- Pharmacokinetics and Biodistribution of GDC-0449 Loaded Micelles in Normal and Liver Fibrotic Mice
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Purposes: To determine the pharmacokinetic parameters and biodistribution of GDC-0449 loaded polymeric micelles after systemic administration into common bile duct ligation (CBDL) induced liver fibrotic mice. Methods: We used GDC-0449 encapsulated methoxy
- Dutta, Rinku,Kumar, Virender,Peng, Yang,Evande, Ruby E.,Grem, Jean L.,Mahato, Ram I.
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- Tagging alcohols with cyclic carbonate: A versatile equivalent of (meth)acrylate for ring-opening polymerization
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Cyclic carbonate monomers based on a single biocompatible scaffold allow for incorporation of a wide range of functional groups into macromolecules via ring-opening polymerization. The Royal Society of Chemistry.
- Pratt, Russell C.,Nederberg, Fredrik,Waymouth, Robert M.,Hedrick, James L.
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- Synthesis and liquid crystal behavior of new side chain aliphatic polycarbonates based on cholesterol
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In this study, we synthesized a series of new liquid crystal aliphatic block polycarbonates copolymers mPEG43-b-P(MCC-Cn)51 (n = 1–4) via the ring-opening polymerization, hydrogenation reduction and coupling reaction, which contained side functionalized cholesteryl groups and were different in the number of the flexible methylene groups. The chemical structures of the chiral compounds and copolymers obtained in this study were characterized by FT-IR and 1H NMR spectra, and the average molecular weights of the copolymers were investigated by average molecular weights gel permeation chromatographic (GPC). The polarizing optical microscopy (POM), differential scanning calorimetry (DSC) and X-ray diffraction (XRD) were used to characterize the liquid crystal behavior. The relationship of the structure and phase behavior of the chiral compounds and copolymers influenced by spacer lengths was discussed. As a result, the chiral compounds with two methylene only showed a smectic A (SmA) phase, while those with more methylene showed a SmA phase and cholesteric phase. As the number of the flexible methylene groups increased, the corresponding melting temperature, the transition temperatures of LC phases and the isotropic temperature of chiral compounds all showed a decreasing trend, and mesophase temperature range narrowed. The polycarbonate copolymer with two methylene did not show mesomorphism, while the copolymers with longer spacer length seemed beneficial for the formation of mesophases at room temperature and revealed a smectic A phase with an interdigitated molecular arrangement on heating and cooling cycles. The results showed a decreased tendency toward the glass temperature, and an increased tendency toward isotropic temperature for the LC copolymers with an increase of the spacer length.
- Liu, Xiaofeng,Guo, Zhihao,Xie, Yujiao,Chen, Zhangpei,Hu, Jianshe,Yang, Liqun
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- Self-assembling, amphiphilic polymer-gemcitabine conjugate shows enhanced antitumor efficacy against human pancreatic adenocarcinoma
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The therapeutic efficacy of gemcitabine is severely compromised due to its rapid plasma metabolism. Moreover, its hydrophilicity poses a challenge for its efficient entrapment in nanosized delivery systems and to provide a sustained release profile. In th
- Chitkara, Deepak,Mittal, Anupama,Behrman, Stephan W.,Kumar, Neeraj,Mahato, Ram I.
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- Enteric Polymer Based on pH-Responsive Aliphatic Polycarbonate Functionalized with Vitamin E To Facilitate Oral Delivery of Tacrolimus
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(Figure Presented) To improve the bioavailability of orally administered drugs, we synthesized a pH-sensitive polymer (poly(ethylene glycol)-poly(2-methyl-2-carboxyl-propylene carbonate)-vitamin E, mPEG-PCC-VE) attempting to integrate the advantages of enteric coating and P-glycoprotein (P-gp) inhibition. The aliphatic polycarbonate chain was functionalized with carboxyl groups and vitamin E via postpolymerization modification. Optimized by comparison and central composite design, mPEG113-PCC32-VE4 exhibited low critical micelle concentration of 1.7 × 10-6 mg/mL and high drug loading ability for tacrolimus (21.2% ± 2.7%, w/w). The pH-responsive profile was demonstrated by pH-dependent swelling and in vitro drug release. Less than 4.0% tacrolimus was released under simulated gastric fluid after 2.5 h, whereas an immediate release was observed under simulated intestinal fluid. The mPEG113-PCC32-VE4 micelles significantly increased the absorption of P-gp substrate tacrolimus in the whole intestine. The oral bioavailability of tacrolimus micelles was 6-fold higher than that of tacrolimus solution in rats. This enteric polymer therefore has the potential to become a useful nanoscale carrier for oral delivery of drugs.
