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Updated: Aug 21, 2026

Synthesis and Bioconjugation of Thiol-Reactive Reagents for the Creation of Site-Selectively Modified Immunoconjugates
Published on: March 6, 2019
[Synthesis of hydrazino alcohols with anti-inflammatory activity]
Laszló Lázár1, Zsolt Szakonyi, Eniko Forró
1Szegedi Tudományegyetem, Gyógyszerkémiai Intézet, Szeged, Eötvös u. 6. - 6720.
Abstract:
Two-step transformations (N-nitrosation and subsequent LiAlH4 reduction) of alicyclic or acyclic amines and 1,2-amino alcohols containing a secondary amino group were applied to prepare novel N1-substituted hydrazines and hydrazino alcohols with wide structural diversity. Methods for the synthesis of certain enantiopure hydrazino alcohols were also developed. The prepared compounds specifically inhibited Vascular Adhesion Protein-1 (VAP-1), a human endothelial cell adhesion molecule with a well-documented role in inflammation. VAP-1 is a semicarbazide-sensitive amine oxidase, activity of which has been demonstrated to play a role in VAP-1 induced inflammation. Some of the hydrazino alcohols obtained reduced the clinical symptoms of inflammation in experimental arthritis in rodents and appear to be potential novel anti-inflammatory drugs.
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