ChemInform Abstract: BROMO DERIVATIVES OF GRAMINES. PREPARATION AND PHARMACOLOGICAL PROPERTIES

Abstract

Bromieten von Gramin (I) ergibt ein nicht trennbares Gemisch des 5‐Bromderivates (II) mit demö‐Bromderivat (III), das durch Mannich‐Reaktion aus 6‐Bromindol (IV) rein . erhalten wird.

Gramine Derivatives Targeting Ca2+ Channels and Ser/Thr Phosphatases: A New Dual Strategy for the Treatment of Neurodegenerative Diseases

“…In this work, we describe the findings observed with a family of indole derivatives, analogues to the natural alkaloid gramine (1, Figure 1), which has shown promising pharmacological activities. 52 Indeed, some of its brominated derivatives have been described as Ca 2+ channels blockers. 53 In our laboratory, we observed that 1 protected SH-SY5Y neuroblastoma cells against the toxic stimulus generated by OA in a wide range of concentrations.…”

“…For all of these reasons, we considered worthwhile to keep deepening the study of PPP enzymes as a part of a multitarget strategy to find new drugs for AD, the control of cytosolic Ca 2+ as the other main therapeutic target remaining. In this work, we describe the findings observed with a family of indole derivatives, analogues to the natural alkaloid gramine ( 1 , Figure ), which has shown promising pharmacological activities …”

Novel, Highly Potent Aldose Reductase Inhibitors: Cyano(2-oxo-2,3-dihydroindol-3-yl)acetic Acid Derivatives

“…As part of an ongoing effort to identify potent and selective ARIs, in view of our long experience in indole chemistry, − we decided to support the acetic acid residue, essential for the inhibition of the enzyme, with the 2-oxoindole nucleus. It has been reported in the literature that potent in vitro inhibition of ALR2 has been observed with a number of acetic acid or spiro-hydantoin derivatives of oxoindole.…”

Regioselective dibromination of methyl indole-3-carboxylate and application in the synthesis of 5,6-dibromoindoles

“…gramine derivatives have previously been investigated for antiinflammatory and analgesic activity. 23 Vilsmeier-Haack formylation of 7 gave the C-3 aldehyde 17 in high yield. Condensation of 17 with creatinine (18) gave the non-natural 5,6-dibromo-4¢-demethylaplysinopsin 19, isolated as a single double bond isomer.…”