1, 2, 4-Triazolo [1, 5-a] pyrimidines in drug design

K Oukoloff, B Lucero, KR Francisco, KR Brunden… - European journal of …, 2019 - Elsevier
Abstract The 1, 2, 4-triazolo [1, 5-a] pyrimidine (TP) heterocycle, in spite of its relatively
simple structure, has proved to be remarkably versatile as evidenced by its use in many …

Synthetic approaches to the 2015–2018 new agrochemicals

S Jeanmart, AJF Edmunds, C Lamberth… - Bioorganic & Medicinal …, 2021 - Elsevier
In this review, the synthesis of 33 agrochemicals that received an international
standardization organization (ISO) name between January 2015 and December 2018 is …

Biological activities of [1,2,4]triazolo[1,5-a]pyrimidines and analogs

S Pinheiro, EMC Pinheiro, EMF Muri… - Medicinal Chemistry …, 2020 - Springer
Abstract The [1, 2, 4] triazolo [1, 5-a] pyrimidines (TPs) comprise an important class of non-
naturally occurring small molecules that aroused the interest of researches. This scaffold is …

[HTML][HTML] Structure-activity relationship of dibenzylideneacetone analogs against the neglected disease pathogen, Trypanosoma brucei

KR Francisco, L Monti, W Yang, H Park, LJ Liu… - Bioorganic & medicinal …, 2023 - Elsevier
Trypanosoma brucei is a protozoan parasite that causes Human African Trypanosomiasis
(HAT), a neglected tropical disease (NTD) that is endemic in 36 countries in sub-Saharan …

From rational design to serendipity: discovery of novel thiosemicarbazones as potent trypanocidal compounds

SFP Braga, VC Santos, RP Vieira, EB da Silva… - European Journal of …, 2022 - Elsevier
Chagas disease is a major public health problem caused by Trypanosoma cruzi, with an
estimated 6–7 million people infected and 70 million at risk of infection. T. brucei gambiense …

Coumarin-based derivatives targeting Trypanosoma cruzi cruzain and Trypanosoma brucei cathepsin L-like proteases

JA Nunes, FN da Silva, EB da Silva… - New Journal of …, 2023 - pubs.rsc.org
The protozoa, Trypanosoma cruzi (etiological agent of Chagas diseases–also named
American trypanosomiasis) and T. brucei (causative agent of human African …

[HTML][HTML] Identification of anisomycin, prodigiosin and obatoclax as compounds with broad-spectrum anti-parasitic activity

G Ehrenkaufer, P Li, EE Stebbins… - PLoS neglected …, 2020 - journals.plos.org
Parasitic infections are a major source of human suffering, mortality, and economic loss, but
drug development for these diseases has been stymied by the significant expense involved …

Structure‐Activity Relationships, Tolerability and Efficacy of Microtubule‐Active 1,2,4‐Triazolo[1,5‐a]pyrimidines as Potential Candidates to Treat Human African …

L Monti, LJ Liu, C Varricchio, B Lucero, T Alle… - …, 2023 - Wiley Online Library
Tubulin and microtubules (MTs) are potential protein targets to treat parasitic infections and
our previous studies have shown that the triazolopyrimidine (TPD) class of MT‐active …

[HTML][HTML] Tubulin inhibitors. Selected scaffolds and main trends in the design of novel anticancer and antiparasitic agents

M Podolak, S Holota, Y Deyak, K Dziduch… - Bioorganic …, 2023 - Elsevier
Abstract Design of tubulin inhibitors as anticancer drugs dynamically developed over the
past 20 years. The modern arsenal of potential tubulin-targeting anticancer agents is …

[HTML][HTML] Anti-trypanosomal and antimalarial properties of tetralone derivatives and structurally related benzocycloalkanones

RM Beteck, LJ Legoabe, M Isaacs, SD Khanye… - Medicina, 2019 - mdpi.com
Background and objectives: Sleeping sickness and malaria alike are insect-borne protozoan
diseases that share overlapping endemic areas in sub-Saharan Africa. The causative agent …