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Development of non-sedating benzodiazepines with antischistosomal activity.
Antimicrob Agents Chemother
September 2024
Department of Cell Biology, Neurobiology and Anatomy, Medical College of Wisconsin, Milwaukee, Wisconsin, USA.
The neglected tropical disease schistosomiasis infects over 200 million people worldwide and is treated with just one broad-spectrum antiparasitic drug (praziquantel). Alternative drugs are needed in the event of emerging praziquantel resistance or treatment failure. One promising lead that has shown efficacy in animal models and a human clinical trial is the benzodiazepine meclonazepam, discovered by Roche in the 1970s.
View Article and Find Full Text PDFTarget-based discovery of a broad-spectrum flukicide.
Nat Struct Mol Biol
September 2024
Department of Cell Biology, Neurobiology, and Anatomy, Medical College of Wisconsin, Milwaukee, WI, USA.
Diseases caused by parasitic flatworms impart a considerable healthcare burden worldwide. Many of these diseases-for example, the parasitic blood fluke infection schistosomiasis-are treated with the drug praziquantel (PZQ). However, PZQ is ineffective against disease caused by liver flukes from the genus Fasciola because of a single amino acid change within the target of PZQ, a transient receptor potential ion channel in the melastatin family (TRPM), in Fasciola species.
View Article and Find Full Text PDFDevelopment of non-sedating antischistosomal benzodiazepines.
bioRxiv
January 2024
Department of Cell Biology, Neurobiology & Anatomy, Medical College of Wisconsin, Milwaukee, WI, United States of America.
Article Synopsis
- - Schistosomiasis, a neglected tropical disease affecting over 200 million people, is primarily treated with praziquantel, but there's a need for alternative treatments due to potential resistance.
- - Researchers explored modifying the benzodiazepine meclonazepam, which had shown promise in treating this disease but was sidelined due to sedative side effects.
- - They synthesized 18 meclonazepam derivatives, identifying two compounds effective against the parasite with less sedation compared to meclonazepam, indicating a pathway to create better antiparasitic drugs.
Development and validation of an LC-MS/MS method for the simultaneous quantification of milbemycin oxime and praziquantel in plasma: application to a pharmacokinetic study in cats.
Front Vet Sci
October 2023
Guangdong Provincial Key Laboratory of Veterinary Pharmaceutics Development and Safety Evaluation, College of Veterinary Medicine, South China Agricultural University, Guangzhou, China.
Introduction: Milbemycin oxime (MBO) and praziquantel (PZQ) have a broad spectrum of biological activity and are commonly used to treat the parasitic infection in the veterinary clinic. In this study, a fast and efficient LC-MS/MS method was established and validated for the simultaneous determination of MBO, PZQ, cis-4-hydroxylated-PZQ (C-4-OH-PZQ) and trans-4-hydroxylated-PZQ (T-4-OH-PZQ) and in cat plasma.
Methods: Extraction of analytes and internal standards from cat plasma by acetonitrile protein precipitation, allows rapid processing of large batches of samples.
Simultaneous determination of praziquantel, fipronil, eprinomectin, (S)-methoprene, their key related substances and butylated hydroxytoluene (BHT) in a topical veterinary drug product by a single stability indicating high performance liquid chromatography method.
J Pharm Biomed Anal
January 2024
Global Pharmaceutical Technical Support (GPTS), Boehringer Ingelheim Animal Health USA Inc., 631 Route 1 South, North Brunswick, NJ 08902, USA.
A simple, robust and QC (quality control) friendly high performance liquid chromatography (HPLC) method was developed and validated for simultaneous determination of four active pharmaceutical ingredient [namely fipronil, (S)-methoprene, eprinomectin, and praziquantel] and their key degradation products in a broad-spectrum topical finished product. Typical sample of the finished product contains a total of 30-plus peaks of interest. Analytes were separated on a HALO C18 column (150 mm × 4.
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