New dibenzothiadiazepine derivatives with antidepressant activities

Abstract

A new series of 11-[(aminoalkyl)carbonyl] derivatives of 6,11-dihydrodibenzo[c,f][1,2,5]thiadiazepine 5,5-dioxide (10-39) were synthesized and evaluated for potential antidepressant activity in the apomorphine-induced hypothermia (Apo 16) test. Effects on reserpine-induced hypothermia and toxicity for the most potent antagonists of Apo 16 hypothermia were also studied. Structure-activity relationships are reported. Anticholinergic effects were evaluated for compound 12, identified as the most potent and least toxic in this series, by assessing physostigmine lethality. Compound 12 was also subjected to X-ray analysis.

Reagent based DOS: A “Click, Click, Cyclize” strategy to probe chemical space

“…1), yet not “preordained bioactivity” as is the case with targeted, medicinally active natural products. In particular, reports include anti-HIV activity,9 antidepressant activity,10 inhibitors of RSV,11 selective tumour necrosis factor,12 and metalloproteinase 13. In addition to this potent biological profile, sultams and their sulfonamide precursors possess a number of advantageous chemical properties.…”

An efficient one‐pot synthesis of N‐(substituted phenyl)‐1,2,5‐thiadiazolidine‐2‐carboxamide 1,1‐dioxide derivatives

“…Among heterocyclic compounds, the 1,2,5‐thiadiazolidine 1,1‐dioxides derivatives of cyclosulfamides containing nitrogen, oxygen and sulfur exhibit multiple biological and pharmacological activities, because of their analogues of cyclosulfamoyl ureas. They are used as diuretic agents, potential inhibitors of HIV‐1 viral protease, antidepressants, and reverse transcriptase inhibitors . For example, sulfonylureas derivative compound 1 shows antituberculous, the sufamoyl ureas 2 influences the cancerous activity, and the cyclosulfamides 3 shows serine protease inhibitors (Figure ).…”

Synthesis of benzannelated sultams by intramolecular Pd-catalyzed arylation of tertiary sulfonamides

“…At the same time, cyclic sulfonamides (sultams) have also received significant attention due to their biological activities and medicinal uses [ 1 – 7 ]. On the other hand, especially fused sultams are among the most commonly used therapeutic agents owing to the broad spectrum of their activities [ 8 – 13 ]. Up to now, sultams have been prepared employing Diels–Alder reactions, radical cyclizations, reductions of sulfonylimines, ring-closing metatheses, nucleophilic aromatic substitutions and Heck cyclizations [ 14 – 16 ].…”