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Medicinal chemistry silicon

Seung-Kyun Kang, Jahyun Koo, Yoon Kyeung Lee, John A Rogers
Recent advances in materials chemistry establish the foundations for unusual classes of electronic systems, characterized by their ability to fully or partially dissolve, disintegrate, or otherwise physically or chemically decompose in a controlled fashion after some defined period of stable operation. Such types of "transient" technologies may enable consumer gadgets that minimize waste streams associated with disposal, implantable sensors that disappear harmlessly in the body, and hardware-secure platforms that prevent unwanted recovery of sensitive data...
May 15, 2018: Accounts of Chemical Research
Huaquan Fang, Wenjun Hou, Guixia Liu, Zheng Huang
Incorporating the silicon element into bioactive organic molecules has received increasing attention in medicinal chemistry. Moreover, organosilanes are valuable synthetic intermediates for fine chemicals and materials. Transition metal-catalyzed C-H silylation has become an important strategy for C-Si bond formations. However, despite the great advances in aromatic C(sp2 )-H bond silylations, catalytic methods for aliphatic C(sp3 )-H bond silylations are relatively rare. Here we report a pincer ruthenium catalyst for intramolecular silylations of various primary C(sp3 )-H bonds adjacent to heteroatoms (O, N, Si, Ge), including the first intramolecular silylations of C-H bonds α to O, N, and Ge...
August 23, 2017: Journal of the American Chemical Society
Tuncay Ozel, Benjamin A Zhang, Ruixuan Gao, Robert W Day, Charles M Lieber, Daniel G Nocera
Development of new synthetic methods for the modification of nanostructures has accelerated materials design advances to furnish complex architectures. Structures based on one-dimensional (1D) silicon (Si) structures synthesized using top-down and bottom-up methods are especially prominent for diverse applications in chemistry, physics, and medicine. Yet further elaboration of these structures with distinct metal-based and polymeric materials, which could open up new opportunities, has been difficult. We present a general electrochemical method for the deposition of conformal layers of various materials onto high aspect ratio Si micro- and nanowire arrays...
July 12, 2017: Nano Letters
Chen Fu, Bin Fu, Xixi Peng, Guojian Liao
Octahedral transition metal complexes have been shown to have tremendous applications in chemical biology and medicinal chemistry. Meanwhile, structural transition metals can be replaced by inert octahedral silicon in a proof-of-principle study. We here introduce the first example of octahedral silicon complexes, which can very well serve as an efficient antimicrobial agent. The typical silicon arenediolate complex 1 {[(phen)₂Si(OO)](PF₆)₂, with phen = 1,10-phenanthroline, OO = 9,10-phenanthrenediolate} exhibited significant inhibition towards the growth of Cryptococcus neoformans with MIC and MFC values of 4...
April 15, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Shinya Fujii, Yuichi Hashimoto
Application of silyl functionalities is one of the most promising strategies among various 'elements chemistry' approaches for the development of novel and distinctive drug candidates. Replacement of one or more carbon atoms of various biologically active compounds with silicon (so-called sila-substitution) has been intensively studied for decades, and is often effective for alteration of activity profile and improvement of metabolic profile. In addition to simple C/Si exchange, several novel approaches for utilizing silicon in medicinal chemistry have been suggested in recent years, focusing on the intrinsic differences between silicon and carbon...
April 2017: Future Medicinal Chemistry
E Peter Magennis, Andrew L Hook, Paul Williams, Morgan R Alexander
Biomedical devices are indispensable in modern medicine yet offer surfaces that promote bacterial attachment and biofilm formation, resulting in acute and chronic healthcare-associated infections. We have developed a simple method to graft acrylates to silicone rubber, polydimethylsiloxane (PDMS), a commonly used device material that is often colonized by bacteria. We demonstrate a novel method whereby nontoxic bacteria attachment-resistant polymers can be readily grafted from and grafted to the surface using thiol-ene chemistry, substantially reducing bacterial colonization...
November 16, 2016: ACS Applied Materials & Interfaces
Adel Dalilottojari, Bahman Delalat, Frances J Harding, Michaelia P Cockshell, Claudine S Bonder, Nicolas H Voelcker
Porous silicon (pSi) substrates are a promising platform for cell expansion, since pore size and chemistry can be tuned to control cell behavior. In addition, a variety of bioactives can be loaded into the pores and subsequently released to act on cells adherent to the substrate. Here, we construct a cell microarray on a plasma polymer coated pSi substrate that enables the simultaneous culture of human endothelial cells on printed immobilized protein factors, while a second soluble growth factor is released from the same substrate...
