A novel class of fast‐acting antimalarial agents: Substituted 15‐membered azalides

M Peric, D Pešić, S Alihodžić, A Fajdetić… - British journal of …, 2021 - Wiley Online Library
Background and Purpose Efficacy of current antimalarial treatments is declining as a result
of increasing antimalarial drug resistance, so new and potent antimalarial drugs are urgently …

Antimalarial Activity of 9a-N Substituted 15-Membered Azalides with Improved in Vitro and in Vivo Activity over Azithromycin

M Perić, A Fajdetić, R Rupčić… - Journal of medicinal …, 2012 - ACS Publications
Novel classes of antimalarial drugs are needed due to emerging drug resistance.
Azithromycin, the first macrolide investigated for malaria treatment and prophylaxis, failed as …

Design, Synthesis, and in Vitro Activity of Novel 2′-O-Substituted 15-Membered Azalides

D Pešić, K Starčević, A Toplak… - Journal of medicinal …, 2012 - ACS Publications
Malaria remains one of the most widespread human infectious diseases, and its eradication
will largely depend on antimalarial drug discovery. Here, we present a novel approach to the …

Novel hybrid molecules based on 15-membered azalide as potential antimalarial agents

K Starčević, D Pešić, A Toplak, G Landek… - European journal of …, 2012 - Elsevier
Malaria remains the most prevalent tropical disease, and due to the spread of resistant
parasites novel therapeutics are urgently needed. Azithromycin has shown potential in …

Synthesis, structure–activity relationship, and antimalarial activity of ureas and thioureas of 15-membered azalides

M Bukvić Krajačić, M Peric, KS Smith… - Journal of medicinal …, 2011 - ACS Publications
Azithromycin, a first member of the azalide family of macrolides, while having substantial
antimalarial activity, failed as a single agent for malaria prophylaxis. In this paper we present …

[HTML][HTML] Targeting malaria parasites with novel derivatives of azithromycin

AL Burns, BE Sleebs, M Gancheva… - Frontiers in Cellular …, 2022 - frontiersin.org
Introduction The spread of artemisinin resistant Plasmodium falciparum parasites is of global
concern and highlights the need to identify new antimalarials for future treatments …

[HTML][HTML] Retargeting azithromycin analogues to have dual-modality antimalarial activity

AL Burns, BE Sleebs, G Siddiqui, AE De Paoli… - BMC biology, 2020 - Springer
Background Resistance to front-line antimalarials (artemisinin combination therapies) is
spreading, and development of new drug treatment strategies to rapidly kill Plasmodium …

Identification of novel quinazoline derivatives as potent antiplasmodial agents

A Bouchut, D Rotili, C Pierrot, S Valente… - European Journal of …, 2019 - Elsevier
Despite the recent reductions in the global burden of malaria, this disease remains a
devastating cause of death in tropical and subtropical regions. As there is no broadly …

An automated, polymer-assisted strategy for the preparation of urea and thiourea derivatives of 15-membered azalides as potential antimalarial chemotherapeutics

A Hutinec, R Rupčić, D Žiher, KS Smith… - Bioorganic & medicinal …, 2011 - Elsevier
A series of 15-membered azalide urea and thiourea derivatives has been synthesized and
evaluated for their in vitro antimalarial activity against chloroquine-sensitive (D6) …

Aminoazabenzimidazoles, a novel class of orally active antimalarial agents

S Hameed P, M Chinnapattu, G Shanbag… - Journal of Medicinal …, 2014 - ACS Publications
Whole-cell high-throughput screening of the AstraZeneca compound library against the
asexual blood stage of Plasmodium falciparum (Pf) led to the identification of amino …