Bromopyrrole Alkaloids as Lead Compounds against Protozoan Parasites

  title={Bromopyrrole Alkaloids as Lead Compounds against Protozoan Parasites},
  author={Fernando Scala and Ernesto Fattorusso and Marialuisa Prof. Menna and Orazio Taglialatela‐Scafati and Michelle S. Tierney and Marcel Kaiser and Deniz Taşdemir},
  journal={Marine Drugs},
  pages={2162 - 2174}
In the present study, 13 bromopyrrole alkaloids, including the oroidin analogs hymenidin (2), dispacamide B (3) and dispacamide D (4), stevensine (5) and spongiacidin B (6), their derivatives lacking the imidazole ring bromoaldisin (7), longamide B (8) and longamide A (9), the dimeric oroidin derivatives sceptrin (10) and dibromopalau’amine (11), and the non-oroidin bromopyrrolohomoarginin (12), manzacidin A (13), and agelongine (14), obtained from marine sponges belonging to Axinella and… 

Figures and Tables from this paper

Manadoperoxides, a new class of potent antitrypanosomal agents of marine origin.
Interestingly, it appears that minor structural changes, such as a shift of the methyl group around the dioxane ring, can dramatically affect the antitrypanosomal activity.
In Vitro and In Vivo Assessment of the Efficacy of Bromoageliferin, an Alkaloid Isolated from the Sponge Agelas dilatata, against Pseudomonas aeruginosa
The first chemical study of the secondary metabolites of the sponge A. dilatata from the coastal area of the Yucatan Peninsula (Mexico) is reported, confirming bromoageliferin as a potential lead for designing new antibacterial drugs.
Antimicrobial Activity of the Marine Alkaloids, Clathrodin and Oroidin, and Their Synthetic Analogues
The marine alkaloids, clathrodin and oroidin, which were originally isolated from sponges of the genus, Agelas, were prepared and evaluated for their antimicrobial activity against three bacterial strains (Enterococcus faecalis, Staphylococcus aureus and Escherichia coli) and one fungal strain (Candida albicans), and Oroidin was found to possess promising Gram-positive antibacterial activity.
Discovery and development of antiplasmodial compounds in Thailand during the 21st century.
  • S. Auparakkitanon
  • Chemistry, Biology
    The Southeast Asian journal of tropical medicine and public health
  • 2014
The screening and synthesis of novel chemicals targeted against parasite enzymes, (carbonic anhydrase, cy- tochrome bcl, dihydrofolate reductase and orotidine 5'-monophosphate decar- boxylase), which have the potential of being developed into antimalarial drugs are described.
Designed Synthesis of Diversely Substituted Hydantoins and Hydantoin-Based Hybrid Molecules: A Personal Account
This work initiated a research program that successfully designed and developed new routes and methods for the formation of hydantoin, thiohydantin, and iminohydantoin substituted at various positions, particularly at the N-1 position without following a protection–deprotection strategy.
Effect of Elatol, Isolated from Red Seaweed Laurencia dendroidea, on Leishmania amazonensis
It is indicated that elatol is a potent antiproliferative agent against promastigotes and intracellular amastigote forms, and may have important advantages for the development of new anti-leishamanial chemotherapies.
Molecular modeling studies of bromopyrrole alkaloids as potential antimalarial compounds: a DFT approach
In this study, a quantitative structure–activity relationship (QSAR) analysis has been performed on data set of 14 bromopyrrole alkaloids (sponge metabolites) for antimalarial activity, which could suggest some characteristics of novel potent bromocarbon alkaloid against malaria.
A Coralline Algal-Associated Bacterium, Pseudoalteromonas Strain J010, Yields Five New Korormicins and a Bromopyrrole
The ethanol extract of Pseudoalteromonas strain J010, isolated from the surface of the crustose coralline alga Neogoniolithon fosliei, yielded thirteen natural products. These included a new


Efficacy of the diamidine DB75 and its prodrug DB289, against murine models of human African trypanosomiasis.
Triclosan offers protection against blood stages of malaria by inhibiting enoyl-ACP reductase of Plasmodium falciparum
It is demonstrated that the enoyl-ACP reductase purified from P. falciparum is triclosan sensitive and the existence of the de novo fatty acid biosynthetic pathway in this parasite is established, and a key enzyme of this pathway for the development of new antimalarials is identified.
Inhibition of Plasmodium falciparum fatty acid biosynthesis: evaluation of FabG, FabZ, and FabI as drug targets for flavonoids.
Polyphenols of C-3 gallic acid esters of catechins showed in vitro activity against chloroquine-sensitive and -resistant P. falciparum strains in the low to submicromolar range.
Novel bromopyrrole alkaloids from the sponge Agelas dispar.
Further investigation of the Caribbean marine sponge Agelas dispar for biologically active constituents has led to the isolation of the novel bromopyrrole alkaloids longamide B (1), and clathramides
Efficient technique for screening drugs for activity against Trypanosoma cruzi using parasites expressing beta-galactosidase
An assay with beta-galactosidase-expressing T. cruzi greatly simplifies screening drugs for selective anti-T.
Novel bioactive bromopyrrole alkaloids from the Mediterranean sponge Axinella verrucosa.