Enhanced Anti-Bacterial Activity of Non-Antibacterial Drug Candesartan Cilexetil by Delivery through Polymeric Micelles was written by Kareem, Faheem;Abdul-Karim, Rubina;Maharjan, Rukesh;Shah, Muhammad Raza;Simjee, Shabana U.;Khan, Khalid M.;Malik, Muhammad Imran. And the article was included in ChemistrySelect in 2020.Electric Literature of C33H34N6O6 This article mentions the following:
Candesartan Cilexetil (CC) is a prodrug of candesartan and an angiotensin II receptor antagonist. It is used as a drug for different diseases like myocardial infarction, hypertension, and heart failure. The applicability of CC is impeded due to its poor water solubility, low permeability, and low bioavailability. This study is targeted to improve the efficacy and bioavailability of CC by its delivery through MeO-PEO5K-PCL micelles. The effect of length of hydrophobic block (PCL) on size of the micelles, drug encapsulation efficiency, and drug release behavior is evaluated. MeO-PEO5K-PCL based micelles were prepared by solvent evaporation method. The size of PMs was determined by dynamic light scattering, morphol. by at. force microscopy, and critical micelles concentration by fluorescence method. Encapsulation efficiency and drug release behaviors of MeO-PEO5K-PCL based PMs were evaluated by UV-visible spectroscopy and dispersion method, resp. The size of micelles increased and drug release rate decreased with increase in the length of PCL block. Maximum encapsulation efficiency of 96.42% for CC is achieved with ABCs having equal PEO and PCL block lengths. A comparison of antibacterial activity of CC in pure form and encapsulated in PMs against MRSA is conducted. The MIC50 for CC loaded PMs has decreased to more than half in comparison to pure drug. AFM based morphol. anal. also confirmed the decrease in MIC50 by delivery through PMs. In the experiment, the researchers used many compounds, for example, 1-(((Cyclohexyloxy)carbonyl)oxy)ethyl 1-((2′-(2H-tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylate (cas: 145040-37-5Electric Literature of C33H34N6O6).
1-(((Cyclohexyloxy)carbonyl)oxy)ethyl 1-((2′-(2H-tetrazol-5-yl)-[1,1′-biphenyl]-4-yl)methyl)-2-ethoxy-1H-benzo[d]imidazole-7-carboxylate (cas: 145040-37-5) belongs to imidazole derivatives. Many natural products, especially alkaloids, contain the imidazole ring. These imidazoles share the 1,3-C3N2 ring but feature varied substituents. Imidazole has been usedin the lysis, wash and elution buffer for the purification of histidine tagged Sonic Hedgehog(shh-N) protein, in elution buffer in stepwise gradient for the purification of histidine tagged aldo keto reductases using nickel affinity chromatography, as a component of homogenization buffer for the purification of phagosomal compartments from dendritic cells.Electric Literature of C33H34N6O6
Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem