Couldn't find what you were looking for?
Advanced Search
Article Types:
Medicinal chemistry and pharmaceutical chemistry are disciplines at the intersection of chemistry, especially synthetic organic chemistry, and pharmacology and various other biological specialties, where they are involved with design, chemical synthesis and development for market of pharmaceutical agents, or bio-active molecules.

26094 Results for the subject "Medicinal Chemistry":

PerspectiveFeatureMedicinal chemistry matters – a call for discipline in our discipline

Medicinal chemistry makes a vital contribution to small molecule drug discovery, and the quality of it contributes directly to research effectiveness as well as to downstream costs, speed and survival in development. In recent years, the discipline of medicinal chemistry has evolved and witnessed many noteworthy contributions that propose and offer potential improvements to medicinal chemistry practice; however, the impact of these ideas is limited by their acceptance and deployment into every-day activity and, as a result, the quality of medicinal chemistry remains variable. For the good of the industry and the medicinal chemistry discipline, there is a need to move from retrospective learning to prospective control of medicinal chemistry practice to improve cost effectiveness, probability of success and survival rates.

Craig Johnstone Publication date: 2012/06/01
ReviewPost screenCollaborative practices for medicinal chemistry research across the big pharma and not-for-profit interface

Highlights•Many global research groups are using collaborative medicinal chemistry to derisk early portfolios.•The opportunities and issues in inter-organizational medicinal chemistry are discussed.•Emerging solutions to enhancing drug discovery by collaboration are presented.

David M. Andrews Publication date: 2014/04/01
Review articleRecent applications of hydantoin and thiohydantoin in medicinal chemistry

Highlights•Recent applications of (thio)hydantoin scaffold in medicinal chemistry and drug discovery.•(Thio)hydantoins as useful scaffold in medicinal chemistry due to their synthetic feasibility and versatility of substituents.•Brief structure-activity relationship for each biological activity.

SeoHyun Cho Publication date: 2019/02/15
Medicinal chemistry in the development of societies: Biodiversity and natural products

AbstractThis document has been elaborated by the IUPAC Medicinal Chemistry section and is backed by a large number of scientists, many of whom have had direct involvement and whose names appear at the end of the article. This work discusses the role that the discovery of new medicinal agents has in the development of societies as well as in the conservation of biodiversity in terms of work carried out on natural products. Also included are several recommendations for countries which are presently in search of their own scientific and technological development in medicinal agents. The IUPAC Medicinal Chemistry section would appreciate the collaboration of the scientific societies in every country to aid in the diffusion of this document.

A. Monge Publication date: 2000/12/01
ReviewFoundationIndustrial medicinal chemistry insights: neuroscience hit generation at Janssen

Highlights•Modern medicinal Chemistry is highly multidisciplinary.•Chemistry can provide drug discovery innovation in many ways.•A dedicated team was established to explore new areas and hit generation.•Impact over many areas including fragment screening, novel synthesis, delivery.

Gary Tresadern Publication date: 2017/10/01
The medicinal chemistry of carboranes

AbstractThe medicinal chemistry of dicarba-closo-dodecaboranes (otherwise referred to as carboranes) has traditionally centered on their use in boron neutron capture therapy (BNCT). More recently, work has begun to exploit the unique chemical and physical properties of carboranes for the preparation of novel inorganic pharmaceuticals and biological probes. This review is designed to highlight some of the recent work concerning medicinal carborane chemistry including the synthesis and testing of new BNCT agents. Following this review, as an appendix, is an illustrated summary of reactions involving carboranes reported in literature since 1992.

John F Valliant Publication date: 2002/10/01
ReviewMedicinal uses, chemistry and pharmacology of Dillenia species (Dilleniaceae)

Highlights•The medicinal uses of Dillenia species are reviewed.•The phytochemistry dominated by flavonoids and triterpenoids is presented.•The pharmacological aspect of extracts and pure compounds is comprehensively discussed.•The relationship of medicinal uses, pharmacology and chemistry is also described.

