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4 results on '"Wagerle T"'

1. A Catalyst that Plays Multiple Roles:  Asymmetric Synthesis of β-Substituted Aspartic Acid Derivatives through a Four-Stage, One-Pot Procedure

Author

Dudding, T., Hafez, A. M., Taggi, A. E., Wagerle, T. R., and Lectka, T.

Abstract

We report a new method for the catalytic, asymmetric synthesis of β-substituted aspartic acid derivatives in which the nucleophilic catalyst serves up to four discrete roles in a one-pot procedure:  catalytic dehydrohalogenation of acid chlorides to form ketenes; catalytic dehydrohalogenation of α-chloroamines to form the corresponding imines; catalyzed [2 + 2]-cycloaddition to produce intermediate acyl β-lactams; and finally, nucleophilic ring opening to afford optically enriched β-substituted aspartic acids in high enantioselectivity and diastereoselectivity.

Published
2002

2. Insecticidal quinoline and isoquinoline isoxazolines.

Author

Xu M, Wagerle T, Long JK, Lahm GP, Barry JD, and Smith RM

Subjects
Animals, Dose-Response Relationship, Drug, Insecticides chemical synthesis, Insecticides chemistry, Isoquinolines chemistry, Isoxazoles chemical synthesis, Isoxazoles chemistry, Molecular Structure, Quinolines chemistry, Hemiptera drug effects, Insecticides pharmacology, Isoxazoles pharmacology, Moths drug effects, Thysanoptera drug effects
Abstract

A series of quinoline and isoquinoline isoxazolines have been designed as pesticides for crop protection. Herein we reported the chemical synthesis, biological activity and structure-activity relationships. The isoquinoline derivative, such as 3i, is discovered as potent new class of isoxazoline insecticide which is competitive with commercial insecticide Indoxacarb., (Copyright © 2014 Elsevier Ltd. All rights reserved.)

Published
2014
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3. Discovery and mode of action of afoxolaner, a new isoxazoline parasiticide for dogs.

Author

Shoop WL, Hartline EJ, Gould BR, Waddell ME, McDowell RG, Kinney JB, Lahm GP, Long JK, Xu M, Wagerle T, Jones GS, Dietrich RF, Cordova D, Schroeder ME, Rhoades DF, Benner EA, and Confalone PN

Subjects
Animals, Antiparasitic Agents blood, Antiparasitic Agents pharmacokinetics, Antiparasitic Agents therapeutic use, Cockroaches drug effects, Dog Diseases drug therapy, Dog Diseases physiopathology, Dogs, Drosophila melanogaster drug effects, Electrophysiological Phenomena drug effects, Female, Flea Infestations drug therapy, Flea Infestations prevention & control, Flea Infestations veterinary, Isoxazoles blood, Isoxazoles pharmacokinetics, Isoxazoles therapeutic use, Male, Naphthalenes blood, Naphthalenes pharmacokinetics, Naphthalenes therapeutic use, Oocytes drug effects, Protein Binding drug effects, Random Allocation, Tick Infestations drug therapy, Tick Infestations prevention & control, Tick Infestations veterinary, Xenopus laevis, Antiparasitic Agents pharmacology, Chloride Channels metabolism, Isoxazoles pharmacology, Naphthalenes pharmacology, Siphonaptera drug effects, Ticks drug effects
Abstract

Afoxolaner is an isoxazoline compound characterized by a good safety profile and extended effectiveness against fleas and ticks on dogs following a single oral administration. In vitro membrane feeding assay data and in vivo pharmacokinetic studies in dogs established an afoxolaner blood concentration of 0.1-0.2 μg/ml to be effective against both fleas (Ctenocephalides felis) and ticks (Dermacentor variabilis). Pharmacokinetic profiles in dogs following a 2.5mg/kg oral dosage demonstrated uniform and predictable afoxolaner plasma concentrations above threshold levels required for efficacy for more than one month. Dose ranging and a 5-month multi-dose experimental study in dogs, established that the 2.5mg/kg oral dosage was highly effective against fleas and ticks, and produced predictable and reproducible pharmacokinetics following repeated dosing. Mode of action studies showed that afoxolaner blocked native and expressed insect GABA-gated chloride channels with nanomolar potency. Afoxolaner has comparable potency between wild type channels and channels possessing the A302S (resistance-to-dieldrin) mutation. Lack of cyclodiene cross-resistance for afoxolaner was confirmed in comparative Drosophila toxicity studies, and it is concluded that afoxolaner blocked GABA-gated chloride channels via a site distinct from the cyclodienes., (Copyright © 2014 The Authors. Published by Elsevier B.V. All rights reserved.)

Published
2014
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4. 4-Azolylphenyl isoxazoline insecticides acting at the GABA gated chloride channel.

Author

Lahm GP, Cordova D, Barry JD, Pahutski TF, Smith BK, Long JK, Benner EA, Holyoke CW, Joraski K, Xu M, Schroeder ME, Wagerle T, Mahaffey MJ, Smith RM, and Tong MH

Subjects
Animals, Chloride Channels metabolism, Dose-Response Relationship, Drug, Insecta, Insecticides chemical synthesis, Insecticides chemistry, Isoxazoles chemical synthesis, Isoxazoles chemistry, Molecular Structure, Structure-Activity Relationship, Chloride Channels antagonists & inhibitors, Insecticides pharmacology, Isoxazoles pharmacology, Receptors, GABA metabolism
Abstract

Isoxazoline insecticides have been shown to be potent blockers of insect GABA receptors with excellent activity on a broad pest range, including Lepidoptera and Hemiptera. Herein we report on the synthesis, biological activity and mode-of-action for a class of 4-heterocyclic aryl isoxazoline insecticides., (Copyright © 2013 Elsevier Ltd. All rights reserved.)

Published
2013
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