Black pepper (Piper nigrum L.) has gained a global consideration because of its volume in the spice industry. This plant has shown great potential for having medical applications and novel biologically active compounds. In black pepper, natural lipophilic amide piperine was isolated. Piperine was isolated from the fruit using glacial acetic acid as solvent. After isolation and characterization of piperine were done, then it is used to prepare new and novel derivatives of piperine through the experimental procedure. The derivatives of piperine were synthesized by condensation of piperic acid with different substituted aromatic amines, to make a new derivative of piperine, such as ((2E, 4E)-5-(1,3-benzodioxol-5-yl)-N-(1,3-benzothiazol-2-yl)penta-2,4-dienamide) and a novel derivative ((2E, 4E)-5-(1,3-benzodioxol-5-yl)-N-(1,3-benzothiazol-2-yl)penta-2,4-dienehydrazide). The structure of piperine and the derivatives were elucidated through a combination of spectrometric techniques, including ultraviolet spectrophotometer, Mass spectrometry Fourier transform infrared spectroscopy, proton nuclear magnetic resonance.