ArticleAngewandte Chemie (International ed. in English)2026
Thiophene-Engineered Lipid II Recognition Enables Potent Membranolytic Eradication of MRSA.
Aniket Jana, Moumita Jash, Samya Sen, Dipro Mukherjee, Surojit Ghosh, Sandip Sarkar, Satyajit Ghosh, Rajsekhar Roy, Monika Singh, Subhadra Nandi and 4 more
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In one paragraphArticle in Angewandte Chemie (International ed. in English), 2026. 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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Aniket JanaSmart Healthcare, Interdisciplinary Research Division, Indian Institute of Technology, Jodhpur, Karwar, Rajasthan, India.ORCID 0000-0002-4379-8417 Moumita JashDepartment of Bioscience and Bioengineering, Indian Institute of Technology, Jodhpur, Karwar, Rajasthan, India.ORCID 0000-0001-6986-7866 Samya SenDepartment of Bioscience and Bioengineering, Indian Institute of Technology, Jodhpur, Karwar, Rajasthan, India.ORCID 0000-0002-3209-1774 Dipro MukherjeeDepartment of Bioscience and Bioengineering, Indian Institute of Technology, Jodhpur, Karwar, Rajasthan, India.
Surojit GhoshSmart Healthcare, Interdisciplinary Research Division, Indian Institute of Technology, Jodhpur, Karwar, Rajasthan, India.
Sandip SarkarDepartment of Chemical Sciences and Center for Advanced Functional Materials, Indian Institute of Science Education and Research (IISER) Kolkata, Nadia, West Bengal, India.
Satyajit GhoshDepartment of Bioscience and Bioengineering, Indian Institute of Technology, Jodhpur, Karwar, Rajasthan, India.
Rajsekhar RoyDepartment of Bioscience and Bioengineering, Indian Institute of Technology, Jodhpur, Karwar, Rajasthan, India.
Monika SinghCentral Research Facility (CRF), Indian Institute of Technology, Jodhpur, Karwar, Rajasthan, India.
Subhadra NandiCentral Research Facility (CRF), Indian Institute of Technology, Jodhpur, Karwar, Rajasthan, India.ORCID 0000-0002-6975-6565 Priya RajdevSchool of Applied and Interdisciplinary Sciences, Indian Association for the Cultivation of Science (IACS), Kolkata, India.
Surajit GhoshSmart Healthcare, Interdisciplinary Research Division, Indian Institute of Technology, Jodhpur, Karwar, Rajasthan, India.ORCID 0000-0002-8203-8613 Jayita SarkarCentral Research Facility (CRF), Indian Institute of Technology, Jodhpur, Karwar, Rajasthan, India.ORCID 0009-0001-3634-429X Amitava DasDepartment of Chemical Sciences and Center for Advanced Functional Materials, Indian Institute of Science Education and Research (IISER) Kolkata, Nadia, West Bengal, India.ORCID 0000-0003-3666-1743 Funding
Science and Engineering Research Board (currently ANRF), DST, Govt. of India
6 · The paper itselfAbstract
Methicillin-resistant Staphylococcus aureus (MRSA) remains a significant global health threat, necessitating the development of new antimicrobials. We report the rational design of a small molecule TPL(II)-07, that combines multiple functional modules: (i) 2-phenylthiophene for specific recognition and binding to lipid II, a key intermediate in peptidoglycan biosynthesis; (ii) an adamantane fragment with high interfacial permeability to destabilize lipid packing; (iii) a cationic lysine moiety to disperse biofilms; and (iv) a moderate aliphatic chain to disrupt membrane integrity. Among seven analogues, TPL(II)-07 exhibited the highest potency, highlighting the synergistic contribution of each component. Mechanistic assays confirmed preferential binding of lipid II, bactericidal potency, biofilm dispersion, and the generation of reactive oxygen species, effective against both drug-resistant (MIC 19 µM) and drug-sensitive (MIC 9 µM) S. aureus strains. TPL(II)-07 demonstrated excellent biocompatibility, with IC
Indexed as
Anti-Bacterial AgentsMethicillin-Resistant Staphylococcus aureusThiophenesUridine Diphosphate N-Acetylmuramic AcidAnimalsBiofilmsHumansMicrobial Sensitivity TestsAnti-Bacterial Agentsmuramyl-NAc-(pentapeptide)pyrophosphoryl-undecaprenolThiophenesUridine Diphosphate N-Acetylmuramic Acid2‐Phenylthiophene hybridslipid II targetingmembrane depolarizationwound‐healing hydrogel
Identifiers
PMID42272170
PMCPMC13452510
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