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In vitro screening and potency determination of carbazole aminoalcohols (CAAs) against Cryptosporidium parvum . (A) General chemical structure of carbazole aminoalcohols, showing the tricyclic carbazole core (cores 1–4) and the variable aminoalcohol side chains. (B) Workflow of the screening strategy used in this study: 36 CAA analogues were screened in vitro, eight hits were selected for dose–response analysis, and three top hits were subsequently evaluated in vivo. (C) Percent inhibition of parasite growth at 2.5 μM and 5 μM for all 36 CAAs, quantified <t>by</t> <t>qRT-PCR</t> in a 44-h infection assay. (D) Dose–response curves for the three selected hits showing EC 50 values. Data represent means of three biological replicates, with technical duplicates per replicate. (E) Chemical structures of the eight most active analogues (core type and side chain indicated). In vitro efficacy (EC 50 values), cytotoxicity on HCT-8 cells (TC 50 values), and selectivity indices (SI = TC 50 /EC 50 ) are provided for each compound.
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In vitro screening and potency determination of carbazole aminoalcohols (CAAs) against Cryptosporidium parvum . (A) General chemical structure of carbazole aminoalcohols, showing the tricyclic carbazole core (cores 1–4) and the variable aminoalcohol side chains. (B) Workflow of the screening strategy used in this study: 36 CAA analogues were screened in vitro, eight hits were selected for dose–response analysis, and three top hits were subsequently evaluated in vivo. (C) Percent inhibition of parasite growth at 2.5 μM and 5 μM for all 36 CAAs, quantified <t>by</t> <t>qRT-PCR</t> in a 44-h infection assay. (D) Dose–response curves for the three selected hits showing EC 50 values. Data represent means of three biological replicates, with technical duplicates per replicate. (E) Chemical structures of the eight most active analogues (core type and side chain indicated). In vitro efficacy (EC 50 values), cytotoxicity on HCT-8 cells (TC 50 values), and selectivity indices (SI = TC 50 /EC 50 ) are provided for each compound.
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In vitro screening and potency determination of carbazole aminoalcohols (CAAs) against Cryptosporidium parvum . (A) General chemical structure of carbazole aminoalcohols, showing the tricyclic carbazole core (cores 1–4) and the variable aminoalcohol side chains. (B) Workflow of the screening strategy used in this study: 36 CAA analogues were screened in vitro, eight hits were selected for dose–response analysis, and three top hits were subsequently evaluated in vivo. (C) Percent inhibition of parasite growth at 2.5 μM and 5 μM for all 36 CAAs, quantified <t>by</t> <t>qRT-PCR</t> in a 44-h infection assay. (D) Dose–response curves for the three selected hits showing EC 50 values. Data represent means of three biological replicates, with technical duplicates per replicate. (E) Chemical structures of the eight most active analogues (core type and side chain indicated). In vitro efficacy (EC 50 values), cytotoxicity on HCT-8 cells (TC 50 values), and selectivity indices (SI = TC 50 /EC 50 ) are provided for each compound.
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In vitro screening and potency determination of carbazole aminoalcohols (CAAs) against Cryptosporidium parvum . (A) General chemical structure of carbazole aminoalcohols, showing the tricyclic carbazole core (cores 1–4) and the variable aminoalcohol side chains. (B) Workflow of the screening strategy used in this study: 36 CAA analogues were screened in vitro, eight hits were selected for dose–response analysis, and three top hits were subsequently evaluated in vivo. (C) Percent inhibition of parasite growth at 2.5 μM and 5 μM for all 36 CAAs, quantified by qRT-PCR in a 44-h infection assay. (D) Dose–response curves for the three selected hits showing EC 50 values. Data represent means of three biological replicates, with technical duplicates per replicate. (E) Chemical structures of the eight most active analogues (core type and side chain indicated). In vitro efficacy (EC 50 values), cytotoxicity on HCT-8 cells (TC 50 values), and selectivity indices (SI = TC 50 /EC 50 ) are provided for each compound.

Journal: International Journal for Parasitology: Drugs and Drug Resistance

Article Title: Anti-cryptosporidial efficacy of tricyclic carbazole aminoalcohols in vitro and in vivo

doi: 10.1016/j.ijpddr.2026.100631

Figure Lengend Snippet: In vitro screening and potency determination of carbazole aminoalcohols (CAAs) against Cryptosporidium parvum . (A) General chemical structure of carbazole aminoalcohols, showing the tricyclic carbazole core (cores 1–4) and the variable aminoalcohol side chains. (B) Workflow of the screening strategy used in this study: 36 CAA analogues were screened in vitro, eight hits were selected for dose–response analysis, and three top hits were subsequently evaluated in vivo. (C) Percent inhibition of parasite growth at 2.5 μM and 5 μM for all 36 CAAs, quantified by qRT-PCR in a 44-h infection assay. (D) Dose–response curves for the three selected hits showing EC 50 values. Data represent means of three biological replicates, with technical duplicates per replicate. (E) Chemical structures of the eight most active analogues (core type and side chain indicated). In vitro efficacy (EC 50 values), cytotoxicity on HCT-8 cells (TC 50 values), and selectivity indices (SI = TC 50 /EC 50 ) are provided for each compound.

Article Snippet: Quantification of parasite and host nucleic acids was performed using a one-step qRT-PCR SYBR Green kit (HiScript II, Vazyme) on a StepOnePlus real-time PCR system (Applied Biosystems).

Techniques: In Vitro, Analogues, In Vivo, Inhibition, Quantitative RT-PCR, Infection