Design and synthesis of low molecular weight compounds with complement inhibition activity.
An attempt was made to synthesize a series of non-cytotoxic low molecular weight compounds of varying substitutions and functionalities having pharmacophore activity like carbonyl compounds, carboxylic acid and bioisosteres like tetrazole and phenyl acrylic acid. The in vitro assay of these analogues for the inhibition of complement activity revealed significant inhibitory activity for varying substituents and, particularly, for bioisosteres, that is, tetrazole and phenyl acrylic acid derivatives.
Nadkarni Sakasa Research Laboratory, Department of Chemistry, St. Xavier's College, Mumbai 400 001, India. kpoojari@rediffmail.com
Hoshang E
HE
Master
Shabana I
SI
Khan
Krishna A
KA
Poojari
D000179:Acrylates / Q000138:chemical synthesis / Q000494:pharmacology; D000818:Animals; D002264:Carboxylic Acids / Q000138:chemical synthesis* / Q000494:pharmacology*; D002460:Cell Line; D003169:Complement Inactivator Proteins / Q000138:chemical synthesis* / Q000494:pharmacology*; D003171:Complement Pathway, Classical / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D004952:Esters / Q000138:chemical synthesis / Q000494:pharmacology; D004987:Ethers / Q000138:chemical synthesis / Q000494:pharmacology; D007668:Kidney / Q000166:cytology / Q000187:drug effects; D009682:Magnetic Resonance Spectroscopy; D008970:Molecular Weight; D013777:Tetrazoles / Q000138:chemical synthesis* / Q000494:pharmacology*
D000179:Acrylates; D002264:Carboxylic Acids; D003169:Complement Inactivator Proteins; D004952:Esters; D004987:Ethers; D013777:Tetrazoles