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

Paper Details 
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
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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 :
  1. Date Completed 2004-09-03
  2. Date Revised 2019-07-23
Further Info :

Pubmed ID

15303493

DOI: Digital Object Identifier

10.7164/antibiotics.57.326

Related Literature

SNS
PICO Info
in preparation
Languages

English

Positive IndicatorAn AI analysis index that serves as a benchmark for how positive the results of the study are. Note that it is a benchmark and requires careful interpretation and consideration of different perspectives.

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