This is the first systematically research which investigates structure-activity relationsips(SAR) of antibiotics of polyyne. In this paper, it is reported that tetrayne compounds composed of hydrophilic unit and tetrayne unit has possibility of strong antimicrobial activity. Based on the above results, the possibility of development as an antibiotic medicine was examined to synthesise the more improved antibiotic compounds with synthesized polyhydroxy novel sugar analog possessing the part of tetrayneol moiety.