Novel conjugates of 2‐aminopurine and purine containing fragments of chiral heterocyclic amines attached at position 6 of purine core via a linker, fragment of omega‐amino acid, have been synthesized and evaluated in vitro for their anti‐herpetic activity in the Vero E6 cells; as a result, a new group of compounds possessing high inhibitory activity against herpes simplex virus type 1, including acyclovir‐resistant (TK–) strain has been revealed. The anti‐herpetic activity of the synthesized compounds is substantially dependent on the stereo configuration of the fragment of heterocyclic amine.

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