Alprazolam, structure

The structures of the drugs used as a small test set for the model are listed in Table 17.1. Loperamide and asimadoline are P-gp substrates terfenadine and ebastine are compounds that are rapidly metabolized alprazolam, dobazam, di-and mono-hydroxy-L66858 [11] are benzodiazepines testosterone and corticosterone are hormones and cefadroxyl, cefaclor, cephalotin and cefmetazole are cephalosporins [12]. Finally, peptides 1 to 10 are peptidomimetic drugs [13]. 

Synthesis of the first two is described in Section 5.1 of Chapter 5. Benzodiazepines are described in the same place where the synthesis of structural analogs of midazolam (alprazolam, etc.) are described. 

Figure 1.4 The chemical structure of alprazolam (Xanax) categorizes the drug as a benzodiazepine. Treatment with benzodiazepine is recommended for patients with panic disorder. Xanax can be habit-forming and treatment should be closely monitored by a physician.

The benzodiazepines are widely used sedative-hypnotics. All of the structures shown in Figure 22-2 are 1,4-benzodiazepines, and most contain a carboxamide group in the 7-membered heterocyclic ring structure. A substituent in the 7 position, such as a halogen or a nitro group, is required for sedative-hypnotic activity. The structures of triazolam and alprazolam include the addition of a triazole ring at the 1,2-position. 

The discovery of the benzodiazepines (BZDs) at Hoffmann-La Roche in the late 1950s provided a more formidable arsenal for the treatment of anxiety [5]. Following the introduction of chlordiazepoxide (1, Librium ) in 1960, a large number of analogues were synthesized and developed, including diazepam (2, Valium ), lorazepam (3, Ativan ), prazepam (4, Cen-trax ), oxazepam (5, Serax ), chlorazepate (5a,Tranxene ), and alprazolam (6, Xanax ). Although other structural classes of compounds for treatment of anxiety have been discovered such as hydroxyzine (7, Atarax ), buspirone (8, Buspar ), and chlormezanone (9, Trancopal ), the prescriptions written for (l)-(7) over the years since their introduction equal or exceed that for any disorder [4, 6], presumably because of their effectiveness and rapid onset of action [7],... 

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