3-Tetrazolyl-ß-carboline derivatives as potential neuroprotective agents

• Type: Article in International Scientific Journal
• Date: 2024-01-01

Authors

Lucilia Saraiva (Author) FFUP

Journal

Title: Bioorganic and Medicinal Chemistry

Vol. 111

ISSN: 0968-0896

Publisher: Elsevier

Indexing

ISI Web of Knowledge - 0 Citations

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Other information

Authenticus ID: P-014-8S9

DOI: 10.1016/j.bmc.2024.117841

Abstract (EN): 3-Tetrazolyl-(3-carbolines were prepared by the Pictet-Spengler approach using a tryptophan analogue as building block, in which the carboxylic acid was replaced by the bioisosteric tetrazole group. Knowing that (3-carbolines are often associated with psychopharmacological effects, the study of the 3-tetrazolyl-(3-carbolines as potential neuroprotective agents against Parkinson's disease was investigated. The evaluation of neuroprotective effects against 1-methyl-4-phenylpyridin-1-ium (MPP+)-induced + )-induced cytotoxicity allowed to identify compounds with relevant neuroprotective activity. One derivative, 3-(1-benzyl-1H-tetrazol-5-yl)-1-(p-dimethylaminophenyl)- H-tetrazol-5-yl)-1-( p-dimethylaminophenyl)- (3-carboline, stood out for its low cytotoxicity and excellent performance, preventing cell death induced by this neurotoxin. The most promising compounds were also evaluated for their neuroprotective properties against iron (III)-induced cytotoxicity. However, only one 3-tetrazolyl-(3-carboline derivative slightly reduced iron-induced cytotoxicity. Overall, the neuroprotective properties of 3-tetrazolyl-(3-carbolines have been demonstrated and this finding may contribute to the development of new therapies for Parkinson's disease.

Language: English

Type (Professor's evaluation): Scientific

No. of pages: 11