Exploiting the Indole Scaffold to Design Compounds Binding to Different Pharmacological Targets

Abstract

Several indole derivatives have been disclosed by our research groups that have been collaborating for nearly 25 years. The results of our investigations led to a variety of molecules binding selectively to different pharmacological targets, specifically the type A γ-aminobutyric acid (GABAA) chloride channel, the translocator protein (TSPO), the murine double minute 2 (MDM2) protein, the A2B adenosine receptor (A2B AR) and the Kelch-like ECH-associated protein 1 (Keap1). Herein, we describe how these works were conceived and carried out thanks to the versatility of indole nucleus to be exploited in the design and synthesis of drug-like molecules.

Keywords

• type A γ-aminobutyric acid (GABA_A) chloride channel
• translocator protein (TSPO)
• murine double Minute 2 (MDM2) protein
• A_2B adenosine receptor (A_2B AR)
• Kelch-like ECH-associated protein 1 (Keap1)