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We report the preparation of new oxygen analogues 2 of twin-drug type bivalent mid-size lead molecule 1 and related single-drug type hydantoin derivatives 3. The new twin-drug type oxygen analogues (2a and 2b) also showed significant antibacterial activity against a Gram-positive strain (S. aureus). A comparison of the two types of twin-drug type mid-size compounds 1 and 2 showed that the original lead 1 had a higher level of antibacterial activity against a Gram-positive strain (S. aureus) than those of the compounds (2a and 2b). We also report the results of antibacterial evaluation of prepared compounds and the investigated structure-activity relationships of these molecules.C 2 -or C 3 -Symmetrical geometric molecules in the search for bioactive compounds have attracted much attention because of their promising pharmacological value for bioactive ligands for many types of receptors. 1-4 A large variety of synthetic bioactive C 2 -symmetrical bivalent molecules have been studied for many types of receptor ligands. It is generally accepted that a bivalent molecule would show enhanced affinity (activity) compared to that of the corresponding univalent molecule. Therefore, a number of studies have been carried out for the development of such symmetrical bivalent molecules. 1,2,4 We have been interested in molecules that interfere with carbohydrate recognition stages in order to find new bioactive candidates. From the viewpoint of molecular geometry, we have already investigated a few symmetrical molecules for the purpose of finding new bioactive leads. 5-10

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