Triazine is a heterocyclic aromatic ring structure, with three isomers distinguished by positions of their nitrogen atoms. 1,2,3-triazine derivatives like tubercidin, toyocamycin, sangivamycin, 2-azaadenosine and 2-aza-2-desamino-5,8-dideazafolic acid are the important active moieties in pharmaceutical field while 6-azacytosine, 6-azauracil, azaribine, tirapazamine, dihydromethyl furalazine, vardenafil, apazone, lamotrigine, ceftriaxone, pymetrozine, fervenulin (planomycin), reumycin and toxoflavin (panthothricin) are 1,2,4-triazine moieties used in clinical practices. The triazine ring structure is also found in naturally occurring antibiotics like fervenulin, reumycin and toxoflavin. 1,3,5-Triazine isomer or s-triazine is an oldest known organic compound, broadly used as a lead structure in ammeline, aceto-guanide, acetoguanamine, cyanuric acid and melamine. Some s-triazine containing drugs are hexamethylmelamine (altretamine), 2-amino-4-morpholino-s-triazine, hydroxymethyl-pentamethyl melamine, triethylenemelamine (tretamine), dioxadet, irsogladine, cycloguanil, almitrine, S9788 and DW1865. Triazines have a high significance in the field of pharmaceutical chemistry with wide-spectrum of pharmacological activities so useful for design and formation of novel drugs. Some triazine analogues are recently screened in clinical trials which may lead to potent type drugs with no side effects as presently available pharmacological agents. This review outlines the biological importance and synthesis of various types of triazine derivatives from various heterocyclic and drugs containing triazine moiety.