November 14, 2016: Biomacromolecules
Laetitia Mistico, Olivier Querolle, Lieven Meerpoel, Patrick Angibaud, Muriel Durandetti, Jacques Maddaluno
A simple and efficient approach to new silylated heterocycles of potential interest in medicinal chemistry is presented. A set of bromophenyl trimethylsilyl pyrazole intermediates can be transformed by direct organometallic routes into two families of regioisomeric iodoaryl substrates; using either arylzinc or aryllithium chemistry, the TMS group remains on the pyrazole ring or translocates to the aryl moiety. These two families can then be efficiently transformed into benzo silino pyrazoles thanks to a single-step cyclization relying on the Pd-catalyzed activation of a non-activated C(sp(3) )-H bond alpha to a silicon atom...
July 4, 2016: Chemistry: a European Journal
Karolina Maria Nowak, Arkadiusz Szterk, Piotr Fiedor, Kazimiera Henryka Bodek
The introduction of new test methods and the modification of existing ones are crucial for obtaining reliable results, which contributes to the development of innovative materials that may have clinical applications. Today, silicone is commonly used in medicine and the diversity of its applications are continually growing. The aim of this study is to evaluate the mucoadhesiveness of polymeric membranes by a method that modifies the existing test methods through the introduction of silicone discs. The matrices were designed for clinical application in the management of diseases within the oral cavity...
March 2016: Acta Poloniae Pharmaceutica
Jens Ducrée
The field of microfluidics has seen breath-taking progress since its beginnings in the 1980s and early 1990s. While much of the initial work was a by-product of mainstream micro-electro-mechanical systems (MEMS) and silicon based fabrication schemes, soon a specialized research field developed. Over the last decade a strong, highly interdisciplinary microfluidics community emerged with roots in classical silicon microfabrication as well as chemistry, physics, biotechnology, medicine and various engineering disciplines...
2012: Diagnostics
Carol A McCarthy, Robert J Ahern, Rakesh Dontireddy, Katie B Ryan, Abina M Crean
INTRODUCTION: Silica materials, in particular mesoporous silicas, have demonstrated excellent properties to enhance the oral bioavailability of poorly water-soluble drugs. Current research in this area is focused on investigating the kinetic profile of drug release from these carriers and manufacturing approaches to scale-up production for commercial manufacture. AREAS COVERED: This review provides an overview of different methods utilized to load drugs onto mesoporous silica carriers...
2016: Expert Opinion on Drug Delivery
Itai Katz, Aharon Blank
Dynamic nuclear polarization (DNP) is a method for enhancing nuclear magnetic resonance (NMR) signals that has many potential applications in chemistry and medicine. Traditionally, DNP signal enhancement is achieved through the use of exogenous radicals mixed in a solution with the molecules of interest. Here we show that proton DNP signal enhancements can be obtained for solid samples without the use of solvent and exogenous radicals. Radicals are generated primarily on the surface of a solid sample using electrical discharges...
December 2015: Journal of Magnetic Resonance
Wing Yin Tong, Martin J Sweetman, Ezzat R Marzouk, Cara Fraser, Tim Kuchel, Nicolas H Voelcker
Advanced biosensors in future medicine hinge on the evolvement of biomaterials. Porous silicon (pSi), a generally biodegradable and biocompatible material that can be fabricated to include environment-responsive optical characteristics, is an excellent candidate for in vivo biosensors. However, the feasibility of using this material as a subcutaneously implanted optical biosensor has never been demonstrated. Here, we investigated the stability and biocompatibility of a thermally-hydrocarbonised (THC) pSi optical rugate filter, and demonstrated its optical functionality in vitro and in vivo...
January 2016: Biomaterials
Marcel Geyer, Johannes A Baus, Ola Fjellström, Eric Wellner, Linda Gustafsson, Reinhold Tacke
The GPR81 and GPR109A receptors mediate antilipolytic effects and are potential drug targets for the treatment of metabolic disorders such as dyslipidemia and type 2 diabetes. There is still a need to identify potent GPR81 agonists as pharmacological tools. A high-throughput screen identified an acylurea-based GPR81 agonist lead series, with activities at the GPR109A receptor as well. To expand the chemical scope and to explore the pharmacological and pharmacokinetic consequences, a series of structurally related organosilicon compounds with a 6-sila-4,5,6,7-tetrahydrobenzo[d]thiazole skeleton was synthesized and studied for their physicochemical properties [octanol/water distribution coefficient (pH 7...
