Wayne State University

Unversität Zürich

University of Georgia Research Foundation Inc

David Crich

Andrea Vasella

Sven N Hobbie

Erik C Bottger

Vikram Sarpe

Amr Sonousi

Takayuki Kato

Guanyu Yang

Girish Sati

Appi Reddy Mandhapati

Jonathan Quirke

Parasuraman Rajasekaran

Michael G Pirrone

Asiri Hettikankanamalage

Jarvis Hill

In one aspect, the disclosure relates to a method for the direct synthesis of complex N,N,O-trisubstituted hydroxylamines by N—O bond formation. In another aspect, the method can successfully be employed using a wide variety of commercially available alcohols and secondary amines and enables the construction of large fragment-based libraries of trisubstituted hydroxylamines for drug discovery purposes. Also disclosed are N,N,O-trisubstituted hydroxylamines having low basicity, high stability at ambient temperatures, and an inherent lack of reactivity towards acetylating and sulfonylating enzymes that confer mutagenicity on less-substituted hydroxylamines.

Diversity-oriented synthesis of N,N,O-trisubstituted hydroxylamines from alcohols and amines by N—O bond formation

The invention relates to derivatives of apramycin-based aminoglycoside antibacterial drugs modified in positions C5 and/or C6 and O5 and/or O6. The modifications impart favourable properties regarding increased selectivity and retention of activity in the presence of resistance determinants of the AAC(3) class. The invention further relates to said compounds for use in the therapy of bacterial infection by systemic administration, especially in instances where the infection is caused by a pathogen comprising a resistance determinant of the AAC(3) class, in particular AAC(3)-IV.

Apramycin derivatives

The present disclosure relates to derivatives of neamine-based aminoglycoside antibacterial drugs modified in position C6', C2&#x2032; and/or C5&#x2033;. The modifications impart favorable properties regarding activity against ESKAPE pathogens, evasion of resistance traits and increased selectivity, enabling systemic use of the compounds.

Neomycin and paromomycin derivatives

Growing community of inventors

Detroit, MI, United States of America

David Crich