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Updated: Jul 1, 2025

Development of a Backbone Cyclic Peptide Library as Potential Antiparasitic Therapeutics Using Microwave Irradiation
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Development of a Backbone Cyclic Peptide Library as Potential Antiparasitic Therapeutics Using Microwave Irradiation

Published on: January 26, 2016

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合成,结构-活性关系研究,生物活性和毒性评估周期性脂质皮Brevicidine B的拟议结构

Dennise Palpal-Latoc1,2,3, Aimee J Horsfall1,2,3, Alan J Cameron1,2,3

  • 1School of Chemical Sciences, The University of Auckland, 23 Symonds Street, Auckland 1010, New Zealand.

Journal of natural products
|February 29, 2024
PubMed
概括

研究人员合成了一种新型抗微生物 - - 布雷维丁B,发现它对阴性细菌有效,但对阳性菌株不有效. 在位置2的修改可能会降低脏毒性.

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Construction of Cyclic Cell-Penetrating Peptides for Enhanced Penetration of Biological Barriers

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Drug design is a dynamic field that involves discovering and developing new medications based on specific biological targets. This process heavily relies on structure-activity relationships (SAR) and quantitative structure-activity relationships (QSAR) to guide the design and optimization of efficient drugs.
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Adrenergic Agonists: Chemistry and Structure-Activity Relationship

Adrenergic agonists' structure-activity relationship (SAR) determines their selectivity and efficacy. These agonists comprise a phenylethylamine moiety with an aromatic ring and an ethylamine side chain.
Aromatic ring substitutions: Substituting the aromatic ring with –OH groups at positions 3 and 4 yields catecholamines (e.g., epinephrine), which have a high affinity for adrenoceptors. Hydrogen bonding between –OH groups and receptors enhances adrenergic activity.
Separation of...
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Pharmaceutical substances known as xenobiotics are predominantly lipophilic and nonionized. This enables them to permeate lipid bilayers, such as cell membranes, and interact with intracellular target receptors. Lipophilic drugs have an advantage in crossing biological barriers and reaching their intended sites of action. However, lipophilic drugs often have a restricted capacity for renal expulsion or elimination from the body. When these drugs enter the kidneys and undergo glomerular...
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