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An efficient method developed for the synthesis of asymmetric (S)-N-benzylidene-2-(benzyloxy)-1-(5-(pyridin-2-yl)-1,3,4-thiadiazol-2-yl)ethanamine derivatives with excellent yield in short reaction time. The antioxidant and antimitotic activities were estimated and strongly correlated with the potential of Ascorbic acid and Methotrexate respectively. All the synthesized molecules were characterized using various spectral techniques including FTIR, 1H NMR, 13C NMR, and Mass spectrometry. The drug-likeness properties were studied using in silico ADME parameters. All the compounds have an acceptable range of values which indicated good drug-like characteristics based on Lipinski's rule of five and to be orally active. The present method is quite easy along with simple operation and offers many benefits including short reaction time, easy work-up, excellent yield, reduced waste production as well as cost effective. In addition structure-activity relationships of AP-1 to AP-10 derivatives have been described. [ABSTRACT FROM AUTHOR]

A new series of 1-Thiazolyl-2-Pyrazolines 5a-g was accomplished by reacting pyrazolealdehyde with an appropriate aromatic ketone in the presence of PEG-300 as a solvent to yield chalcone. The chalcones reacted with thiosemicarbazide to yield asymmetric 1-thiocarbamoyl pyrazoles. The above formed 1-thiocarbamoyl pyrazoles reacted with appropriate α- haloketones to yield 1-Thiazolyl-2-Pyrazolines. The structural interpretations of newly formed compounds were done by 1H NMR, 13CNMR, IR and mass spectroscopic methods. The newly prepared asymmetric 1-Thiazolyl-2-pyrazoline derivatives were evaluated to their in vitro antioxidant (H2O2, DPPH, SOR and NO radical inhibiting activity) as well as anti-inflammatory activity. The 1-Thiazolyl-2-pyrazoline derivatives 5a-g exhibited moderate to good H2O2 scavenging activity as match up to ascorbic acid. All the 1-Thiazolyl-2-pyrazoline derivatives exhibited excellent SOR scavenging activity except 5 b. All the tested compounds have shown good to excellent, NO radical inhibiting activity. DPPH radical scavenging activity results have shown low antioxidant activity. Also, all the 1-Thiazolyl-2-pyrazoline derivatives were tested for their in vitro anti-inflammatory activity. The compounds 5a, 5 b, 5c, 5f and 5 g were exhibited good anti-inflammatory activity and 5d showed moderate activity while 5e less active as match up to diclofenac sodium as a standard reference. [ABSTRACT FROM AUTHOR]