Medicinal Chemistry of IBD Flashcards
What is Inflammatory Bowel Disease
Chronic inflammatory condition of the GI tract that results from recurring ummune response leading to inflammation and/or ulceration
What are symptoms of IBD
diarrhea, rectal blood loss, abdominal pain, and weight loss
What are the treatment goals of IBD
Induce remission, prevent flare ups
What are the treatment options for IBD
Aminosalicylates, glucocorticoids, immunomodulators
What is an aminosalicylate used in IBD, how does it work
Mesalamine, appears to work by blocking cyclooxygenase and inhibiting prostaglandin syntheses in the colon
Which aminosalicylate is linked together by an azo bond, what is the determing factor of how much is released
Olsalazine, bacteria present in the lower intestine
What is consequence of calcineurin inhibitors
Prevents translocation of NFAT to nucleaus, inhibts transcription of cytokines (IL-2)
What Jak/Stat inhibitor is used for the treatment of ulcerative colitis
Tofacitinib
What are the monoclonal antibodies that bind to TNF-alpha
Infliximab and Adalimumab
What investigation agent accelerates the degredation of TNF-alpha mRNA, what are some of the dangers
Thaliomide, teratogenic
What is the MOA of pentoxyfiline, what is the active metabolite
down regulates the TNF-alph production at both the protein and mRNA levels, lisohyline
Which histamine antagonists are used to treat allergies
H1
What is the general formula for a H1 receptor antagonist
Two aromatic rings, Tertiary amine
If H1 activity was to be decreased where would the substituents be place on aromatic ring 1, increased
ortho or meta, para
T/F: Para substituents on both aromatic rings will decrease H1 activity
True
