Evidence map›Paper›PMID 39723690›Full record

ArticleFuture medicinal chemistry2025

Synthesis and antimicrobial activity evaluation of pyrazole derivatives containing imidazothiadiazole moiety.

Lan-Ying Han, Jing-Xin Sun, Chuang Liu, Bing Ai, Ming-Guan Piao, Changhao Zhang, Ji-Shan Quan, Cheng-Hua Jin

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Article in Future medicinal chemistry, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.

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1 · What the graph read from it

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2 · The registry

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3 · Its place in the literature

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4 · The record

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5 · Who and what money

Authors and funding

8 authors.

Lan-Ying HanKey Laboratory of Natural Medicines of the Changbai Mountain, Ministry of Education, College of Pharmacy, Yanbian University, Yanji, China.
Jing-Xin SunKey Laboratory of Natural Medicines of the Changbai Mountain, Ministry of Education, College of Pharmacy, Yanbian University, Yanji, China.
Chuang LiuKey Laboratory of Natural Medicines of the Changbai Mountain, Ministry of Education, College of Pharmacy, Yanbian University, Yanji, China.
Bing AiKey Laboratory of Natural Medicines of the Changbai Mountain, Ministry of Education, College of Pharmacy, Yanbian University, Yanji, China.
Ming-Guan PiaoKey Laboratory of Natural Medicines of the Changbai Mountain, Ministry of Education, College of Pharmacy, Yanbian University, Yanji, China.
Changhao ZhangKey Laboratory of Natural Medicines of the Changbai Mountain, Ministry of Education, College of Pharmacy, Yanbian University, Yanji, China.
Ji-Shan QuanKey Laboratory of Natural Medicines of the Changbai Mountain, Ministry of Education, College of Pharmacy, Yanbian University, Yanji, China.
Cheng-Hua JinKey Laboratory of Natural Medicines of the Changbai Mountain, Ministry of Education, College of Pharmacy, Yanbian University, Yanji, China.ORCID 0000-0001-5534-4845

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

aimThe purpose of this work was to investigate the antimicrobial activity of pyrazole derivatives (21a - i and 23a - o) synthesized. MATERIALS &

methodsThe pyrazole derivatives were synthesized, molecular docked and tested for their antimicrobial activity, cytotoxicity, and hemolysis rate.

resultsMost of the target compounds showed high selective inhibitory activity against multi-drug resistance compared with other strains. Of these, compounds 21c (MIC = 0.25 µg/mL) and 23 h (MIC = 0.25 µg/mL) showed the strongest antibacterial activity, which was 4-flods than that of the positive control compound gatifloxacin (MIC = 1 µg/mL). Furthermore, compound 23 h showed no cytotoxicity to human LO2 cells, and did not show hemolysis even at ultra-high concentration.

conclusionThese results prompted that these compounds are valuable for further development as antimicrobial agents.

Indexed as

Anti-Bacterial AgentsAntifungal AgentsPyrazolesThiadiazolesBacteriaCell LineHemolysisHumansImidazolesMicrobial Sensitivity TestsMolecular Docking SimulationMolecular StructureStructure-Activity RelationshipAnti-Bacterial AgentsAntifungal AgentsImidazolesimidazothiadiazolePyrazolesThiadiazolesantimicrobial activityhemolysisimidazo[2,1-b][1,3,4]thiadiazolemulti-drug resistancePyrazole

Identifiers

PMID39723690
PMCPMC11749441

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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.