Eisa H M, Tantawy A S, el-Kerdawy M M
Department of Medicinal Chemistry, Faculty of Pharmacy, University of Mansoura, Egypt.
Pharmazie. 1991 Mar;46(3):182-4.
1-(2-Adamantyl-3-(5-arylhydrazono-6-methyl-4-oxopyrimidin -2-yl)guanidines, 2-(2-adamantylamino)-4-amino-s-triazine and its 6-chloromethyl derivative were prepared by cyclization of 1-(2-adamantyl)biguanide.HCl with ethyl 2-arylhydrazono-3-oxobutyrates, ethyl formate and ethyl chloroacetate, respectively. 1-(2-damantyl)-3-(4,5-dioxo-2-imidazolidinylidene)guanidine was used as intermediate for the synthesis of amides, hydrazide and azomethine derivatives of alkyl 2-(2-adamantylamino)-4-amino-s-triazine-6-carboxylates. The antimicrobial testing of the prepared compounds proved that an azomethine derivative was the most active. It showed a marked bacteriostatic effect against Staphylococcus aureus and Bacillus subtilis.
1-（2-金刚烷基-3-（5-芳基腙基-6-甲基-4-氧代嘧啶-2-基）胍、2-（2-金刚烷基氨基）-4-氨基-s-三嗪及其6-氯甲基衍生物分别通过1-（2-金刚烷基）双胍盐酸盐与2-芳基腙基-3-氧代丁酸乙酯、甲酸乙酯和氯乙酸乙酯环化制备。1-（2-金刚烷基）-3-（4,5-二氧代-2-咪唑烷叉基）胍用作合成2-（2-金刚烷基氨基）-4-氨基-s-三嗪-6-羧酸烷基酯的酰胺、酰肼和甲亚胺衍生物的中间体。对所制备化合物的抗菌测试证明，一种甲亚胺衍生物活性最高。它对金黄色葡萄球菌和枯草芽孢杆菌显示出明显的抑菌作用。
