For the last few decades, the chemistry of 1, 2, 4-Triazole derivatives has received significant popularity due their substantial synthetic and diverse therapeutic activities viz Anti-inflammatory, antimicrobial agents, anti-anxiety, C.N.S stimulants and sedatives, anti-mycotic activity. Therefore, 1, 2, 4-Triazole has made essential beacon for design and development of new pharmacological agents. The review herein enlightens the biologically worthwhile 1, 2, 4- Triazole derivatives. Numerous therapeutically active 1, 2, 4-Triazole derivatives have been developed by scientists across the globe are documented herein this review.