Synthesis of low molecular weight compounds with complement inhibition activity.
An attempt was made to synthesize a series of non-cytotoxic low molecular weight meta-substituted aromatic ethers (2-4, 5-7) and some of their bioisosteres (14-16) and to evaluate their activity on the activation of human complement (classical pathway) and their intrinsic hemolytic activity. The in vitro assay results of the inhibition of complement-mediated hemolysis by these analogues indicate that the aldehydic meta substituted aromatic ethers show inhibitory potency, while carboxylic acid meta substituted aromatic ethers show hemolytic activity. Some of the bioisosteres exhibit both inhibitory as well as hemolytic property.
Master
Hoshang E
HE
Department of Chemistry, St. Xavier's College, 5, Mumbai, India. hosangm@rediffmail.com
Khan
Shabana I
SI
Poojari
Krishna A
KA
D003169:Complement Inactivator Proteins / Q000138:chemical synthesis* / Q000494:pharmacology*; D003171:Complement Pathway, Classical / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004952:Esters / Q000138:chemical synthesis / Q000494:pharmacology; D004987:Ethers / Q000138:chemical synthesis / Q000494:pharmacology; D006461:Hemolysis / Q000187:drug effects; D006801:Humans; D066298:In Vitro Techniques; D007202:Indicators and Reagents; D008970:Molecular Weight
D003169:Complement Inactivator Proteins; D004952:Esters; D004987:Ethers; D007202:Indicators and Reagents