WS Historically, we have treated inflammatory bowel disease (IBD) using small molecules such as prednisone, budesonide, and mesalamine, along with immunosuppressive drugs such as azathioprine, 6-mercaptopurine, and methotrexate. Until infliximab (Remicade, Janssen) was approved in 1998, the treatment of IBD was entirely based on small molecules. Since that time, virtually all new medications ap...

Experimental uveitis in rabbits was induced by single intraocular antigen injection. Treatment with 6-MP for 14 days suppressed the allergic inflammation and antibody response. A good correlation was demonstrated between the degree of uveitis and the antibody titer.

The administration of 6-MP to rabbits led to either suppression or enhancement of antibody production, depending on when the drug was given in relation to the antigenic challenge. Maximum enhancement of antibody synthesis was found when a small dose of BGG was administered 5 days after the last dose of a 1 wk course of 6-MP. There were no indications that the macrophage system or immunological ...

The crystal structures of five 6-mercaptopurine derivatives, viz. 2-[(9-acetyl-9H-purin-6-yl)sulfan-yl]-1-(3-meth-oxy-phen-yl)ethan-1-one (1), C16H14N4O3S, 2-[(9-acetyl-9H-purin-6-yl)sulfan-yl]-1-(4-meth-oxy-phen-yl)ethan-1-one (2), C16H14N4O3S, 2-[(9-acetyl-9H-purin-6-yl)sulfan-yl]-1-(4-chloro-phen-yl)ethan-1-one (3), C15H11ClN4O2S, 2-[(9-acetyl-9H-purin-6-yl)sulfan-yl]-1-(4-bromo-phen-yl)etha...

Azathioprine (AZA) and its active metabolite, 6-mercaptopurine (6-MP), are purine analogues that interfere with the synthesis of adenine and guanine ribonucleosides. These ribonucleosides are important precursors of DNA and RNA. Because AZA and 6-MP act predominantly on rapidly dividing cells such as the T lymphocytes, these drugs are not only cytotoxic but also immunosuppressive and anti-infla...