19 sec</p><p><a href="https://www.youtube.com/v/92mFRfBJgBw">Tail suspension test</a>: 8 min 5 sec</p><p> </p>

Fourteen novel [1,2,4]triazolo[3,4‐b][1,3,4]thiadiazine derivatives bearing benzimidazole moiety (7a‐n) have been synthesized using the one‐pot nitro reductive cyclization method. All the synthesized compounds were confirmed by 1H nuclear magnetic resonance (1H NMR), 13C NMR, fourier‐transform infrared (FT‐IR), mass spectrum, and elemental analyses. All the title compounds were subjected to in vitro antioxidant activity. The free radical scavenging activity of the compounds was examined using DPPH, nitric oxide, and superoxide radical scavenging methods. The results demonstrated that compound 3‐(2‐(3,4‐dimethoxyphenyl)‐1‐propyl‐1H‐benzo[d]imidazol‐5‐yl)‐6‐4‐tolyl‐7H‐[1,2,4]triazolo[3,4‐b][1,3,4]thiadiazine (7c) was potent in scavenging both DPPH and nitric oxide radical with IC50 values of 13.57 and 18.55 μg/ml when compared to the standard with IC50 values of 23.75 and 23.14 μg/ml, respectively, which was due to the presence of electron‐donating groups. The activity was found to decline when electron‐donating groups were replaced by electron‐withdrawing groups. Moderate scavenging activity was observed for the superoxide radical. Structure activity relationship and physiochemical properties were studied for all the derivatives.

Antioxidants exert their action chiefly in controlling and preventing the free-radicals and their reactions and thus it has a vital role as health protecting factor. There are many scientific data proposing that antioxidants lower the threats of some chronic diseases including cancer and heart disease. In the present work, the hybrid molecule i.e benzothiazole substituted 4-thiazolidinone, has been taken for the study and different novel benzothiazole substituted 4-thiazolidinone derivatives were synthesized by reacting 2-amino-6-methyl benzothiazole with aromatic aldehydes in alcohol media. The resulting Schiff bases were made to react with thioglycolic acid in dioxane. Characterization of synthesized compounds was done by IR, 1 H NMR and Mass spectroscopy. The same reaction was performed in the microwave assisted reaction condition and compared with conventional synthesis. In vitro antioxidant activities of compounds were performed by three different methods, out of which Compound TZ4 emerged as a promising molecule.