- Wang, Menglin,Sun, Jin,Zhai, Yinglei,Lian, He,Luo, Cong,Li, Lin,Du, Yuqian,Zhang, Dong,Ding, Wenya,Qiu, Shuhong,Liu, Yuhai,Kou, Longfa,Han, Xiangfei,Xiang, Rongwu,Wang, Yongjun,He, Zhonggui
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- Degradation behavior of poly(lactide-co-carbonate)s controlled by chain sequences
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Immortal copolymerization of lactide (LA) and 2-methyl-2-benzyloxycarbonyl-1,3-trimethylene carbonate (MBC) affords random, tapered, and diblock microstructured poly(lactide-co-carbonate)s. Subsequent debenzylation of these poly(LA-co- MBC)s by Pd/C catalytic hydrogenation gives poly(LA-co-MCC)s containing carboxylic acid, which show controlled degradation performance during in vitro hydrolytic degradation experiments. The degradation rates of poly(LA-co-MCC)s are proved for the first time to be affected significantly by lactide-carbonate linkages in the main chains, following the trend of lactide-carbonate unit (L- C/C-L)>carbonate-carbonate unit (C-C)>lactide-lactide unit (L-L). The resultant hydrolysis products are the precursors for synthesizing the corresponding monomers. Therefore, the degradable and recyclable materials are accomplished.
- Liu, Xinli,Cui, Dongmei,Hua, Xiufang
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- Synthesis and characterization of hyperbranched poly(ε-caprolactone)s having different lengths of homologous backbone segments
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Hyperbranched poly(ε-caprolactone)s (HPCLs) were synthesized by moisture-sensitive catalyst-free polycondensation of AB2 macromonomers, 2,2-bis[ω-hydroxy oligo(ε-caprolactone)methyl]-propionic acids. The HPCLs were designed to incorporate diffe
- Choi, Jeongsoo,Kwak, Seung-Yeop
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- Polycarbonates with Potent and Selective Antimicrobial Activity toward Gram-Positive Bacteria
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The resistance developed by life-threatening bacteria toward conventional antibiotics has become a major concern in public health. To combat antibiotic resistance, there has been a significant interest in the development of antimicrobial cationic polymers
- Nimmagadda, Alekhya,Liu, Xuan,Teng, Peng,Su, Ma,Li, Yaqiong,Qiao, Qiao,Khadka, Nawal K.,Sun, Xiaoting,Pan, Jianjun,Xu, Hai,Li, Qi,Cai, Jianfeng
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- Cholesterol and Morpholine Grafted Cationic Amphiphilic Copolymers for miRNA-34a Delivery
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miR-34a is a master tumor suppressor playing a key role in the several signaling mechanisms involved in cancer. However, its delivery to the cancer cells is the bottleneck in its clinical translation. Herein we report cationic amphiphilic copolymers graft
- Sharma, Saurabh,Mazumdar, Samrat,Italiya, Kishan S.,Date, Tushar,Mahato, Ram I.,Mittal, Anupama,Chitkara, Deepak
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- EGFR-Targeted Polymeric Mixed Micelles Carrying Gemcitabine for Treating Pancreatic Cancer
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The objective of this study was to design GE11 peptide (YHWYGYTPQNVI) linked micelles of poly(ethylene glycol)-block-poly(2-methyl-2-carboxyl-propylene carbonate-graft-gemcitabine-graft-dodecanol (PEG-b-PCC-g-GEM-g-DC) for enhanced stability and target sp
- Mondal, Goutam,Kumar, Virender,Shukla, Surendra K.,Singh, Pankaj K.,Mahato, Ram I.
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- Lactic acid- and carbonate-based crosslinked polymeric micelles for drug delivery
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Our objective was to synthesize and evaluate lactic acid- and carbonate-based biodegradable core- and core-corona crosslinkable copolymers for anticancer drug delivery. Methoxy poly(ethylene glycol)-b-poly(carbonate-co- lactide-co-5-methyl-5-allyloxycarbo
- Danquah, Michael,Fujiwara, Tomoko,Mahato, Ram I.
