Novel carbazole aminoalcohols as inhibitors of β -hematin formation: Antiplasmodial and antischistosomal activities

Wang, Weisi; Li, Qiang; Wei, Yufen; Xue, Jing-Bo; Sun, Xiao; Yang, Yu; Chen, Zhuo; Li, Shi-Zhu; Duan, Liping

doi:10.1016/j.ijpddr.2017.03.007

Cited by 15 publications

(8 citation statements)

References 36 publications

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“…Spectroscopic investigations revealed that 100 possessed a promising binding affinity with free heme moieties (IC 50 = 55.43 ± 6.78 µM) . Duan et al identified a series of novel carbazole amino alcohols ( 102 ) as potential antiplasmodial and antischistosomal agents and correlated the inhibitory activity of β‐hematin formation and antiparasitic activity through investigations on dual antiparasitic mechanisms . The xanthone derivatives were extracted from the sea urchin Strongylocentrotus purpuratus , and the identification of the antimalarial activity was serendipitous .…”

Section: Pigments Of Representative Colored Pathogens and Their Inhibmentioning

confidence: 99%

Targeting virulence factors as an antimicrobial approach: Pigment inhibitors

et al. 2019

Medicinal Research Reviews

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The fascinating and dangerous colored pathogens contain unique chemically pigmented molecules, which give varied and efficient assistance as virulence factors to the crucial reproduction and growth of microbes. Therefore, multiple novel strategies and inhibitors have been developed in recent years that target virulence factor pigments. However, despite the importance and significance of this topic, it has not yet been comprehensively reviewed. Moreover, research groups around the world have made successful progress against antibacterial infections by targeting pigment production, including our serial works on the discovery of CrtN inhibitors against staphyloxanthin production in Staphylococcus aureus. On the basis of the previous achievements and recent progress of our group in this field, this article will be the first comprehensive review of pigment inhibitors against colored pathogens, especially S. aureus infections, and this article includes design strategies, representative case studies, advantages, limitations, and perspectives to guide future research.

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Section: Pigments Of Representative Colored Pathogens and Their Inhibmentioning

confidence: 99%

Targeting virulence factors as an antimicrobial approach: Pigment inhibitors

et al. 2019

Medicinal Research Reviews

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“…This skeleton is present in many biologically active compounds [ [26] , [27] , [28] ]. One of the most important properties of the carbazole-core agent is antiplasmodial activity [ [29] , [30] , [31] ]. Many recently published reports confirmed also that carbazole-based compounds exert promising antibacterial [ 32 ], antiviral [ 33 ], antifungal [ 34 ] and antiparasite [ 35 ] activities.…”

Section: Introductionmentioning

confidence: 99%

Azacarbazole n-3 and n-6 polyunsaturated fatty acids ethyl esters nanoemulsion with enhanced efficacy against Plasmodium falciparum

Jaromin

Parapini

Zaremba-Czogalla

et al. 2021

Bioactive Materials

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Alternative therapies are necessary for the treatment of malaria due to emerging drug resistance. However, many promising antimalarial compounds have poor water solubility and suffer from the lack of suitable delivery systems, which seriously limits their activity. To address this problem, we synthesized a series of azacarbazoles that were evaluated for antimalarial activity against D10 (chloroquine-sensitive) and W2 (chloroquine-resistant) strains of P. falciparum . The most active compound, 9 H -3-azacarbazole ( 3 ), was encapsulated in a novel o/w nanoemulsion consisting of ethyl esters of polyunsaturated fatty acids n-3 and n-6 obtained from flax oil as the oil phase, S mix (Tween 80 and Transcutol HP) and water. This formulation was further analyzed using transmission electron microscopy, dynamic light scattering and in vitro and in vivo studies. It was shown that droplets of the 3 -loaded nanosystem were spherical, with satisfactory stability, without cytotoxicity towards fibroblasts and intestinal cell lines at concentrations corresponding to twice the IC 50 for P. falciparum . Moreover, the nanoemulsion with this type of oil phase was internalized by Caco-2 cells. Additionally, pharmacokinetics demonstrated rapid absorption of compound 3 (t max = 5.0 min) after intragastric administration of 3 -encapsulated nanoemulsion at a dose of 0.02 mg/kg in mice, with penetration of compound 3 to deep compartments. The 3 -encapsulated nanoemulsion was found to be 2.8 and 4.2 times more effective in inhibiting the D10 and W2 strains of the parasite, respectively, compared to non-encapsulated 3 . Our findings support a role for novel o/w nanoemulsions as delivery vehicles for antimalarial drugs.

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“…Compound 20a Antiplasmodial and antischistosomal activities: Weisi Wang et al (2017) synthesized carbazole amino alcohols derivatives. The compounds were tested for invitro anti-plasmodial and antischistosomal activity againstPlasmodium falciparum 3D7 and Dd2 strains and adult and juvenileSchistosoma japonicum.by P. falciparum whole cell assay using Chloroquine and dihydroartemisinin as stanadard drugs.The result shows that the compound 21a exhibit potent dual anti-parasitic activities27 .…”

mentioning

confidence: 99%

A Review on Biological Activity of Heterocyclic Nucleus Carbazole

Meghani

Mahawar

Sharma

et al. 2020

Asian J Pharm Res Dev

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Alzheimer’s disease (AD) is a progressive neurodegenerative disorder associated with cognitive deterioration affecting day to day living and behavioural activities. It is commonest cause of senile and pre-senile dementia. In Alzheimer’s disease, a peptide referred as amyloid beta aggregates (oligomers), and accumulates in the brain to form deposits called as amyloid plaques. According to the world health organization (WHO), 5% of men and 6% of women of above 60 years are victims with Alzheimer’s type dementia globally. In India prevalence of dementia is 33.6%, of which AD contributes approximately 54% and vascular dementia constitutes approximately 39%. Patients with the prolonged use of some Non-steroidal anti-inflammatory (NSAID) drugs such as ibuprofen have lower risk of developing the symptoms of AD; however the chronic use of NSAID can produce a toxic effect on the kidney, liver and GI tract. Recent studies have demonstrated that a curcumin delivery system based on nanoscience and nanotechnology increases the therapeutic potential of this compound. Specifically, several nano-sized carriers such as phospholipid vesicles (liposomes), micelles, solid lipid nanoparticles, polymeric nanoparticles, emulsions, proteins and other molecular complexes have been developed for the efficient delivery of curcumin. Nano particles have demonstrated the enhanced Bioavailability of curcumin including circulation time in the blood. Various nano technology drug delivery system of curcumin showed increased Bio accessibility during treatment of Alzheimer’s disease.

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Novel carbazole aminoalcohols as inhibitors of β -hematin formation: Antiplasmodial and antischistosomal activities

Cited by 15 publications

References 36 publications

Targeting virulence factors as an antimicrobial approach: Pigment inhibitors

Targeting virulence factors as an antimicrobial approach: Pigment inhibitors

Azacarbazole n-3 and n-6 polyunsaturated fatty acids ethyl esters nanoemulsion with enhanced efficacy against Plasmodium falciparum

A Review on Biological Activity of Heterocyclic Nucleus Carbazole

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