N-isopropyl-(4-methoxy-3-difluoromethyl)cinnamoyl amide targets mycobacterial MmpL3

التفاصيل البيبلوغرافية
العنوان:	N-isopropyl-(4-methoxy-3-difluoromethyl)cinnamoyl amide targets mycobacterial MmpL3
المؤلفون:	Mario D. Martínez, Liliana Rondón, Lisandro Ronconi, Mariano Prado Acosta, Agostina Crotta Asis, Gabriela Gago, Florencia Di Salvo, Gerardo Burton, Fernando Durán, Mariana Piuri
المصدر:	European Journal of Medicinal Chemistry Reports, Vol 12, Iss , Pp 100188- (2024)
بيانات النشر:	Elsevier, 2024.
سنة النشر:	2024
المجموعة:	LCC:Pharmacy and materia medica LCC:Other systems of medicine
مصطلحات موضوعية:	Mycobacteria, MmpL3, Difluoromethylcinnamoyl amides, Pharmacy and materia medica, RS1-441, Other systems of medicine, RZ201-999
الوصف:	Mycobacterial infections still need new and more efficient drugs. In the present work we developed a new and simpler protocol for the synthesis of N-isopropyl-(4-methoxy-3-difluoromethyl)cinnamoyl amide, here named as 3M99F1, a promising candidate for mycobacterial growth inhibition. Using whole genome sequencing of 3M99F1 resistant strains we were able to identify Mycobacterial membrane protein Large 3 (MmpL3) as the target for this compound. MmpL3 inhibition by 3M99F1 was further confirmed by lipid analysis of Mycobacteria in the presence and absence of the drug. MmpL3 is well conserved in Mycobacteria, including atypical or NTM (non-tuberculous mycobacteria) and other Actinobacteria, but it is not present in humans, encouraging the development of new inhibitors using 3M99F1 as scaffold.
نوع الوثيقة:	article
وصف الملف:	electronic resource
اللغة:	English
تدمد:	2772-4174
Relation:	http://www.sciencedirect.com/science/article/pii/S2772417424000608; https://doaj.org/toc/2772-4174
DOI:	10.1016/j.ejmcr.2024.100188
URL الوصول:	https://doaj.org/article/9faf70d0f10c45b0b8cebca4309a75c5
رقم الانضمام:	edsdoj.9faf70d0f10c45b0b8cebca4309a75c5
قاعدة البيانات:	Directory of Open Access Journals

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الوصف
تدمد:	27724174
DOI:	10.1016/j.ejmcr.2024.100188