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• W2005710852 abstract "The interrelationships between physicochemical properties, absorption and potency of 2‐desoxoparaherquamide and five analogs, representing a new anthelmintic class, were evaluated in in vitro and in vivo assays. At pH 7.5, rates of drug absorption by the gastrointestinal nematode Haemonchus contortus and jird small intestine, parameterized by the permeability coefficient, P e , ranged from 1.2–2.4 × 10 −4 cm/min (nematode) to 2.5–5.5 × 10 −3 cm/min (jird). In the jird intestine, absorption was pH‐dependent, with P e at pH 7.5 being twice that at pH 4.5, reflecting the negative influence of protonation on transport of these weakly basic molecules. Each compound rapidly paralyzed H. contortus during in vitro exposure to therapeutically relevant concentrations (1–10 μ m ). The kinetics of drug action on motility in vivo mirrored their in vitro effects; motility concentrations were reduced in nematodes collected from jird stomach 3 h following oral drug dosing, by which time ≥50% clearance of the parasites had occurred. The nematode/medium partition coefficient K ranged from 10.1 to 16.1, consistent with the lipophilic nature of the compounds. The time required to reduce motility in vitro by 50% ( t 50 * ) and P e were used to determine C n * , the concentration of drug in the nematode at t 50 * , as an indicator of intrinsic potency. In the jird, the apparent potencies of the compounds were insensitive to route of administration (i.e. oral = i.v. = i.p. = i.m.) for H. contortus and two other gastrointestinal nematodes, Ostertagia ostertagi and Trichostrongylus colubriformis ; topical administration, however, required three to 10‐fold higher doses for equivalent efficacy." @default.
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• W2005710852 date "2004-06-01" @default.
• W2005710852 modified "2023-10-18" @default.
• W2005710852 title "Interrelationships among physicochemical properties, absorption and anthelmintic activities of 2-desoxoparaherquamide and selected analogs" @default.
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• W2005710852 doi "https://doi.org/10.1111/j.1365-2885.2004.00577.x" @default.
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