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A Synopsis of the Properties and Applications of Heteroaromatic Rings in Medicinal Chemistry
Five- and six-membered heteroaromatic rings and their benzo-fused homologues are well established as important structural elements in drug design and are well represented in approved drugs. The key properties of these heterocycles that are of?interest to medicinal chemists include lipophilicity, pKa, aromaticity, ionization potential, H-bond acceptor, and H-bond donor (N?H, O?H, C?H) capability, electron withdrawing effects, dipole values, and bond angles. The judicious and productive application of azoles and azines in drug design requires an understanding of the intrinsic physical chemical properties of the individual heterocycles and how these interact with substituents. In this article, the key properties of azole and azine heterocycles are summarized followed by a synopsis of applications where some of these factors play a role in drug?target interactions and/or potency.
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Reference£º
Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com