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- Nanoparticulate delivery of potent microtubule inhibitor for metastatic melanoma treatment
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Melanoma is the most aggressive type of skin cancer, which readily metastasizes through lymph nodes to the lungs, liver, and brain. Since the repeated administration of most chemotherapeutic drugs develops chemoresistance and severe systemic toxicities, h
- Bariwal, Jitender,Kumar, Virender,Chen, Hao,Bhattarai, Rajan Sharma,Peng, Yang,Li, Wei,Mahato, Ram I.
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- Sensitization of LnIII (Ln = Eu, Tb, Tm) Ion Luminescence by Functionalized Polycarbonate-Based Materials and White Light Generation
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We prepared pyridine-2,6-bis(ethyl)ester [BEP] and pyridine-2,6-bis(diethylamide) [BDP] polymers with polycarbonate backbones by ring-opening polymerization of the pyridine-bis(ethyl)ester and pyridine-bis(diethylamide) units appended to a cyclic carbonat
- Tigaa, Rodney A.,Aerken, Xuekelaiti,Fuchs, Alan,de Bettencourt-Dias, Ana
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- Rapid, efficient synthesis of heterobifunctional biodegradable dendrimers
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A method for the preparation of heterobifunctional biodegradable dendrimers is described involving the preparation of a symmetric aliphatic ester dendrimer derived from 2,2-bis(hydroxymethyl)propanoic acid bearing a cyclic carbonate periphery, followed by
- Goodwin, Andrew P.,Lam, Stephanie S.,Frechet, Jean M. J.
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- EGFR-Targeted Cationic Polymeric Mixed Micelles for Codelivery of Gemcitabine and miR-205 for Treating Advanced Pancreatic Cancer
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Gemcitabine (GEM), a first-line chemotherapy for pancreatic cancer undergoes rapid metabolism and develops chemoresistance after repeated administration. We previously demonstrated that the combination of GEM and miR-205 provides an effective therapeutic strategy to sensitize GEM-resistant pancreatic cancer cells. Since epidermal growth factor receptor (EGFR) is overexpressed in pancreatic cancer cells, in this study, we aimed to deliver mixed micelles containing GEM and miR-205 decorated with EGFR-targeting cetuximab (C225) monoclonal antibody for targeted therapy. Cetuximab C225 was conjugated to malemido-poly(ethylene glycol)-block-poly(2-methyl-2-carboxyl-propylene carbonate-graft-dodecanol (C225-PEG-PCD) to prepare mixed micelles with mPEG-b-PCC-g-GEM-g-DC-g-TEPA for targeted codelivery of GEM and miR-205. This mixed micelle formulation showed a significant enhancement in EGFR-mediated cellular uptake in GEM-resistant MIA PaCa-2R cells. Further, an enhanced tumor accumulation of C225-micelles conjugated with near-infrared fluorescent Cy7.5 dye and Dy677-labeled miR-205 in orthotopic pancreatic tumor bearing NSG mice was evident after systemic administration. In addition, inhibition of tumor growth was also observed with increased apoptosis and reduced EMT after treatment with C225-micelles containing GEM and miR-205. Therefore, we believe that the targeted delivery of GEM and miR-205 in combination could be a novel strategy for treating advanced pancreatic cancer.
- Mondal, Goutam,Almawash, Saud,Chaudhary, Amit Kumar,Mahato, Ram I.
