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Hydrophobic vancomycin derivatives with improved ADME properties: discovery of telavancin (TD-6424).
Author: AdamsStacy M, BazziniBettina, ChristensenBurton G, FathereePaul R, JudiceJ Kevin, KarrDane E, KrauseKevin M, LamBernice M T, LeadbetterMichael R, LinsellMartin S, NodwellMatthew B, PaceJohn L, QuastKelly, ShawJeng-Pyng, SorianoElizabeth, TrappSean G, VillenaJenny D, WuTerry X
Original Abstract of the Article :
Novel derivatives of N-decylaminoethylvancomycin (2), containing appended hydrophilic groups were synthesized and their antibacterial activity and ADME properties were evaluated. The compounds were prepared by reacting amines with the C-terminus (C-) of 2 using PyBOP mediated amide formation, or wit...See full text at original site
Dr.Camel's Paper Summary Blogラクダ博士について
ラクダ博士は、Health Journal が論文の内容を分かりやすく解説するために作成した架空のキャラクターです。
難解な医学論文を、専門知識のない方にも理解しやすいように、噛み砕いて説明することを目指しています。
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* 解説の内容は Health Journal が独自に解釈・作成したものであり、原論文の著者または出版社の見解を反映するものではありません。
引用元:
https://doi.org/10.7164/antibiotics.57.326
データ提供:米国国立医学図書館(NLM)
Improving Vancomycin: A Journey Through the Desert of Drug Discovery
The quest for new and effective antibiotics is a constant battle in the ever-evolving landscape of medicine. Vancomycin, a powerful antibiotic, has been a valuable weapon in the fight against bacterial infections, but its limitations, like a desert without water, have led to the emergence of resistant strains. This study, like a team of intrepid explorers, embarked on a journey to improve vancomycin's efficacy. They embarked on a journey through the vast desert of drug discovery, synthesizing and evaluating novel derivatives of N-decylaminoethylvancomycin (2). These derivatives, like oases in a barren landscape, displayed improved antibacterial activity and pharmacokinetic properties compared to the original compound. The authors, like skilled cartographers, mapped the structure-activity relationships, pinpointing modifications that enhanced the antibiotic's efficacy. Among the novel derivatives, compound 21, a phosphonomethylaminomethyl derivative, stood out as a promising candidate. Its favorable properties, like a well-stocked caravan, suggested its potential for clinical development. This study, like a beacon in the desert, highlights the importance of ongoing research in the pursuit of new and improved antibiotics.
A New Dawn in Antibiotic Development
The discovery of telavancin (TD-6424), a potent vancomycin derivative with improved pharmacokinetic properties, represents a significant advancement in the fight against antibiotic resistance. The authors' findings, like a fertile valley in a desolate desert, offer hope for a future where we can more effectively combat bacterial infections.
The Promise of Telavancin
Telavancin, with its enhanced efficacy and favorable pharmacokinetic profile, could prove to be a valuable asset in the fight against antibiotic resistance. The study's findings, like a guiding star in the desert, point towards a more promising future for treating bacterial infections.
Dr.Camel's Conclusion
This study, like a well-charted route, guides us towards a more effective and safe approach to treating bacterial infections. The discovery of telavancin, a potent vancomycin derivative, represents a significant milestone in the fight against antibiotic resistance. The authors' research, like a beacon in the desert, illuminates the path towards a future where we can effectively combat bacterial infections and protect human health.
Date :
- Date Completed 2004-09-03
- Date Revised 2019-07-23
Further Info :
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