Insights into the structural patterns of the antileishmanial activity of bi- and tricyclic N-heterocycles

Lizzi Herrera; David E. Stephens; Abigail D'Avila; Kathryn G. George; Hadi D. Arman; Yu Zhang; George Perry; Ricardo Lleonart; Oleg V. Larionov; Patricia L. Fernández

doi:10.1039/c6ob01149g

Back

Shared by

George Perry

Insights into the structural patterns of the antileishmanial activity of bi- and tricyclic N-heterocycles

Article 2016 en

Authors

LH
Lizzi Herrera
DS
David E. Stephens
AD
Abigail D'Avila

Abstract

1 min read

The influence of various structural patterns in a series of novel bi- and tricyclic N-heterocycles on the activity against Leishmania major and Leishmania panamensis has been studied and compounds that are active in the low micromolar region have been identified. Both quinolines and tetrahydrooxazinoindoles (TOI) proved to have significant antileishmanial activities, while substituted indoles were inactive. We have also showed that a chloroquine analogue induces Leishmania killing by modulating macrophage activation.

Discussion(0)

No comments yet. Be the first to comment.

Related publications

Article1998

Regiospecific Synthesis and Anti-Human Immunodeficiency Virus Activity of Novel 5-Substituted N-Alkylcarbamoyl and N,N-Dialkyl Carbamoyl 1,2,3-Triazole-TSAO Analogues

Sonsoles Velázquez, Rosa Álvarez, Carlos A. Perez, Federico Gago, De Clercq Erik, Jan Balzarini, Marı́a-José Camarasa

Article2002

Comparative Study of Bis(Benzyl)Phosphate Triesters of 2′,3′-Dideoxy-2′,3′-Didehydrothymidine (d4T) andCycloSal-d4TMP — Hydrolysis, Mechanistic Insights and Anti-HIV Activity

Chris Meier, Ulrike Muus, Jürgen Renze, Lieve Naesens, De Clercq Erik, Jan Balzarini

Article1991

Geiparvarin analogs. 2. Synthesis and cytostatic activity of 5-(4-arylbutadienyl)-3(2H)-furanones and of N-substituted 3-(4-oxo-2-furanyl)-2-buten-2-yl carbamates

Daniele Simoni, Stefano Manfredini, Mojgan Aghazadeh Tabrizi, Rita Bazzanini, Pier Giovanni Baraldi, Jan Balzarini, De Clercq Erik

Article2003

Structural Complementarity of Toll/Interleukin-1 Receptor Domains in Toll-like Receptors and the Adaptors Mal and MyD88

Aisling Dunne, Mikael Ejdebäck, Phumzile L. Ludidi, Luke O'neill, Nicholas J. Gay

Journal of Biological Chemistry

Preprint2023

Author response: Regulation of inflammation and protection against invasive pneumococcal infection by the long pentraxin PTX3

Rémi Porte, Rita Silva-Gomes, Charlotte Théroude, Raffaella Parente, Fatemeh Asgari, Marina Sironi, Fabio Pasqualini, Sonia Valentino, Rosanna Asselta, Camilla Recordati, Marta Monari, Andrea Doni, Antonio Inforzato, Carlos Rodríguez‐Gallego, Ignacio Obando, Elena Colino, Barbara Bottazzi, Alberto Mantovani

Insights into the structural patterns of the antileishmanial activity of bi- and tricyclic N-heterocycles

Abstract

Discussion(0)

Related publications

Regiospecific Synthesis and Anti-Human Immunodeficiency Virus Activity of Novel 5-Substituted <i>N</i>-Alkylcarbamoyl and <i>N,N</i>-Dialkyl Carbamoyl 1,2,3-Triazole-TSAO Analogues

Comparative Study of Bis(Benzyl)Phosphate Triesters of 2′,3′-Dideoxy-2′,3′-Didehydrothymidine (d4T) and<i>Cyclo</i>Sal-d4TMP — Hydrolysis, Mechanistic Insights and Anti-HIV Activity

Geiparvarin analogs. 2. Synthesis and cytostatic activity of 5-(4-arylbutadienyl)-3(2H)-furanones and of N-substituted 3-(4-oxo-2-furanyl)-2-buten-2-yl carbamates

Structural Complementarity of Toll/Interleukin-1 Receptor Domains in Toll-like Receptors and the Adaptors Mal and MyD88

Author response: Regulation of inflammation and protection against invasive pneumococcal infection by the long pentraxin PTX3