Synthesis and immunotropic properties of 5-substituted 1,5-benzodiazepin-2-ones derivatives in cultures of human peripheral blood cells, part III

The reaction of 4-methyl-(A) and 3-methyl-1H-2,3,4,5-tetrahydro-1,5-benzodi azepin-2-one (B) with selected alpha,beta -unsaturated acid chlorides: crot onoyl, cinnamoyl, and 4-nitrocinnamoyl is described. We have also character ized immunotropic activities of these compounds in the proliferative respon se of human lymphocytes to phytohemagglutinin A (PHA) or to allogeneic cell s in one-way mixed lymphocyte reaction (MLR), as well as their action on tu mor necrosis factor alpha (TNF-alpha) and interleukin 6 (IL-6) production i n peripheral blood mononuclear cells (PBMC) and mixed lymphocyte cultures ( MLC). Some of the compounds exhibited regulatoly activities in the prolifer ative response of cells to PHA depending on the reactivity of cells to PHA. The MLR induced proliferation of lymphocytes was moderately inhibited by t wo selected compounds. The compounds showed also inhibitory properties with regard to lipopolysaccharide (LPS)- and MLR-induced TNF-alpha production. Structure-activity relationship was discussed.