التفاصيل البيبلوغرافية
| العنوان: |
Discovery of 4,6‐bis(2‐((E)‐benzylidene)hydrazinyl)pyrimidin‐2‐Amine with Antibiotic Activity |
| المؤلفون: |
Dr. Cecilia C. Russell, Dr. Andrew Stevens, Kelly A. Young, Jennifer R. Baker, Siobhann N. McCluskey, Dr. Manouchehr Khazandi, Hongfei Pi, Dr. Abiodun Ogunniyi, Dr. Stephen W. Page, Prof. Darren J. Trott, Prof. Adam McCluskey |
| المصدر: |
ChemistryOpen, Vol 8, Iss 7, Pp 896-907 (2019) |
| بيانات النشر: |
Wiley-VCH, 2019. |
| سنة النشر: |
2019 |
| المجموعة: |
LCC:Chemistry |
| مصطلحات موضوعية: |
Aminopyrimidines, antibacterial activity, robenidine, drugs discovery, Chemistry, QD1-999 |
| الوصف: |
Abstract Robenidine (E)‐N′‐((E)‐1‐(4‐chlorophenyl)ethylidene)‐2‐(1‐(4‐chlorophenyl)ethylidene)hydrazine‐1‐carboximidhydrazide displays methicillin‐resistant Staphyoccoccus aureus (MRSA) and vancomycin‐resistant Enterococci (VRE) MICs of 2 μg mL−1. Herein we describe the structure‐activity relationship development of a novel series of guanidine to 2‐aminopyrimidine isosteres that ameliorate the low levels of mammalian cytotoxicity in the lead compound while retaining good antibiotic activity. Removal of the 2‐NH2 pyrimidine moiety renders these analogues inactive. Introduction of a central 2‐NH2 triazine moiety saw a 10‐fold activity reduction. Phenyl to cyclohexyl isosteres were inactive. The 4‐BrPh and 4‐CH3Ph with MIC values of 2 and 4 μg mL−1, against MRSA and VRE respectively, are promising candidates for future development. |
| نوع الوثيقة: |
article |
| وصف الملف: |
electronic resource |
| اللغة: |
English |
| تدمد: |
2191-1363 |
| Relation: |
https://doaj.org/toc/2191-1363 |
| DOI: |
10.1002/open.201800241 |
| URL الوصول: |
https://doaj.org/article/f15d4513c76b48c9946eb2ad916f65ad |
| رقم الانضمام: |
edsdoj.f15d4513c76b48c9946eb2ad916f65ad |
| قاعدة البيانات: |
Directory of Open Access Journals |
Full Text Finder