Class 74 Structure Activity relationship SAR of NSAIDs Medicinal Chemistry 01 BPharmacy

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Download the Solution Pharmacy Mobile App to Get All Uploaded Notes, Model Question Papers, Answer Papers, Online Tests and other GPAT Materials - https://play.google.com/store/apps/de... • Solution Pharmacy will cover this syllabus of medicinal chemistry 01 for B.Pharmacy 4th semester • Unit 05 - • (01) Drugs acting on the central nervous system – general anaesthetics • (02) Inhalational anaesthetics – Halothane, methoxyflurane, enflurane, sevoflurane, isoflurane, desflurane • (03) Ultra-short acting barbiturate – methohexital sodium, Thiopental sodium • (04) Dissociative anaesthetics – Ketamine hydrochloride • (05) Narcotic and non-narcotic analgesic • (06) Morphine and related drugs – SAR of morphine analogous, morphine sulphate, codeine, meperidine hydrochloride, loperamide hydrochloride, pentazocine, • (07) Narcotic analgesic- nalorphine, • (08) Anti-inflammatory agents – Sodium salicylate, aspirin, mefenamic acid, meclofenamate, indomethacin, tolmetin, diclofenac, ketorolac, ibuprofen, naproxen, piroxicam, phenacetin, acetaminophen, antipyrine, phenylbutazone • The non-steroidal antiinflammatory drugs (NSAIDs) are widely used for the treatment of minor • pain and for the management of edema and tissue damage resulting from inflammatory joint • disease (arthritis). A number of these drugs possess antipyretic activity in addition to having • analgesic and antiinflammatory actions, and thus have utility in the treatment of fever. Most of • these drugs express their therapeutic actions by inhibition of prostaglandin biosynthesis as • described in the sections that follow. Some of the primary indications for NSAID therapy • include • In general, NSAIDs structurally consist of an acidic moiety (carboxylic acid, enols) attached to a • planar, aromatic functionality. Some analgesics also contain a polar linking group, which • attaches the planar moiety to an additional lipophilic group. • SAR OF INDOLE ACETIC ACID DERIVATIVES • 1. MODIFICATION IN THE CARBOXYLIC ACID GROUP: • The presence of the -COOH group is very much essential for the activity of the compound. On the α position, if a methyl group is substituted, then it will retain the activity of the compound and give different conformations. • 2. MODIFICATION/SUBSTITUTION IN THE 2nd POSITION • Any substitution in the R2 group will increase the activity of the compound. Substitution of a methyl group will show better activity than an aryl group. Dextrorotatory isomer is more active. • 3. MODIFICATION/SUBSTITUTION IN THE 1-N POSITION: Substitution of the R1 group with Benzoyl (e.g., indomethacin) or an alkyl group or hydrogen will increase the activity of the compound. To the benzoyl group of indomethacin, if a para substitution is made with electron-withdrawing groups like -Cl/-CF3/-SCH3, then greater activity is shown. • 4. SUBSTITUTION IN THE 5TH POSITION. This substitution affects the potency of the compound in general. If a substitution is made with -OCH3/-N(CH3)2/Alkoxy group, then potency increases. • SAR OF PYRAZOLIDINEDIONE DERIVATIVES • 1. ACIDIC HYDROGEN AT POSITION 4: • In 3,5-thiazolidinedione derivatives, the pharmacological activities are closely related to their acidity, which is influenced by the acidity of the H-atom at position 4. The carbonyl groups at the 3rd and 5th positions enhance the acidity of the compound. • If the acidity is decreased by the removal of the H-atom, it leads to the abolition of the anti-inflammatory activity of the compound. Enhancement of acidity also increases the uricosuric effect and sodium retaining property. • ALKYL GROUP SUBSTITUTION (R2): • A single alkyl group at the 4th position enhances the anti-inflammatory activity. Substitutions can be made with propyl/butyl/n-butyl groups, of which the n-butyl group is shown to give the best anti-inflammatory activity. • The introduction of an -OH (hydroxyl) group in place of an alkyl group generally enhances the uricosuric effect but decreases the anti-inflammatory effect. Substitution with 2-phenylthioethyl group gives anti-gout properties (SULFIOYRAZONE) • PHENYL GROUPS: • The presence of both phenyl groups is a must for the compound to show anti-inflammatory and analgesic activity. • ARYL GROUP SUBSTITUTION: • Various substitutions in the para position of one or both the aromatic rings do not drastically affect the activity. The p-hydroxy group present in oxyphenbutazone, the major metabolite of phenylbutazone, contributes therapeutically useful anti-inflammatory activity. Other derivatives such as methyl, chloro, it, and nitro group also possess activity. • E-Mail for official and other work - [email protected] • #solutionpharmacy #Pharmacologyclass #Pharmacognosyvideos #GPAT

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