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- Architectural effects of poly(∈-caprolactone)s on the crystallization kinetics
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The architectural effects of poly(ε-caprolactone)s on the crystallization kinetics were examined. The nonisothermal crystallization exotherms of HPCLs and LPCL were measured by DSC and analysed by Avrami method. Steady shear melt viscosity measurements we
- Choi, Jeongsoo,Kwak, Seung-Yeop
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- Biodegradable broad-spectrum antimicrobial polycarbonates: Investigating the role of chemical structure on activity and selectivity
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A series of biodegradable polycarbonate polymers was designed and synthesized via organocatalytic ring-opening polymerization of functional cyclic carbonate monomer (MTC-OCH2BnCl). By adopting a facile postpolymerization functionalization strategy, the polycarbonates were quaternized to yield cationic polymers with quaternary ammonium groups of various pendant structures (e.g., alkyl, aromatic, imidazolinium). The biological properties of these polymers were investigated by microbial growth inhibition assays against clinically relevant Gram-positive and Gram-negative bacteria, fungus as well as hemolysis assays using rat red blood cells. A judicious choice in the structure of the cationic appendages elucidated that the amphiphilic balance of the polymers is a pertinent determinant to render substantial antimicrobial potency and low hemolysis, consequently affording the polymer pButyl-20 (degree of polymerization, 20; quaternary ammonium group, N,N-dimethylbutylammonium) as a highly efficacious and nonhemolytic antimicrobial agent with a remarkable selectivity of more than 1026. To ameliorate the selectivity against a wider spectrum of microbes including the difficult-to-kill Pseudomonas aeruginosa, it was shown that polymers containing N,N-dimethylbutylammonium and N,N-dimethylbenzylammonium groups in 1:1 molar ratio exerted considerable antimicrobial potency while remaining relatively nonhemolytic. Biophysical studies encompassing the determination of water-octanol partition coefficients (log P) and dye leakage studies from model liposomes provided useful insights which delineate the pivotal role of cationic group structure in the antimicrobial activity and mechanism of these polymers. Through field emission scanning electron microscopy (FE-SEM), a physical lysis of microbial cell membranes was deemed operative in the antimicrobial action of these macromolecular agents, which would consequently reduce the propensity toward resistance development. These polymers are envisaged to be promising antimicrobial agents for the prevention and treatment of multidrug-resistant pathogenic infections.
- Chin, Willy,Yang, Chuan,Ng, Victor Wee Lin,Huang, Yuan,Cheng, Junchi,Tong, Yen Wah,Coady, Daniel J.,Fan, Weimin,Hedrick, James L.,Yang, Yi Yan
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- Highly Stable, Coordinated Polymeric Nanoparticles Loading Copper(II) Diethyldithiocarbamate for Combinational Chemo/Chemodynamic Therapy of Cancer
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Disulfiram (DSF) has excellent in vitro anticancer activity in the presence of Cu(II). The anticancer mechanism studies have demonstrated that copper(II) diethyldithiocarbamate, Cu(DDC)2, is the crucial DSF's metabolite exhibiting anticancer ac
- Peng, Xinyu,Pan, Qingqing,Zhang, Boya,Wan, Shiyu,Li, Sai,Luo, Kui,Pu, Yuji,He, Bin
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- Construction of Janus dendrimers through a self-assembly approach involving chiral discrimination at a focal point
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A strategy to build Janus dendrimersviathe chirality-directed self-assembly of heteroleptic Zn(ii) BOX complexes is reported. The method allows quantitative synthesis of Janus dendrimersin situwithout the need for purifications. Each dendritic domain of t
- Cole, Ashley M.,Kilway, Kathleen V.,Menuey, Elizabeth M.,Moteki, Shin A.,Zhou, John
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supporting information
p. 6404 - 6407
(2021/07/02)
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- Synthesis of Heterofunctional Polyester Dendrimers with Internal and External Functionalities as Versatile Multipurpose Platforms
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Heterofunctional dendrimers with internal and external representations of functionalities are considered as the ultimate dendritic frameworks. This is reflected by their unprecedented scaffolding, such as precise control over the structure, molecular weig
- Garciá-Gallego, Sandra,Stenstr?m, Patrik,Mesa-Antunez, Pablo,Zhang, Yuning,Malkoch, Michael
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p. 4273 - 4279
(2020/11/09)
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- Selective monobenzylation of 2,2-bis(hydroxymethyl)propionic acid (bis-MPA) to yield an AB linear monomer and analogous linear oligomers
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The synthesis of a mono-benzylated AB monomer based on bis-MPA is explored and accomplished via a three-step synthesis without column chromatography. This optimized synthesis utilizes a generic acid-catalyzed esterification of bis-MPA to the ethyl ester.
- Giesen, Joseph A.,Grayson, Scott M.
