Antiamoebic activity of 3-aryl-6,7-dimethoxyquinazolin-4(3H)-one library against Acanthamoeba castellanii

Shahbaz, Muhammad Saquib; Anwar, Ayaz; Saad, Syed Muhammad; Kanwal,; Ali, Anwar; Khan, Khalid Mohammed; Siddiqui, Ruqaiyyah; Khan, Naveed Ahmed

doi:10.1007/s00436-020-06710-7

Cited by 9 publications

(7 citation statements)

References 45 publications

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“…To address these effects, the wells were inspected through a light microscope (magnification 40×), and those wells containing crystals were excluded from the analysis. Previous inhibition assays have used Trypan blue and a hemocytometer to determine the cell count, , which overcomes the problems caused by crystal formation. However, using a hemocytometer introduces the risk that the medium sample in the hemocytometer does not necessarily represent the density of cells in the whole assay.…”

Section: Discussionmentioning

confidence: 99%

Novel Drug Screening Assay for Acanthamoeba castellanii and the Anti-Amoebic Effect of Carbonic Anhydrase Inhibitors

Haapanen,

Barker,

Carta

et al. 2023

J. Med. Chem.

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Acanthamoeba castellanii is an amoeba that inhabits soil and water in every part of the world. Acanthamoeba infection of the eye causes keratitis and can lead to a loss of vision. Current treatment options are only moderately effective, have multiple harmful side effects, and are tedious. In our study, we developed a novel drug screening method to define the inhibitory properties of potential new drugs against A. castellanii in vitro. We found that the clinically used carbonic anhydrase inhibitors, acetazolamide, ethoxzolamide, and dorzolamide, have promising antiamoebic properties.

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Section: Discussionmentioning

confidence: 99%

Novel Drug Screening Assay for Acanthamoeba castellanii and the Anti-Amoebic Effect of Carbonic Anhydrase Inhibitors

Haapanen,

Barker,

Carta

et al. 2023

J. Med. Chem.

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“…For example, a group of researchers have studied the effects of povidone-iodine against Acanthamoeba cysts and trophozoites, and they found that a 0.5 to 2.5% solution exhibits a good amount of antiamoebic activity [ 23 ]. Another group of researchers studied the effects of dihydropyridines synthesized by cyclic dimerization of alkylidene malononitrile derivatives for their antiamoebic activity; their results concluded the efficacy of the compounds against A. castellanii cysts and trophozoites [ 24 ].…”

Section: Discussionmentioning

confidence: 99%

Synthesis and Evaluation of Novel DNA Minor Groove Binders as Antiamoebic Agents

et al. 2022

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The free-living amoeba Acanthamoeba castellanii is responsible for the central nervous infection granulomatous amoebic encephalitis and sight-threatening infection Acanthamoeba keratitis. Moreover, no effective treatment is currently present, and a combination drug therapy is used. In this study, twelve DNA minor groove binders (MGBs) were synthesized and tested for their antiamoebic activity via amoebicidal, encystation, excystation, and cytopathogenicity assays. It was found that the compounds MGB3, MGB6, MGB22, MGB24, and MGB16 significantly reduce amoeba viability to 76.20%, 59.45%, 66.5%, 39.32%, and 43.21%, respectively, in amoebicidal assays. Moreover, the compounds MGB6, MGB20, MGB22, MGB28, MGB30, MGB32, and MGB16 significantly inhibit Acanthamoeba cysts, leading to the development of only 46.3%, 39%, 30.3%, 29.6%, 27.8%, 41.5%, and 45.6% cysts. Additionally, the compounds MGB3, MGB4, MGB6, MGB22, MGB24, MGB28, MGB32, and MGB16 significantly reduce the re-emergence of cysts to trophozoites, with viable trophozoites being only 64.3%, 47.3%, 41.4%, 52.9%, 55.4%, 40.6%, 62.1%, and 51.7%. Moreover, the compounds MGB3, MGB4, and MGB6 exhibited the greatest reduction in amoeba-mediated host-cell death, with cell death reduced to 41.5%, 49.4%, and 49.5%. With the following determined, future in vivo studies can be carried out to understand the effect of the compounds on animal models such as mice.

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“…In medicinal chemistry, the quinazoline class of heterocyclic compounds represents a potential platform against several diseases. 67,68 To date, several investigations have been reported on the biological activities of quinazoline analogues such as fungicidal, antileishmanial, antitrauma activities, antiviral, antitumour, and antibacterial. [69][70][71][72][73] Quinazolines are also used in agrochemical and pharmaceutical industries.…”

Section: Quinazolinones (Qnzs)mentioning

confidence: 99%

“…Medicinally quinazolinones are very important class of compounds, since they have shown a great potential against Acanthamoeba castellanii. 68 Our group recently synthesised a new library of 19 compounds. All of these compounds were derived from 3-aryl-6,7-dimethoxyquinazolin-4(3H)-one.…”

Section: Quinazolinones (Qnzs)mentioning

confidence: 99%

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Applications of medicinal chemistry for drug discovery against Acanthamoeba infections

Ahmed

Anwar

Ong

et al. 2021

Medicinal Research Reviews

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Acanthamoeba is a genus of free‐living amoebae, pervasively found in the environment. Most of its pathogenic species are the causative agent of sight‐threatening Acanthamoeba keratitis and fatal granulomatous amoebic encephalitis. Despite the advancements in the field of chemotherapy, treating Acanthamoeba infections is still challenging due to incomplete knowledge of the complicated pathophysiology. In case of infection, the treatment regimen for the patients is often ineffective due to delayed diagnosis, poor specificity, and side‐effects. Besides the resistance of Acanthamoeba cysts to most of the drugs, the recurrence of infection further complicates the recovery. Thus, it is necessary to develop an effective treatment which can eradicate these rare, but serious infections. Based on various computational and in vitro studies, it has been established that the synthetic scaffolds such as heterocyclic compounds may act as potential drug leads for the development of antiamoebic drugs. In this review, we report different classes of synthetic compounds especially heterocyclic compounds which have shown promising results against Acanthamoeba. Moreover, the antiamoebic activities of synthetic compounds with their possible mode of actions against Acanthamoeba, have been summarized and discussed in this review.

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Antiamoebic activity of 3-aryl-6,7-dimethoxyquinazolin-4(3H)-one library against Acanthamoeba castellanii

Cited by 9 publications

References 45 publications

Novel Drug Screening Assay for Acanthamoeba castellanii and the Anti-Amoebic Effect of Carbonic Anhydrase Inhibitors

Novel Drug Screening Assay for Acanthamoeba castellanii and the Anti-Amoebic Effect of Carbonic Anhydrase Inhibitors

Synthesis and Evaluation of Novel DNA Minor Groove Binders as Antiamoebic Agents

Applications of medicinal chemistry for drug discovery against Acanthamoeba infections

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