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Based on the recorded pharmacological potencies of numerous substituted pyrimidines as antihyperlipemic and antihypertensive agents, synthesis of condensed and spiro bis-heterocyclic systems; oxazole-pyrimidines as well as pyrimido-oxazines; bearing a phosphonate substituent was undertaken. The bioassay indicated that some of the products have effect on the central nervous system (CNS), and other products have good selective anti-tumor activity and the structure-activity relationship (SAR) of new phosphonates has also been indicated. In addition, a new class of C-glycosyl amino acids bearing a thiourea segment as a linker has been designed and synthesized by addition of glycosylmethyl isothiocyanates to an amine-functionalized amino acid. The orthogonal set of protective groups makes these compounds suitable substrates for the co-translational modification of natural peptides. The study included the synthesis of a set of new sugar isothiocyanates and their coupling with the alanine derivative.