Bis-alkylamineIndolo[3,2-b]quinolines as hemozoin ligands: implications for antimalarialcytostatic and cytocidal activities

Authors: Charneira C, Figueiras M, Gut J, Lavrado J, Lopes D, Machado M, Moreira R, Nogueira F, Paulo A, Rosenthal PJ, Santos SA
Publication Year: 2014
Journal: Journal of Medicinal Chemistry
Link: http://www.ncbi.nlm.nih.gov/pubmed/24673163

To get insight into the relevance of targeting hemozoin (Hz) crystals, two isomeric series, N5,N10-bis-alkylamine (2a-k) and N10,O11-bis-alkylamine (3a-k) indolo[3,2-b]quinolines, were evaluated for their in vitro activity against chloroquine (CQ)-resistant and sensitive strains of Plasmodium falciparum.
Read More

Probing the aurone scaffold against Plasmodium falciparum: design, synthesis and antimalarial activity

Authors: Carrasco MP, dos Santos DJ, Gois A, Gonçalves L, Guedes RC, Gut J, Hänscheid T, Machado M, Moreira R, Newton AS, Nogueira F, Rosenthal PJ
Publication Year: 2014
Journal: European Journal of Medicinal Chemistry
Link: http://www.ncbi.nlm.nih.gov/pubmed/24813880

A library comprising 44 diversely substituted aurones derivatives was synthesized by straightforward aldol condensation reactions of benzofuranones and the appropriately substituted benzaldehydes. Microwave enhanced synthesis using palladium catalyzed protocols was introduced as a powerful strategy for extending the chemical space around the aurone scaffold.
Read More

N-Cinnamoylation of Antimalarial Classics: Effects of Using Acyl Groups Other than Cinnamoyl toward Dual-Stage Antimalarials

Authors: Gomes A, Gomes P, Lobo L, Machado M, Nogueira F, Prudencio M, Teixeira C
Publication Year: 2015
Journal: Chemmedchem
Link: http://www.ncbi.nlm.nih.gov/pubmed/26038181

In a follow-up study to our reports of N-cinnamoylated chloroquine and quinacrine analogues as promising dual-stage antimalarial leads with high in vitro potency against both blood-stage Plasmodium falciparum and liver-stage Plasmodium berghei, we decided to investigate the effect of replacing the cinnamoyl moiety with other acyl groups. Thus, a series of N-acylated analogues were synthesized, and their activities against blood- and liver-stage Plasmodium spp. were assessed along with their in vitro cytotoxicities.
Read More

Treatment of plasmodium chabaudi parasites with curcumin in combination with antimalarial drugs: Drug interactions and implications on the ubiquitin/proteasome system

Authors: Do Rosário V, Gazarini ML, Lindeza A, Lopes D, Machado M, Neto Z
Publication Year: 2013
Journal: Journal of Parasitology Research
Link: http://www.ncbi.nlm.nih.gov/pubmed/23691276

Antimalarial drug resistance remains a major obstacle in malaria control. Evidence from Southeast Asia shows that resistance to artemisinin combination therapy (ACT) is inevitable. Ethnopharmacological studies have confirmed the efficacy of curcumin against Plasmodium spp.
Read More

A review of antimalarial plants used in traditional medicine in communities in Portuguese-speaking countries: Brazil, Mozambique, Cape Verde, Guinea-Bissau, São Tomé and Príncipe and Angola.

The isolation of bioactive compounds from medicinal plants, based on traditional use or ethnomedical data, is a highly promising potential approach for identifying new and effective antimalarial drug candidates.
Read More

Bis-alkylamineIndolo[3,2-b]quinolines as hemozoin ligands: implications for antimalarialcytostatic and cytocidal activities

Probing the aurone scaffold against Plasmodium falciparum: design, synthesis and antimalarial activity

N-Cinnamoylation of Antimalarial Classics: Effects of Using Acyl Groups Other than Cinnamoyl toward Dual-Stage Antimalarials

Treatment of plasmodium chabaudi parasites with curcumin in combination with antimalarial drugs: Drug interactions and implications on the ubiquitin/proteasome system

A review of antimalarial plants used in traditional medicine in communities in Portuguese-speaking countries: Brazil, Mozambique, Cape Verde, Guinea-Bissau, São Tomé and Príncipe and Angola.

About GHTM

Contacts

Funding