MAOS and Medicinal Chemistry: Some Important Examples from the Last Years (original) (raw)
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ChemInform Abstract: Microwave-Assisted Organic Synthesis: An Alternative Synthetic Strategy
ChemInform, 2011
Pharmaceutical companies have made major investments in high-throughput technologies for genomic and proteomic research, combinatorial chemistry and biological screening in order to identify more potential drug candidates at a faster pace. However, synthesis and lead compound optimisation remain the bottlenecks in the drug discovery process. Developing chemical compounds with the desired biological properties is time-consuming and expensive. Consequently, increasing interest is being directed towards technologies that allow more rapid synthesis and screening of chemical substances to identify compounds with functional qualities. Microwave heating is a process within a family of electroheat techniques, such as induction, radio frequency, direct resistance or infra-red heating, all of which utilise specific parts of the electromagnetic spectrum. These processes supplement, and in specific cases totally replace, conventional heating or drying systems used in industry. There is hardly any reaction type or name reaction that has not yet been tested in the microwave field. This is because some conventional systems are very bulky, not easy to operate, can pollute the environment due to harmful omissions and above all can be very inefficient. The major advantages of using microwaves are rapid heat transfer, volumetric and selective heating, compactness of equipment, speed of switching on and off and pollution-free environment as there are no products of combustion. Microwave leakage can certainly be kept well below government recommended levels. It has long been established that a dielectric material can be processed with energy in the form of high-frequency electromagnetic waves. The present review article describes the mechanism of microwave heating and comparison of the conventional and microwave assisted organic synthesis to improve the synthesis of the organic molecules.
A simple and efficient method has been developed for the synthesis of 1,3-dihydro-2H-indol-2-one derivatives using microwave irradiation technique. By taking advantage of the efficient source of energy of microwave, compound libraries for lead generation and optimization can be assembled in a fraction of time. In the present work, first the Schiff 's bases are synthesized by reaction of isatin with substituted anilines in the presence of acetic acid under microwave heating. Then the condensation of Schiff bases with different secondary amines in the presence of formaldehyde produces Mannich bases. The newly synthesized Mannich bases were characterized by means of spectral data and then evaluated for anthelmintic activity against Pheretima posthuma (Indian earthworm) and compared with standard albendazole. The compounds were evaluated at the concentrations of 10, 20, and 50 mg/mL. The effect of the standard drug albendazole at 10 mg/mL was also evaluated. The results of the present study indicate that some of the test compounds significantly demonstrated paralysis and also caused death of worms in a dose-dependent manner.
The Impact of Microwave Irradiation Reaction in Medicinal Chemistry: A Review
Oriental journal of chemistry, 2021
The present review collects an update of the reactions in the area of medicinal chemistry using microwave irradiation. This review come up with an overview of most salient reactions performed under microwave irradiation in the field of drug discovery. Moreover, chemists are preferring to use this reaction rapidly in the academic as well as pharmaceutical laboratory during their drug discovery and making library of compounds. This reaction is much greener using less amount and readily recyclable solvents or sometimes reaction process without solvents and product become much cleaner, often yields are better than the conventional heating. Microwave irradiation is now very robust instrument used in company in the field of drug discovery, due to reduce the reaction time from hour to minute or even second and efficiently creation of compound libraries through combinatorial methodology associated with drug discovery so that new therapeutic agents bring to the market quicker. Hopefully, we ...
Recent Applications of Microwaves in Synthesis of Bioactive Heterocyclic Compounds
Current Organic Chemistry, 2008
Over the past decade, use of microwave energy, to heat chemical reactants on a laboratory scale, has evolved as a well-demonstrated alternative to traditional heating. Clean chemistry, reduction in reaction times, improved yields, and applicability to wide range of reactions, greatly improved efficiency with better quality, safety and tremendous scope for automation are some of the benefits of this emerging technology. Association of biological activity with heterocyclic motifs is well known and is important from drug discovery viewpoint. This article gives an account of the recent applications of microwaves in the synthesis of biologically active heterocyclic compounds with synthesis schemes and/or comprehensive review of reaction conditions and biological importance of over 50 such applications.
Microwave Assisted Synthesis: A New Technology in Drug Discovery
Mini-Reviews in Medicinal Chemistry, 2009
The interest in the microwave assisted organic synthesis has been growing during the recent years. It results from an increasing knowledge of fundamentals of the dielectric heating theory, availability of an equipment designed especially for the laboratory use as well as the discovery of the special techniques of the microwave syntheses. The efficiency of microwave flash-heating chemistry in dramatically reducing reaction times (reduced from days and hours to minutes and seconds) has recently been proven in several different fields of organic chemistry and this aspect is of great importance in high-speed combinatorial and medicinal chemistry. In this contribution, the current state of the art is summarized providing examples of the most recent applications in the field of microwave assisted synthesis of biologically active compounds both in heterocyclic and in peptide and peptidomimetic optimization.
Microwave-Assisted Syntheses in Organic Chemistry
SpringerBriefs in Molecular Science, 2016
The second part focuses on the summary of typical organic chemical reactions selected, such as coupling reactions (C-C bond formation reactions, carbon-heteroatom bond formations),
Microwave Synthesis-A Potential Tool for Green Chemistry
sphinxsai.com
Microwave radiation, an electromagnetic radiation, is widely use as a source of heating in organic synthesis. The basic mechanisms observed in microwave assisted synthesis are dipolar polarization and conduction. Microwave assisted organic synthesis (MAOS) has emerged as a new "lead" in organic synthesis. The technique offers simple, clean, fast, efficient, and economic for the synthesis of a large number of organic molecules, have provided the momentum for many chemists to switch from traditional heating method to microwave assisted chemistry. In the recent year microwave assisted organic reaction has emerged as new tool in organic synthesis. In the present article an attempt was made to focus on what is microwave, how is it generated and what importance may it have.
Combinatorial Chemistry & High Throughput Screening, 2007
Microwave irradiation has been successfully applied in organic chemistry. Spectacular accelerations, higher yields under milder reaction conditions and higher product purities have all been reported. Indeed, a number of authors have described success in reactions that do not occur under conventional heating and modifications in selectivity (chemo-, regio-and stereoselectivity) have even been reported. Recent advances in microwave-assisted combinatorial chemistry include high-speed solid-phase and polymer-supported organic synthesis, rapid parallel synthesis of compound libraries, and library generation by automated sequential microwave irradiation. In addition, new instrumentation for high-throughput microwave-assisted synthesis continues to be developed at a steady pace. The impressive speed combined with the unmatched control over reaction parameters justifies the growing interest in this application of microwave heating. In this review we highlight our recent advances in this area, with a particular emphasis on cycloaddition reactions of heterocyclic compounds both with and without supports, applications in supramolecular chemistry and the reproducibility and scalability of organic reactions involving the use of microwave irradiation techniques.