VEDA-1209 / Cureveda - LARVOL DELTA

OPTIMIZATION AND EVALUATION OF PYRIDINYL VINYL SULFONES AS NRF2 ACTIVATOR FOR THE ANTIOXIDANT AND ANTI-INFLAMMATORY EFFECTS (ADPD 2024) - "Most of the synthesized compounds showed excellent Nrf2 activation and improved drug-like properties by introducing sulfone core, pyridine rings, and functional groups of VEDA-1209. The compound 10e was selected for further evaluation as it exhibited potent Nrf2 activation and favorable drug-like properties. Furthermore, the 10e remarkably upregulated Nrf2-dependent antioxidant response genes, and suppressed NO production and proinflammatory cytokines in the BV-2 microglial cells."

Oncology

Promising vinyl sulfone Nrf2 activator discovery based on the chalcone derivative using LPS-induced Alzheimer's disease mouse model (ACS-Fall 2023) - "Among disclosed chalcones, Veda-1209, a synthetic chalcone derivative, is Nrf2 activator currently undergoing preclinical testing for the treatment of ulcerative colitis...Compound 10e induced the expression of the Nrf2-dependent enzymes at protein levels and suppressed the induction of pro-inflammatory effects. For further validation, we analyzed antioxidant and anti-inflammatory effects in microglial cells of 10e, and it also significantly restored spatial memory and cognition in LPS-induced mouse model."

Preclinical • Alzheimer's Disease • CNS Disorders • Gastroenterology • Gastrointestinal Disorder • Immunology • Movement Disorders • Multiple Sclerosis • Oncology • Parkinson's Disease • Ulcerative Colitis

Optimization and evaluation of pyridinyl vinyl sulfones as Nrf2 activator for the antioxidant and anti-inflammatory effects. (PubMed, Eur J Med Chem) - "Among the published chalcone derivatives, (E)-1-(3-methoxypyridin-2-yl)-3-(2-(trifluoromethyl)phenyl)prop-2-en-1-one (VEDA-1209), which is currently undergoing preclinical study, was selected as a starting compound for the development of new nuclear factor erythroid 2-related factor 2 (Nrf2) activators...In addition, 10e effectively improved drug-like properties such as CYP inhibition probability and metabolic stability. Finally, 10e demonstrated excellent antioxidant and anti-inflammatory effects in BV-2 microglial cells and significantly restored spatial memory deficits in lipopolysaccharide (LPS)-induced neuroinflammatory mouse models."

Journal • Inflammation • Oncology

SYNTHESIS AND EVALUATION OF NOVEL SERIES OF VINYL SULFONE DERIVATIVES FROM VEDA-1209 AS PROMISING NRF2 ACTIVATORS FOR ALLEVIATING NEUROINFLAMMATION (ADPD 2022) - "6e, a new vinyl sulfone compound synthesized based on the structure of Veda-1209, was confirmed to have proper drug-like properties, including an potent Nrf2 activation effect."

Alzheimer's Disease • CNS Disorders • Immunology • Inflammation • Movement Disorders • Parkinson's Disease