Inhibition of C1r̄, C1s̄ and generation of C1s̄ by amidino compounds

摘要: Abstract A series of amidino compounds has been investigated for their inhibitory effects on C1s, C1r, and generation C1s. Diamidines consisting two amidinophenyl residues linked in para position by a molecular bridge proved to be the strongest competitive inhibitors whereas those meta were C1r. They inhibited overall C1s when added system containing three subunits C1 Ca 2+ . Diphenylamidines more active than single ring amidines. Of all tested, dibromopropamidine was most effective inhibitor with K i value 3 · 10 −5 M ΔF ′ values 6.4 kcal mole −1 , amicarbalide B 4596 C1r 3.5 3.25 6.3 6.34 respectively. e-Aminocaproic acid also included this study comparison purposes found inert as its these reactions. The possibility that some might prove useful treatment hereditary angioneurotic edema is discussed.