Solid-Phase Syntheses of Two Deacetyl-Thymosin β4 Analogues with Substitution at Position 12 and Their Effects on Impaired Blastogenic Response of T Lymphocytes of Uremic Patients

Two deacetyl-thymosin β₄ analogues containing Phe(4Br) or D-Phe(4Br) as position 12 were synthesized by the manual solid-phase method, and their immunological effects on the impaired blastogenic response of phytohemagglutinin-stimulated T lymphocytes of uremic patients with infectious diseases were studied. Bromination of the p-position of Phe¹² resulted in a marked restorative effect on the impaired blastogenic response of T lympocytes compared with that of our synthetic deacetyl-thymosin β₄ The synthetic [Phe(4Br)¹²]deacetyl-thymsin β₄ was approximately equal in potency to our synthetic [Phe(4F)¹²]deacetyl-thymosin β₄ in uremic patients, but the other analogue, [D-Phe(4Br)¹²]deacetyl-thymosin β₄, had no effect.