Transcription of Drug Design: Functional groups / Pharmacological Activity
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Drug Design: Functional groups / Pharmacological Activity
Drug Design: Functional groups / Pharmacological ActivityStructure - Mechanism of action (Interaction with target)Structure - Physiochemical properties (Bioavailability etc) Acid / base properties Water solubility Partition coefficient (Crystal structure) StereochemistryADMEA bsorbtion. Distribution, Metabolism, Excretion(ADMET, ADMEtox)Structure - Mechanism of actionNOOOHca. 5 Acetylcholin (Neurotransmittor)NOOH2 NCarbacholinNNHNNMeHOOA cetylcholin AgonistsNicotinePilocarpineProtonated av phys. pH (pH )Acetylcholin AntagonistsNOOOHA tropinOONOHC yclopentolatMeOOHOOOHOMeNHMeNMeMeTubocur arinCNSE ffektor celleReseptorSynapseAcetylkolinNoradrena linDet somatiske nervesystemDet autonome nervesystemCNSCNSDet sympatiskenervesystemDet parasympatiskenervesystemganglionStructu re - Mechanism of actionSAR: Structure Activity RelationshipsAcetylcholine agonists: Small N-quartenary antagonists: Larger N-quartenary (1905)NHNL idocaine/Xylocaine(1946)OAcid labile esterHydrophilicAminogroup(can be protonated)Spacer-Cn-X-X: -CO2- -CONH- -NHCO-Lipophilic(Aryl)Active compound identifiedTarget?
Antibacterial sulfonamides Old compound S NH2 O O H2N Acid form - neutral Low watersol. - crystals - Kidney damage [acid form] [base form] At pH 6 (urine) 10.4 = 6 + log [acid form] [base form] ≈ 25000 Modern compound S Ar O O HN Sulfametoksasol pKa 6.1 S Ar O O N - H+ S Ar O O N S Ar O O N N O N O N O N O S Ar O O N N O At pH 6 (urine) [acid ...
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