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supporting information
(2020/05/28)
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- MITOGEN-ACTIVATED PROTEIN KINASE INHIBITORS, METHODS OF MAKING, AND METHODS OF USE THEREOF
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Compounds that inhibit mitogen-activated protein kinases (MAPKs) are disclosed. Some inhibitor compounds specifically target a single MAPK such as MAPK13, while others target multiple MAPKs such as MAPK13 and MAPK12. The compounds can be used therapeutica
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(2019/12/25)
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- Cationic poly(ester amide) dendrimers: Alluring materials for biomedical applications
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Novel cationic poly(ester amide) dendrimers have been synthesized by copper(i) azide-alkyne cycloaddition (CuAAC) of a tripropargylamine core and azide-terminated dendrons, in turn prepared by iterative amide coupling of the new monomer 2,2′-bis(glycyloxymethyl)propionic acid (bis-GMPA). The alternation of ester and amide groups provided a dendritic scaffold that was totally biocompatible and degradable in aqueous media at physiological and acidic pH. The tripodal dendrimers naturally formed rounded aggregates with a drug that exhibited low water solubility, camptothecin, thus improving its cell viability and anti-Hepatitis C virus (anti-HCV) activity. The presence of numerous peripheral cationic groups enabled these dendrimers to form dendriplexes with both pDNA and siRNA and they showed effective in vitro siRNA transfection in tumoral and non-tumoral cell lines.
- Lancelot, Alexandre,González-Pastor, Rebeca,Clavería-Gimeno, Rafael,Romero, Pilar,Abian, Olga,Martín-Duque, Pilar,Serrano, José L.,Sierra, Teresa
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supporting information
p. 3956 - 3968
(2018/06/21)
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- 2-methyl-2-(5-fluorouracil)carbonyltrimethylene carbonate as well as preparation method and application thereof
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The invention provides a monomer material 2-methyl-2-(5-fluorouracil)carbonyltrimethylene carbonate which can be used for synthesizing biodegradable polycarbonate, wherein the 2-methyl-2-(5-fluorouracil)carbonyltrimethylene carbonate is a white crystal, t
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Paragraph 0015, 0016; 0017; 0018
(2017/06/02)
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- ANTIBACTERIAL POLYMER, PRODUCTION METHOD THEREFOR, AND USAGE THEREOF
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Provided is a polymer material having effective antibacterial properties and having bio adaptability in which cytotoxicity, especially low hemolysis, when used in contact with in vivo tissue and blood is suppressed so as to be low. The polymer is characte
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Paragraph 0125; 0126
(2017/08/07)
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- Fluorine-containing carboxylic acid compound
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PROBLEM TO BE SOLVED: To provide a fluorinated carbon group-containing carboxylic acid that is dissolved in organic solvent, has excellent surface tension reduction ability, and has a small number of carbon atoms, and a surfactant. SOLUTION: The present i
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Paragraph 0051
(2017/04/25)
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- Method of biomolecule immobilization on polymers using click-type chemistry
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The present invention provides a method for the covalent immobilization of biomolecules on polymers for delivery of the biomolecules, which has the advantage of being simple, highly efficient, environmentally friendly and free of side products relative to traditional immobilization techniques. The invention provides a modified micro/nanoparticle system, which uses a functionalized polymer formed into micro or nanoparticles to bind a molecule to the particles using uses facile chemistry, the Diels-Alder cycloaddition between a diene and a dienophile with the polymer being functionalized with one of them and the molecule with the other, or the Huisgen 1,3-dipolar cycloaddition between a terminal alkyne and an azide to bind the molecule to the particle. The molecules and/or other therapeutic agents may be encapsulated within the polymer particles for intravenous therapeutic delivery. The invention also provides a novel synthetic biodegradable polymer, a furan/alkyne-functionalized poly(trimethylene carbonate) (PTMC)-based polymer, whose composition can be designed to meet the defined physical and chemical property requirements. In one example, the particle system self-aggregates from functionalized PTMC-based copolymers containing poly(ethylene glycol) (PEG) segments. The composition of the copolymers can be designed to meet various particle system requirements, including size, thermodynamic stability, surface PEG density, drug encapsulation capacity and biomolecule immobilization capacity.
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- 1,3,6-DIOXAZOCAN-2-ONES AND ANTIMICROBIAL CATIONIC POLYCARBONATES THEREFROM
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Eight-membered ring cyclic carbonates comprising a ring nitrogen at position 6 (1,3,6-dioxazocan-2-ones) were prepared by reaction of precursor diols with active carbonates. The ring nitrogen is linked to a pendant group Y′ via a methylene linking group.