December 2015: ChemMedChem
Hyder Aliyar, Gerald Schalau
Silicones have been used in medicines, cosmetics and medical devices for over 60 years. Polydimethylsiloxanes are polymers that are typically used either as an active in oral drug products or as excipients in topical and transdermal drug products. Inherent characteristics like hydrophobicity, adhesion and aesthetics allow silicones to offer function and performance to drug products. Recent technologies like swollen crosslinked silicone elastomer blend networks, sugar siloxanes, amphiphilic resin linear polymers and silicone hybrid pressure sensitive adhesives promise potential performance advantages and improved drug delivery efficacy...
July 2015: Therapeutic Delivery
Lifei Zhu, Miao Li, Junxing Dong, Yiguang Jin
Acute lung injury (ALI) is a severe disease, leading to death if not treated quickly. An emergency medicine is necessary for ALI therapy. Dimethyl silicone (DMS) is an effective agent to defoam the bubbles in the lung induced by ALI. However, DMS aerosols, a marketed formulation of DMS, affect environments and will be limited in the future. Here we firstly report a dry nanoemulsion inhalation for pulmonary delivery. Novel DMS dry nanoemulsion inhalations (DSNIs) were developed in this study. The optimal formulation of stable and homogenous DMS nanoemulsions (DSNs) was composed of Cremophor RH40/PEG 400/DMS (4:4:2, w/w/w) and water...
August 1, 2015: International Journal of Pharmaceutics
Lauren D Zarzar, Vishnu Sresht, Ellen M Sletten, Julia A Kalow, Daniel Blankschtein, Timothy M Swager
Emulsification is a powerful, well-known technique for mixing and dispersing immiscible components within a continuous liquid phase. Consequently, emulsions are central components of medicine, food and performance materials. Complex emulsions, including Janus droplets (that is, droplets with faces of differing chemistries) and multiple emulsions, are of increasing importance in pharmaceuticals and medical diagnostics, in the fabrication of microparticles and capsules for food, in chemical separations, in cosmetics, and in dynamic optics...
February 26, 2015: Nature
Raquel Ortega, Jorge Sanchez-Quesada, Christoph Lorenz, Grzegorg Dolega, Anna Karawajczyk, Miguel Sanz, Graham Showell, Fabrizio Giordanetto
The introduction of silicon in biologically-relevant molecules represents an interesting medicinal chemistry tactic. Its use is mainly confined to the fine-tuning of specific molecular properties and organosilicon compounds are underrepresented in typical screening libraries. As part of the European Lead Factory efforts to generate novel, drug discovery-relevant chemical matter, the design and synthesis of 1,1-disubstituted-1-silacycloalkane-based compound libraries is described.
June 1, 2015: Bioorganic & Medicinal Chemistry
Xiaolin Wang, Nada Ben Ahmed, Gisela S Alvarez, Maria V Tuttolomondo, Christophe Hélary, Martin F Desimone, Thibaud Coradin
The sol-gel process provides a robust and versatile technology for the immobilization of biologicals. A wide range of inorganic, composites and hybrid materials can be prepared to encapsulate molecular drugs, proteins, antibodies/antigens, enzymes, nucleic acids, prokaryotic and eukaryotic cells into bulk gels, particles and films. This review describes the applications of sol-gel encapsulation relevant to medicinal chemistry focusing on the recent development of biosensors as well as systems for production, screening and delivery of bioactive compounds and biomaterials...
2015: Current Topics in Medicinal Chemistry
Wan-Ling Liu, Ni-Shin Yang, Ya-Ting Chen, Stephen Lirio, Cheng-You Wu, Chia-Her Lin, Hsi-Ya Huang
A green and sustainable strategy synthesizes clinical medicine warfarin anticoagulant by using lipase-supported metal-organic framework (MOF) bioreactors (see scheme). These findings may be beneficial for future studies in the industrial production of chemical, pharmaceutical, and agrochemical precursors.
January 2, 2015: Chemistry: a European Journal
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