Medicinal Chemistry-I ; BP402T
Hello everyone today topic is nasa now nasa are a class of drug that will leave pain reduce inflammation and bring down a high temperature which means a fever nussaids work by blocking the production of prostaglandins chemical messengers that often are responsible for the pain and swelling of inflammatory conditions some of the primary indication for nasal therapy
Include rheumatoid arthritis osteoarthritis acute gouty arthritis ankylosing spandulitis dysmenorrhea and tissue damage resulting from inflammatory joint disease the prostaglandins are the mediators of inflammation inflammatory response is the body’s natural response that occurs immediately following tissue damage most of the nusset are irreversible inhibitors
Of cyclooxygenase activity thus they prevent the formation of prostaglandin and consequently reducing the sign and symptom of inflammation now how nasaid work then nasa were by inhibit the prostaglandin synthesis by inhibit cyclo oxygen one and two cyclooxazines are the enzymes which form prostaglandins from arachidonic acid now you look phospholipids is occur
In the membrane that release archetonic acid and with the help of cyclooxygenase 1 and 2 endo peroxide release and after the endoperoxide prostaglandins with the help of poster glandine isomerase and thromboxine release with the help of thromboxane synthase and prostacyclin is with the help of forestry cycling synthesis then the sad act on these cyclooxygenase
Enzyme and inhibit the synthesis of prostaglandins now classification prognosites non-selective cox inhibitors preferential cox-2 inhibitors selective cox-2 inhibitors an analgesic antibiotic but poor inflammatory action and there are the drugs under these categories like in non-selective cox inhibitors category salicylate example is aspirin acetic acid
Derivatives indomitability then parasolution derivative oxy fin butazone phenylbutazone and propionic acid derivative ketoprofen ibuprofen and naproxen and phenomate me mafinamic acid inolic acid derivative like peroxide in oxygen and in preferential cox2 inhibitors the example of the drug are pneumoslavid diclofenac acilophenac meloxicum and selective cox 2
Inhibitors are selective heterocoxy and anaerobic antibiotic with poor anti-inflammatory action like a paracetamol profineo zone and napofer after the classification we discussed the drugs under the nasty selective cox inhibitors first is an aryl antennalic acid derivative these are phenomic acid be carrying these are the general structures for nri anthemic
Acid derivative having enthalic acid ring and an aryl ring and the drug are these categories mafinamic acid mafnamic acid exerts analgesic action on both center and peripheral region however the analgesic effect is comparatively weaker than aspirin it also possess a fairly good antibiotic action but its anti-inflammatory activity is relatively weak there is a
Structure for graffinamic acid 2 2 3 ty methyl anilino benzoic acid and synthesis of magnamic acid started with orthochlorobenzoic acid react with 2 3 xylidine condensation reaction occur with the help of potassium chromate and potassium salt of methanolic acid produced after hydro hcl hydrolysis excel released and mafinamic acid produced the uses of methanamic
Acid is administered twice daily in doses of 250 mg to treat dysmenorrhea osteoarthritis rheumatoid arthritis soft tissue muscles and joint pain then parazolone and parasolid dome derivatives and the drug are in this category are anti-pyramid lycophenol zone and phenylbutazone the structure is phenyl butazone brand name is butazolidine it is also used to
Treat inflammation and pain that result from enclosing spondylitis rheumatide arthritis gout and osteoarthritis then after this salicylates salicylic acid derivative and the salicylic acid derivative was the first class of nasals to be used they possess analgesic antibiotic as well as anti-inflammatory properties they are also used as anti-gaud drug as they
Promote the excretion of uric acid these are mainly used in the treatment of arthritis the drugs are in this categories aspirin and sodium salicylate research structure was aspirin two acetoxy benzoic acid then sodium salicylate it is used in medicine as an energetic and antibiotic sodium salicylate also act as non-steroidal anti-inflammatory drug and induces
Apoptosis in cancer cells and also necrosis after the salicylic acid derivatives here is aryl and hydropropanoic acid derivatives the drug in this category is ibuprofen catapult phanoprofen and naproxen and here is the structure of naproxen naproxen is used to relieve pain from various conditions such as headache muscles aches dental pain and menstrual cramps
It also reduces pain swelling and joint stiffness this medication is also known as non-steroidal anti-inflammatory drug the next drug in this category is ibuprofen is most widely used reversible cox inhibitor it is administered only or applied topically in the form of cream and gel there is a structure 2 4 isobutyl phenyl propanoic acid and for the synthesis
We required isobutyl benzene and react it with acetate chloride in the presence of aluminium trichloride and then we get isobutyl acetophenone and after this hydrogen cyanide case our reactor k a cyanohydrin menthol then again react with hydrogen iodine and hydrolysis we get ibuprofen ibuprofen is used to treat mild to moderate painful conditions such as in
Fractures injuries of soft tissue etc it is used in the treatment of rheumatoid arthritis osteoarthritis and guide to goity arthritis the next drug is diclofenac diclofenac was introduced in u.s in the year 1989 it is the most widely used nasa today its structural features are related to both aryl alkenoic acid and n-aryl anthranilic acid structure is two two
Two six dichloro anilinophenyl acetic acid the next drug is indomethacin it is indole acidic acid either the heteroaryl group present in the structure is indole this is a structure for indomethacin 2 1 4 chloro benzoyl 5 methoxy 2-methyl indole 3-isle acetic acid then sulein deck it is an assad the structure of nasolin deck work by reducing hormone that cause
Inflammation and pain in the body and the syllan deck is used to treat pain or inflammation caused by arthritis spondylitis tenderitis or goat the next drug is keto lack used short term to treat moderate to swear pain help to decrease swelling pain or fever thank you
Transcribed from video
Unit-5 : NSAIDS: Non-steroidal anti-inflammatory Drugs By Sachdeva College of Pharmacy Gharuan