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Paragraph 0201
(2015/11/10)
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- ANTIMICROBIAL CATIONIC POLYAMINES
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Antimicrobial, non-hemolytic cationic polyamines were prepared by treating partially N-acylated polyethylenimines and/or partially oxidized polyethylenimines with a protic acid. The cationic polyamines can have a linear or branched polyethylenimine backbone structure. Preferably, the cationic polyamines comprise pendant urea groups, which can be introduced via a cyclic carbonate comprising a pendant urea group. The cationic polyamines can be active against a tuberculosis mycobacterium at low concentration. The cationic polyamines are also effective against Gram-negative Escherichia coli and Pseudomonas aeruginosa, Gram-positive Staphylococcus aureus, and fungus Candida albicans in solution and in the form of a film.
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Paragraph 0159-0160
(2015/12/23)
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- SELF-ASSEMBLING BIS-UREA COMPOUNDS FOR DRUG DELIVERY
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Cationic, anionic, and/or zwitterionic bis-urea compounds self-assemble by non-covalent interactions in aqueous solution to form high aspect ratio nanofibers. The nanofibers reversibly bind drugs by non-covalent interactions, forming drug compositions for exhibiting sustained release of the drug.
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Paragraph 0078
(2015/02/19)
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- ANTI-MUCUS DRUGS AND USES THEREFOR
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Disclosed are methods of identifying, generating and synthesizing compounds that inhibit MAPK13 activity. In various embodiments, compounds, salts thereof and prodrugs thereof of the present teachings can be useful for the treatment of diseases and disord
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Paragraph 0207; 0211
(2015/07/15)
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- Highly Selective Biocatalytic Transesterification Reactions on Aryl 3-hydroxy-2-(hydroxymethyl)-2-methylpropanoates
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Acid anhydrides have been used to carry out the regioselective acylation of primary hydroxyl group in benzyl 3-hydroxy-2-(hydroxymethyl)-2-methylpropanoate and 4-fluorobenzyl 3-hydroxy-2-(hydroxymethyl)-2-methylpropanoate and deacylation of their diesters in the presence of Lipozyme TL IM in diisopropyl ether. Amongst different acid anhydrides used, butanoic anhydride was found to be the best acylating agent as compared to others. Both acylation and deacylation reactions were highly selective and efficient yielding exclusively the monoacylated products in 70-88 % yields.
- Kumar, Gaurav,Dhawan, Ashish,Singh, Brajendra K.,Sharma, Nawal K.,Sharma, Sunil K.,Prasad, Ashok K.,Van Der Eycken, Erik V.,Len, Christophe,Watterson, Arthur C.,Parmar, Virinder S.
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p. 919 - 929
(2015/08/06)
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- POLYCARBONATES BEARING PENDANT PRIMARY AMINES FOR MEDICAL APPLICATIONS
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An antimicrobial composition comprises an anionic drug and an amine polymer comprising a first repeat unit of formula (2); wherein a' is an integer equal to 1 or 2, b' is an integer equal to 1 or 2, and each R' is an independent monovalent radical selecte
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Paragraph 00119-00120
(2014/04/03)
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- ANTIMICROBIAL CATIONIC POLYCARBONATES
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Antimicrobial cationic polymers having one or two cationic polycarbonate chains were prepared by organocatalyzed ring opening polymerization. One antimicrobial cationic polymer has a polymer chain consisting essentially of cationic carbonate repeat units
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Paragraph 0470-0471
(2014/10/16)
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- ANTIMICROBIAL CATIONIC POLYCARBONATES
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Antimicrobial cationic polymers having one or two cationic polycarbonate chains were prepared by organocatalyzed ring opening polymerization. One antimicrobial cationic polymer has a polymer chain consisting essentially of cationic carbonate repeat units
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Paragraph 0457; 0458
(2014/10/16)
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- ANTIMICROBIAL COMPOSITIONS, METHODS OF PREPARATION THEREOF, AND USES THEREOF
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A composition of matter comprises a cationic polymer comprising a polycarbonate chain fragment, the polycarbonate chain fragment comprising a repeat unit comprising a side chain moiety containing a quaternary amine group; and a non-charged polymer comprising a polyester chain segment and a poly(alkylene oxide) chain segment; wherein i) the cationic polymer and the non-charged polymer are amphiphilic and biocompatible, ii) the cationic polymer and the non-charged polymer form a mixed complex by non-covalent interactions in water, and iii) the mixed complex is a more effective antimicrobial agent against at least a Gram-negative microbe compared to the cationic polymer and the non-charged polymer alone when tested using otherwise identical conditions.
