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Atypical Elements in Drug Design by Jacob Schwarz PDF

By Jacob Schwarz

ISBN-10: 3319277405

ISBN-13: 9783319277400

ISBN-10: 3319277421

ISBN-13: 9783319277424

Medicinal chemistry is either technology and paintings. The technology of medicinal chemistry bargains mankind one in every of its top hopes for bettering the standard of existence. The artwork of medicinal chemistry keeps to problem its practitioners with the necessity for either instinct and adventure to find new medications. accordingly sharing the event of drug examine is uniquely valuable to the sphere of medicinal chemistry. Drug examine calls for interdisciplinary team-work on the interface among chemistry, biology and drugs. for this reason, the topic-related sequence subject matters in Medicinal Chemistry covers all correct elements of drug study, e.g. pathobiochemistry of ailments, identity and validation of (emerging) drug objectives, structural biology, drugability of goals, drug layout ways, chemogenomics, artificial chemistry together with combinatorial equipment, bioorganic chemistry, normal 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, removal, toxicology and pharmacogenomics. as a rule, designated volumes are edited by way of popular visitor editors.

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In these studies, the natural ligand 9-cis-retinoic acid (9-cisRA) served as the positive control. As can be seen from Fig. 18, bexarotene (3a) is more potent than 9-cis-retinoic acid, and disila-bexarotene (3b) has a profile comparable to that of its carbon analogue 3a. Thus, despite of the structural and electronic changes upon C/Si exchange, very similar RXRβ agonistic potencies of the C/Si analogues 3a and 3b were observed. Drug Design Based on the Carbon/Silicon Switch Strategy Scheme 6 Synthesis of 3b Fig.

30 31 32 32 37 45 53 55 56 57 1 Introduction Over the past five decades, many biologically active organosilicon compounds have been synthesized, and silicon chemistry has been demonstrated to be a novel source of chemical diversity in drug design (for reviews, see [1–17]). There are two different approaches that can be used for the design of silicon-based drugs: (1) synthesizing a silicon analogue of a known drug in which at least one carbon atom has been replaced by a silicon atom, with the rest of the molecule being identical (carbon/silicon exchange, carbon/silicon switch, sila-substitution) and (2) synthesizing completely new silicon-based classes of compounds (the carbon analogues of which are unknown or do not exist for principal reasons) that exploit specific features of silicon chemistry to address a well-validated target.

19 Chemical structures of the C/Si pairs 12a/12b–18a/18b [45] – the silicon analogues of the retinoid agonists TTNPB (12a), 3-methyl-TTNPB (13a), SR11237 (14a), tamibarotene (AM80, 15a), AM580 (16a), EC23 (17a), and TTNN (18a), respectively (Fig. 19). In these studies, some of the tested silicon compounds showed an enhanced agonistic potency compared to the parent carbon compounds. For example, as can be seen from Fig. 20, 2-fold sila-substitution of the pan-RXR-selective retinoid agonist SR11237 (14a !

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