Atypical Elements in Drug Design (Topics in Medicinal by Jacob Schwarz

By Jacob Schwarz

Medicinal chemistry is either technology and artwork. The technological know-how of medicinal chemistry bargains mankind one in all its top hopes for making improvements to the standard of existence. The artwork of medicinal chemistry keeps to problem its practitioners with the necessity for either instinct and event to find new medications. for that reason sharing the adventure of drug examine is uniquely important to the sphere of medicinal chemistry. Drug study calls for interdisciplinary team-work on the interface among chemistry, biology and drugs. as a result, the topic-related sequence subject matters in Medicinal Chemistry covers all correct features of drug learn, e.g. pathobiochemistry of ailments, id and validation of (emerging) drug objectives, structural biology, drugability of ambitions, drug layout methods, chemogenomics, artificial chemistry together with combinatorial equipment, bioorganic chemistry, traditional compounds, high-throughput screening, pharmacological in vitro and in vivo investigations, drug-receptor interactions at the molecular point, structure-activity relationships, drug absorption, distribution, metabolism, removing, toxicology and pharmacogenomics. usually, detailed volumes are edited via popular visitor editors.

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24: the muscarinic antagonists 20a/20b [46], 21a/21b [46], and 22a/22b [47]; the σ receptor ligands 23a/23b–26a/26b [48]; the calcium channel antagonists niguldipine (27a) and sila-niguldipine (27b) [49]; the histaminic H1 antagonists terfenadine (28a), sila-terfenadine-A (28b), sila-terfenadine-B (28c), disila-terfenadine (28d), fexofenadine (29a), and sila-fexofenadine (29b) [50]; the σ receptor ligands panamesine (30a) and sila-panamesine (30b) [51]; the GnRH antagonists AG-045572 (31a) and disila-AG-045572 (31b) [52]; the antiviral agents 32a/32b–35a/35b [53]; the antiallergic agents 36a/36b [54]; the σ receptor ligands 37a/37b–40a/40b [55]; the estrogenic agents 41a/41b [56]; and the androgen receptor antagonists LG190178 (42a), sila-LG190178 (42b), LG190176 (43a), and sila-LG190176 (43b) [57].

2 Sila-Haloperidol: A Silicon Analogue of the Dopamine Antagonist Haloperidol Haloperidol (2a) is a dopamine (D2) antagonist that is in clinical use as an antipsychotic agent for the treatment of schizophrenia. Sila-haloperidol (2b), a silicon analogue of 2a, was synthesized in a multistep synthesis, starting from Si(OMe)4 (Scheme 3) [32, 33]. An alternative synthesis, also starting from Si(OMe)4, is shown in Scheme 4 [34]. In both cases, sila-haloperidol (2b) was isolated as the hydrochloride 2b·HCl.

3 Sila-Substitution of Drugs: Selected Examples . . . . . . . . . . . . . . . . . . . . . . . 1 Sila-Venlafaxine: A Silicon Analogue of the Serotonin/Noradrenaline Reuptake Inhibitor Venlafaxine . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . 2 Sila-Haloperidol: A Silicon Analogue of the Dopamine Antagonist Haloperidol . . 3 Disila-Bexarotene: A Silicon Analogue of the Retinoid Agonist Bexarotene .

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