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Page/Page column 29-30
(2012/10/08)
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- Degradable self-assembling dendrons for gene delivery: Experimental and theoretical insights into the barriers to cellular uptake
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This paper uses a combined experimental and theoretical approach to gain unique insight into gene delivery. We report the synthesis and investigation of a new family of second-generation dendrons with four triamine surface ligands capable of binding to DN
- Barnard, Anna,Posocco, Paola,Pricl, Sabrina,Calderon, Marcelo,Haag, Rainer,Hwang, Mark E.,Shum, Victor W. T.,Pack, Daniel W.,Smith, David K.
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supporting information; scheme or table
p. 20288 - 20300
(2012/02/05)
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- Novel chemoenzymatic methodology for the regioselective glycine loading on polyhydroxy compounds
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In the present work, we have developed a highly efficient temperature-dependent chemo-enzymatic methodology for the regioselective synthesis of novel esters of glycerol, G1 tri-glycerol dendrons and related esters for the first time using 4-nitrophenyl 2-(tert-butoxycarbonyl)acetate (Boc-gly-Ph-pNO2) (2) as the acylating agent. This methodology offers efficient and controlled loading of amino acid (glycine) on polyhydroxy compounds.
- Malhotra, Shashwat,Calderon, Marcelo,Prasad, Ashok K.,Parmar, Virinder S.,Haag, Rainer
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experimental part
p. 2228 - 2237
(2010/07/04)
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- MASKED CARBOXYLATE NEOPENTYL SULFONYL ESTER CYCLIZATION RELEASE PRODRUGS OF ACAMPROSATE, COMPOSITIONS THEREOF, AND METHODS OF USE
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Masked carboxylate neopentyl sulfonyl ester prodrugs of acamprosate, pharmaceutical compositions comprising such prodrugs, and methods of using such prodrugs and compositions thereof for treating diseases are disclosed. In particular, acamprosate prodrugs
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(2009/04/24)
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- Synthesis and catalytic antibody functionalization of dendrimers
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Antibody 38C2 catalyzed a retro-aldol process upon dendritic modified aliphatic polyesters. This catalytic system was studied in detail and displayed rate enhancements, kcat/kuncat, of greater than 106. These antibody-catalyzed reactions took place in a stepwise manner yielding partially modified aldol-dendrimers until a fully substituted aldehyde dendrimer was formed. The catalytic antibody 38C2 only reacted with surface-exposed aldol moieties and did not significantly interact with the core groups for dendrons 4 and 8. For a higher generation dendron 8 the rate of unmasking slightly decreased presumably due to steric crowding of the aldol functionalities. In addition, catalytic antibody 38C2 was able to selectively differentiate block-hybrid dendrons and was regiospecific in the retro-aldol reaction of dendron 21. This is an inaugural report of a catalytic antibody utilizing dendrimers as substrates and suggests that antibodies could be used as selective catalysts for the controlled release and activation of specific molecules attached to biodegradable polymeric materials. Furthermore, this is the first example of catalytic antibody 38C2 displaying regioselectivity on a multifunctional aldol substrate. Important for synthetic applications is the antibody's ability to selectively differentiate regions on dendritic substrates and produce partly aldol functionalized dendrons under conditions mild enough to avoid β-elimination.
- Cordova,Janda
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p. 8248 - 8259
(2007/10/03)
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- Synthesis, characterization, and 1H NMR self-diffusion studies of dendritic aliphatic polyesters based on 2,2-bis(hydroxymethyl)propionic acid and 1,1,1-tris(hydroxyphenyl)ethane
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Dendritic aliphatic polyesters of one, two, three, and four generations (M(w): 906, 1856, 3754, and 7549 g/mol) were synthesized in the convergent fashion, using 2,2-bis(hydroxymethyl)propionic acid as building block and 1,1,1-tris(hydroxyphenyl)ethane as
- Ihre, Henrik,Hult, Anders,S?derlind, Erik
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p. 6388 - 6395
(2007/10/03)
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