Tetrahydro-β-carboline, a derivative of β-carboline alkaloid, is found in a variety of plants, animals, insects, mammals, and human tissues and body fluids. It is found abundantly in nature and includes both natural and synthetic forms. Tetrahydro-β-carboline and their derivatives have been proven to exhibit important biological features, which makes it easier to build novel synthetic techniques for the alteration of Tetrahydro-β-carboline core to create high potential medications. Tetrahydro-β-carboline was proven to exhibit various pharmacological activities such as antiviral, antileishmanial, anticancer, antifungal, HDAC inhibitor, antithrombotic, antimalarial, analgesic, and anti-AD inhibitor action. The characterization, chemistry, structure activity relationship, and Antimicrobial activities of tetrahydro-β-carboline derivatives are highlighted in this review along with recent research and developments in these areas. Keywords: Tetrahydro-β-carboline, Tetrahydro-pyrido[3,4-b]-indole, Heterocycle, Alkaloid, Structure, Activity, Derivative, Antimicrobial activity, Occurrence.