{"title":"新型噻唑腙衍生物的发现作为治疗人畜共患犬弓形虫的替代选择:体外和计算机评价。","authors":"Mustafa Eser, Derya Osmaniye","doi":"10.1002/vms3.70144","DOIUrl":null,"url":null,"abstract":"<p><p>Thiazoles serve as pharmacophores in many molecules that exhibit significant biological activity. This study used in vitro assays and in silico methodologies to identify novel medication candidates for preclinical evaluation of visceral toxocariasis treatment. The objective was to assess the impact of 11 thiazolohydrazone derivative compounds on the larval eggs of Toxocara canis. In addition, the inhibitory effects of these compounds on IL-6 levels in THP-1 cells stimulated with larval eggs have been examined. Compounds indicating the most significant inhibitory effect on IL-6 and a suppressive effect on larval eggs have been included in molecular dynamics studies. The study revealed that, when evaluating all thiazolohydrazone derivatives together, Compounds 3g and 3h possessed the highest antiparasitic efficiency, encouraging further molecular dynamics investigations on these compounds. Consequently, it can be theorised that if the results from this study are corroborated by in vivo studies, new anti-nematodal medication candidates may be identified.</p>","PeriodicalId":23543,"journal":{"name":"Veterinary Medicine and Science","volume":"11 1","pages":"e70144"},"PeriodicalIF":1.8000,"publicationDate":"2025-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11706067/pdf/","citationCount":"0","resultStr":"{\"title\":\"Discovery of Novel Thiazolohydrazone Derivatives as an Alternative Option in the Treatment of Zoonotic Toxocara canis: In Vitro and In Silico Evaluation.\",\"authors\":\"Mustafa Eser, Derya Osmaniye\",\"doi\":\"10.1002/vms3.70144\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>Thiazoles serve as pharmacophores in many molecules that exhibit significant biological activity. This study used in vitro assays and in silico methodologies to identify novel medication candidates for preclinical evaluation of visceral toxocariasis treatment. The objective was to assess the impact of 11 thiazolohydrazone derivative compounds on the larval eggs of Toxocara canis. In addition, the inhibitory effects of these compounds on IL-6 levels in THP-1 cells stimulated with larval eggs have been examined. Compounds indicating the most significant inhibitory effect on IL-6 and a suppressive effect on larval eggs have been included in molecular dynamics studies. The study revealed that, when evaluating all thiazolohydrazone derivatives together, Compounds 3g and 3h possessed the highest antiparasitic efficiency, encouraging further molecular dynamics investigations on these compounds. Consequently, it can be theorised that if the results from this study are corroborated by in vivo studies, new anti-nematodal medication candidates may be identified.</p>\",\"PeriodicalId\":23543,\"journal\":{\"name\":\"Veterinary Medicine and Science\",\"volume\":\"11 1\",\"pages\":\"e70144\"},\"PeriodicalIF\":1.8000,\"publicationDate\":\"2025-01-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11706067/pdf/\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Veterinary Medicine and Science\",\"FirstCategoryId\":\"97\",\"ListUrlMain\":\"https://doi.org/10.1002/vms3.70144\",\"RegionNum\":3,\"RegionCategory\":\"农林科学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q2\",\"JCRName\":\"VETERINARY SCIENCES\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Veterinary Medicine and Science","FirstCategoryId":"97","ListUrlMain":"https://doi.org/10.1002/vms3.70144","RegionNum":3,"RegionCategory":"农林科学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"VETERINARY SCIENCES","Score":null,"Total":0}
Discovery of Novel Thiazolohydrazone Derivatives as an Alternative Option in the Treatment of Zoonotic Toxocara canis: In Vitro and In Silico Evaluation.
Thiazoles serve as pharmacophores in many molecules that exhibit significant biological activity. This study used in vitro assays and in silico methodologies to identify novel medication candidates for preclinical evaluation of visceral toxocariasis treatment. The objective was to assess the impact of 11 thiazolohydrazone derivative compounds on the larval eggs of Toxocara canis. In addition, the inhibitory effects of these compounds on IL-6 levels in THP-1 cells stimulated with larval eggs have been examined. Compounds indicating the most significant inhibitory effect on IL-6 and a suppressive effect on larval eggs have been included in molecular dynamics studies. The study revealed that, when evaluating all thiazolohydrazone derivatives together, Compounds 3g and 3h possessed the highest antiparasitic efficiency, encouraging further molecular dynamics investigations on these compounds. Consequently, it can be theorised that if the results from this study are corroborated by in vivo studies, new anti-nematodal medication candidates may be identified.
期刊介绍:
Veterinary Medicine and Science is the peer-reviewed journal for rapid dissemination of research in all areas of veterinary medicine and science. The journal aims to serve the research community by providing a vehicle for authors wishing to publish interesting and high quality work in both fundamental and clinical veterinary medicine and science.
Veterinary Medicine and Science publishes original research articles, systematic reviews, meta-analyses, and research methods papers, along with invited editorials and commentaries. Original research papers must report well-conducted research with conclusions supported by the data presented in the paper.
We aim to be a truly global forum for high-quality research in veterinary medicine and science, and believe that the best research should be published and made widely accessible as quickly as possible. Veterinary Medicine and Science publishes papers submitted directly to the journal and those referred from a select group of prestigious journals published by Wiley-Blackwell.
Veterinary Medicine and Science is a Wiley Open Access journal, one of a new series of peer-reviewed titles publishing quality research with speed and efficiency. For further information visit the Wiley Open Access website.