探索磺胺类药物的二茂铁衍生物作为潜在的抗疟疾和抗结核分枝杆菌药物

IF 2.7 3区化学 Q2 CHEMISTRY, INORGANIC & NUCLEAR

Inorganica Chimica Acta Pub Date : 2025-04-16 DOI:10.1016/j.ica.2025.122725

Katleho Setlaba , Vuyo Mavumengwana , Lucinda Baatjies , Malcolm T. Ndlovu , Catherine H. Kaschula , Prinessa Chellan

{"title":"探索磺胺类药物的二茂铁衍生物作为潜在的抗疟疾和抗结核分枝杆菌药物","authors":"Katleho Setlaba , Vuyo Mavumengwana , Lucinda Baatjies , Malcolm T. Ndlovu , Catherine H. Kaschula , Prinessa Chellan","doi":"10.1016/j.ica.2025.122725","DOIUrl":null,"url":null,"abstract":"<div><div>A series of new ferrocenyl sulfonamide derivatives (C1-C5) were synthesized from ferrocene carboxylic acid. The complexes were evaluated for their in vitro antimicrobial activities against Plasmodium falciparum and Mycobacterium tuberculosis H37Rv strains. They demonstrated moderate activities against the chloroquine-sensitive (NF54) strain of Plasmodium falciparum, with complex C2 being the most active, displaying an IC50 value of 3.715 μM. Furthermore, the complexes were non-cytotoxic towards the human embryonic kidney and normal prostate cells, indicating their selectivity towards parasitic cells. The complexes also exhibited moderate activity against Mycobacterium smegmatis mc2155, with an increase in activity observed against the Mycobacterium tuberculosis H37Rv strain. Among the complexes, C3 was the most active, displaying a MIC range of 31.73–15.86 μM. Moreover, all the complexes showed 10-fold greater potency than Isoniazid.</div></div>","PeriodicalId":13599,"journal":{"name":"Inorganica Chimica Acta","volume":"584 ","pages":"Article 122725"},"PeriodicalIF":2.7000,"publicationDate":"2025-04-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Exploring ferrocenyl derivatives of sulfa-drugs as potential antimalarial and anti-Mycobacterium tuberculosis agents\",\"authors\":\"Katleho Setlaba , Vuyo Mavumengwana , Lucinda Baatjies , Malcolm T. Ndlovu , Catherine H. Kaschula , Prinessa Chellan\",\"doi\":\"10.1016/j.ica.2025.122725\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><div>A series of new ferrocenyl sulfonamide derivatives (C1-C5) were synthesized from ferrocene carboxylic acid. The complexes were evaluated for their in vitro antimicrobial activities against Plasmodium falciparum and Mycobacterium tuberculosis H37Rv strains. They demonstrated moderate activities against the chloroquine-sensitive (NF54) strain of Plasmodium falciparum, with complex C2 being the most active, displaying an IC50 value of 3.715 μM. Furthermore, the complexes were non-cytotoxic towards the human embryonic kidney and normal prostate cells, indicating their selectivity towards parasitic cells. The complexes also exhibited moderate activity against Mycobacterium smegmatis mc2155, with an increase in activity observed against the Mycobacterium tuberculosis H37Rv strain. Among the complexes, C3 was the most active, displaying a MIC range of 31.73–15.86 μM. Moreover, all the complexes showed 10-fold greater potency than Isoniazid.</div></div>\",\"PeriodicalId\":13599,\"journal\":{\"name\":\"Inorganica Chimica Acta\",\"volume\":\"584 \",\"pages\":\"Article 122725\"},\"PeriodicalIF\":2.7000,\"publicationDate\":\"2025-04-16\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Inorganica Chimica Acta\",\"FirstCategoryId\":\"92\",\"ListUrlMain\":\"https://www.sciencedirect.com/science/article/pii/S0020169325001914\",\"RegionNum\":3,\"RegionCategory\":\"化学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q2\",\"JCRName\":\"CHEMISTRY, INORGANIC & NUCLEAR\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Inorganica Chimica Acta","FirstCategoryId":"92","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S0020169325001914","RegionNum":3,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"CHEMISTRY, INORGANIC & NUCLEAR","Score":null,"Total":0}

引用次数: 0

摘要

以二茂铁羧酸为原料合成了一系列新的二茂铁基磺酰胺衍生物（C1-C5）。研究了该配合物对恶性疟原虫和结核分枝杆菌H37Rv的体外抑菌活性。对氯喹敏感型（NF54）恶性疟原虫具有中等抑菌活性，其中复合物C2活性最强，IC50值为3.715 μM。此外，该复合物对人胚胎肾和正常前列腺细胞无细胞毒性，表明其对寄生细胞有选择性。这些复合物对耻垢分枝杆菌mc2155也表现出中等的活性，对结核分枝杆菌H37Rv菌株的活性增加。其中C3活性最强，MIC范围为31.73 ~ 15.86 μM。此外，所有配合物的效价都比异烟肼高10倍。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

Exploring ferrocenyl derivatives of sulfa-drugs as potential antimalarial and anti-Mycobacterium tuberculosis agents

查看原文本刊更多论文

Exploring ferrocenyl derivatives of sulfa-drugs as potential antimalarial and anti-Mycobacterium tuberculosis agents

A series of new ferrocenyl sulfonamide derivatives (C1-C5) were synthesized from ferrocene carboxylic acid. The complexes were evaluated for their in vitro antimicrobial activities against Plasmodium falciparum and Mycobacterium tuberculosis H37Rv strains. They demonstrated moderate activities against the chloroquine-sensitive (NF54) strain of Plasmodium falciparum, with complex C2 being the most active, displaying an IC₅₀ value of 3.715 μM. Furthermore, the complexes were non-cytotoxic towards the human embryonic kidney and normal prostate cells, indicating their selectivity towards parasitic cells. The complexes also exhibited moderate activity against Mycobacterium smegmatis mc²155, with an increase in activity observed against the Mycobacterium tuberculosis H37Rv strain. Among the complexes, C3 was the most active, displaying a MIC range of 31.73–15.86 μM. Moreover, all the complexes showed 10-fold greater potency than Isoniazid.

求助全文

通过发布文献求助，成功后即可免费获取论文全文。去求助

来源期刊

Inorganica Chimica Acta 化学-无机化学与核化学

CiteScore

6.00

自引率

3.60%

发文量

440

审稿时长

35 days

期刊介绍： Inorganica Chimica Acta is an established international forum for all aspects of advanced Inorganic Chemistry. Original papers of high scientific level and interest are published in the form of Articles and Reviews. Topics covered include: • chemistry of the main group elements and the d- and f-block metals, including the synthesis, characterization and reactivity of coordination, organometallic, biomimetic, supramolecular coordination compounds, including associated computational studies; • synthesis, physico-chemical properties, applications of molecule-based nano-scaled clusters and nanomaterials designed using the principles of coordination chemistry, as well as coordination polymers (CPs), metal-organic frameworks (MOFs), metal-organic polyhedra (MPOs); • reaction mechanisms and physico-chemical investigations computational studies of metalloenzymes and their models; • applications of inorganic compounds, metallodrugs and molecule-based materials. Papers composed primarily of structural reports will typically not be considered for publication.