Imidazo[1,2-a]pyridine: a Highly Potent Therapeutic Agent Clears Piroplasm Infection In Vitro

Rizk, Mohamed Abdo; El‒Sayed, Shimaa Abd El‒Salam; El-Alfy, El-Sayed; Igarashi, Ikuo

doi:10.1007/s11686-022-00655-w

Cited by 4 publications

(1 citation statement)

References 39 publications

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“…Combination therapies of FLLL-32 with the commonly used (DA, and ID), and the recently identified antibabesial drugs (MMV396693) were evaluated. The combination ratios ranged from 0.50 to 0.75 IC 50 s of the selected drugs (Supplementary Table S1) were prepared as previously described (Rizk et al, 2023). A 96-well plate containing B. bovis, B. bigemina, B. caballi, and T. equi pRBCs was treated with a two-drug combination; FLLL-32+DA, FLLL-32+ID, and FLLL-32+MMV396693 at concentrations of 0.5 x IC 50 and 0.75 x IC 50 in triplicates.…”

Section: In Vitro Growth Inhibition Assay and Viability Testmentioning

confidence: 99%

Antiparasitic activity of FLLL-32 against four Babesia species, B. bovis, B. bigemina, B. divergens and B. caballi, and one Theileria species, Theileria equi in vitro, and Babesia microti in mice

El-Sayed,

El-Alfy,

Baghdadi

et al. 2023

Front. Pharmacol.

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Introduction: FLLL-32, a synthetic analog of curcumin, is a potent inhibitor of STAT3’s constitutive activation in a variety of cancer cells, and its anticancer properties have been demonstrated both in vitro and in vivo. It is also suggested that it might have other pharmacological activities including activity against different parasites.Aim: This study therefore investigated the in vitro antiparasitic activity of FLLL-32 against four pathogenic Babesia species, B. bovis, B. bigemina, B. divergens, and B. caballi, and one Theileria species, Theileria equi. In vivo anti-Babesia microti activity of FLLL-32 was also evaluated in mice.Methods: The FLLL-32, in the growth inhibition assay with a concentration range (0.005–50 μM), was tested for it’s activity against these pathogens. The reverse transcription PCR (RT-PCR) assay was used to evaluate the possible effects of FLLL-32 treatment on the mRNA transcription of the target B. bovis genes including S-adenosylhomocysteine hydrolase and histone deacetylase.Results: The in vitro growth of B. bovis, B. bigemina, B. divergens, B. caballi, and T. equi was significantly inhibited in a dose-dependent manner (in all cases, p < 0.05). FLLL-32 exhibits the highest inhibitory effects on B. bovis growth in vitro, and it’s IC50 value against this species was 9.57 μM. The RT-PCR results showed that FLLL-32 inhibited the transcription of the B. bovis S-adenosylhomocysteine hydrolase gene. In vivo, the FLLL-32 showed significant inhibition (p < 0.05) of B. microti parasitemia in infected mice with results comparable to that of diminazene aceturate. Parasitemia level in B. microti-infected mice treated with FLLL-32 from day 12 post infection (pi) was reduced to reach zero level at day 16 pi when compared to the infected non-treated mice.Conclusion: The present study demonstrated the antibabesial properties of FLLL-32 and suggested it’s usage in the treatment of babesiosis especially when utilized in combination therapy with other antibabesial drugs.

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Section: In Vitro Growth Inhibition Assay and Viability Testmentioning

confidence: 99%

Antiparasitic activity of FLLL-32 against four Babesia species, B. bovis, B. bigemina, B. divergens and B. caballi, and one Theileria species, Theileria equi in vitro, and Babesia microti in mice

El-Sayed,

El-Alfy,

Baghdadi

et al. 2023

Front. Pharmacol.

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Insights into medicinal attributes of imidazo[1,2‐a]pyridine derivatives as anticancer agents

Kumar,

Sharma,

Behl

et al. 2024

Archiv der Pharmazie

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Cancer ranks among the most life‐threatening diseases worldwide and is continuously affecting all age groups. Consequently, many research studies are being carried out to develop new cancer treatments, but many of them experience resistance and cause severe toxicity to the patients. Therefore, there is a continuous need to design novel anticancer agents that are target‐based, have a higher potency, and have minimal toxicity. The imidazo[1,2‐a]pyridine (IP) pharmacophore has been found to be a prominent moiety in the field of medicinal chemistry due to its vast biological properties. Also, it holds immense potential for combating cancer with minimal side effects, depending on the substitution patterns of the core structure. IPs exhibit significant capability in regulating various cellular pathways, offering possibilities for targeted anticancer effects. The present review summarizes the anticancer profile of numerous IP derivatives synthesized and developed by various researchers from 2016 till now, as inhibitors of phosphoinositide‐3‐kinase/mammalian target of rapamycin (PI3K/mTOR), protein kinase B/mammalian target of rapamycin (Akt/mTOR), aldehyde dehydrogenase (ALDH), and tubulin polymerization. This review provides a comprehensive analysis of the anticancer activity afforded by the discussed IP compounds, emphasizing the structure–activity‐relationships (SARs). The aim is also to underscore the potential therapeutic future of the IP moiety as a potent partial structure for upcoming cancer drug development and to aid researchers in the field of rational drug design.

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Visible light-mediated copper catalyzed regioselective diamination of terminal alkynes at room temperature: a facile synthesis of substituted imidazo[1,2-α]pyridines

Charpe,

Gupta,

Hwang

2024

Green Chem.

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Imidazo[1,2-a]pyridine: a Highly Potent Therapeutic Agent Clears Piroplasm Infection In Vitro

Cited by 4 publications

References 39 publications

Antiparasitic activity of FLLL-32 against four Babesia species, B. bovis, B. bigemina, B. divergens and B. caballi, and one Theileria species, Theileria equi in vitro, and Babesia microti in mice

Antiparasitic activity of FLLL-32 against four Babesia species, B. bovis, B. bigemina, B. divergens and B. caballi, and one Theileria species, Theileria equi in vitro, and Babesia microti in mice

Insights into medicinal attributes of imidazo[1,2‐a]pyridine derivatives as anticancer agents

Visible light-mediated copper catalyzed regioselective diamination of terminal alkynes at room temperature: a facile synthesis of substituted imidazo[1,2-α]pyridines

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