With the goal of developing a modular approach leading to different indoline alkaloid natural-product-like tricyclic derivatives having an unsaturated lactam (see compounds 13, 14, and 16), an aminoindoline-based bicyclic scaffold 10 was obtained from 9. The selective deprotection of the indoline NTeoc or benzylic NHAlloc in compound 10, followed by N-acryloylation and then subjection to a ring...

Reprint requests to Dr. L.M. Sabet, Health Sciences Centre, Department of Pathology, London, Canada N6A 5CI. The pathophysiological effects and clinical features of overdosage with tricyclic antidepressants have been described in detail (Moraguerra, 1977; Petit, 1977; Bilgi, 1979). However, published accounts of morphological changes in the brain are scarce and lacking in detail. We are not awa...

Acrocyanosis is probably the most unusual side effect of tricyclic antidepressant drugs. In this paper, we report a 10-year-old boy with primary enuresis nocturna and attention deficit hyperactivity disorder who developed two episodes of acrocyanosis, the first of which was after imipramine treatment and the second after desipramine usage. We also review the possible pathogenesis of acrocyanosi...

The development of a ring-opening metathesis/ring-closing metathesis/cross metathesis (ROM-RCM-CM) cascade strategy to the synthesis of a diverse collection of bi- and tricyclic sultams is reported. In this study, functionalized sultam scaffolds derived from intramolecular Diels-Alder (IMDA) reactions undergo metathesis cascades to yield a collection tricyclic sultams. Additional appendage base...

In the present paper, we report an expedient total synthesis of triciribine, a tricyclic 7-deazapurine nucleoside and protein kinase B (AKT ) inhibitor, in 35% overall yield. Our synthesis route features a highly regioselective substitution of 1-N-Boc-2-methylhydrazine and a trifluoroacetic acid catalyzed one-pot transformation which combined the deprotection of the tert-butylcarbonyl (Boc) gro...

Of 80 consecutive admissions to a general hospital for drug overdose, 10 had taken one or other of the tricyclic antidepressants. All 10 had abnormalities of cardiac conduction as shown by prolonged Q-T(e) intervals, and eight had S-T segment and T-wave changes. Five of the 10 patients had arrhythmias and two of these died. Continuous electrocardiographic monitoring is recommended in patients w...

Tricyclic Steiner Triple Systems with 1-Rotational Subsystems by

Morphine is an effective analgesic in clinical practice; however, its long-term administration causes tolerance, thereby limiting its use. The development of opioid tolerance and its associated hyperalgesia has been associated with interactions between opioid receptors and excitatory amino acids or cytokines. Targeted inhibition of excitatory amino acidand cytokine-mediated signaling pathways m...

Hydroxyindoline-derived scaffold, 9, was synthesized with the goal of generating a library of indoline-based natural product-like tricyclic derivatives to be utilized as small-molecule chemical probes. The tricyclic ring was obtained by a Mitsunobu reaction of the N-nosyl amino acid conjugate with the primary hydroxyl group. The solid-phase synthesis was achieved by immobilizing scaffold 9 onto...

ROTH, K. A. AND R. J. KATZ. Further studies on a novel animal model of depression: Therapeutic effects of a tricyclic antidepressant. NEUROSCI. BIOBEHAV. REV. 5(2) 253-258, 1981.--We have previously shown that rats given stress before open field testing have elevated activity in comparison with unstressed rats. This acute behavioral response may be eliminated by chronic stress and restored by p...