Carla W. Sabandar Publication date: 2017/02/01
ReviewMedicinal chemistry and therapeutic potential of CpG DNA

AbstractThe observation that oligodeoxynucleotides containing CpG dinucleotides (CpG DNA) exhibit several immunological effects has led to their use as therapeutic agents and adjuvants for various diseases. Several CpG DNA drug candidates are currently being evaluated, either as monotherapies or as adjuvants (with vaccines, antibodies, antigens and allergens), in preclinical and clinical trials against cancers, viral and bacterial infections, allergies and asthma. Knowledge gained from studies of the medicinal chemistry of CpG DNA has provided a basis for designing a second generation of CpG DNA agents with desirable cytokine-inducing and potent immunomodulatory activity. This article reviews recent progress in understanding the effects of CpG DNA, the medicinal chemistry of CpG DNA, and its possible therapeutic applications.

Sudhir Agrawal Publication date: 2002/03/01
Digest paperC–H activation reactions as useful tools for medicinal chemists

AbstractIn recent years, there has been an exponential rise in the number of reports describing synthetic methods that utilize catalytic sp3 and sp2 C–H bond activation. Many have emerged as powerful synthetic tools for accessing biologically active motifs. Indeed, application to C–C and C–heteroatom bond formation, provides new directives for the construction of new pharmaceutical entities. Herein, we highlight some recent novel C–H activation processes that exemplify the utility of these transformations in medicinal chemistry.

Eduardo J.E. Caro-Diaz Publication date: 2016/11/15
ReviewMicrowave-assisted high-speed chemistry: a new technique in drug discovery

AbstractIn both lead identification and lead optimization processes there is an acute need for new organic small molecules. Traditional methods of organic synthesis are orders of magnitude too slow to satisfy the demand for these compounds. The fields of combinatorial and automated medicinal chemistry have been developed to meet the increasing requirement of new compounds for drug discovery; within these fields, speed is of the essence. 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. We believe that the time saved by using focused microwaves is potentially important in traditional organic synthesis but could be of even greater importance in high-speed combinatorial and medicinal chemistry.

Mats Larhed Publication date: 2001/04/15
Chapter 2 - Recent Progress of Phosphonium Coupling in Heterocyclic and Medicinal Chemistry

AbstractThe discovery, development, and recent application of phosphonium coupling as a new methodology for the efficient synthesis of heterocyclic compounds in the past 10 years are reviewed.

Fu-An Kang Publication date: 2015/01/01
Synthesis of novel halo-oxybispyridines, new building blocks in cholinergic medicinal chemistry

AbstractThis paper describes a method for the preparation of oxybispyridines bearing several halogens, which could be further transformed into other functional groups thus giving access to libraries with the bis-pyridyl ether moiety as the common structural feature of interest in cholinergic medicinal chemistry. Scope and limitation of the method are outlined.

Anne Sophie Voisin Publication date: 2006/06/19
Chapter Twenty-Eight - Drug Design Strategies for GPCR Allosteric Modulators

AbstractTerms such as “nondruggable GPCRs” describe a unique group of GPCRs having strong biological hypothesis validation, but for which medicinal chemistry efforts based on orthosteric ligands have failed to produce marketed drugs (or even clinical development candidates). These receptors remain attractive as biological targets for new drugs, but a novel medicinal chemistry strategy must be developed to modulate their biological effects. This may be possible by modulating receptors using allosteric ligands, which interact with the receptor at a binding site topographically distinct from the endogenous ligandThis account reviews emerging empirical observations on GPCR allosteric ligand design and presents a number of medicinal chemistry strategies to address current challenges in a productive manner from the drug discovery standpoint.

P. Jeffrey Conn Publication date: 2012/01/01
ReviewPost screenSubtleties in GPCR drug discovery: a medicinal chemistry perspective

Therapeutic effects through G protein-coupled receptors (GPCRs) are promoted by a full agonist, partial agonist, neutral antagonist or inverse agonist. Dramatic change of function such as from a neutral antagonist to a full agonist with minimal variation of ligand structure is a phenomenon that medicinal chemists often encounter. This is also influenced by a change of assay format. The subtle nature of structure–function relationships is difficult to grasp unless carefully considered from both chemistry and assay perspectives. In this article we discuss the subtle aspects of GPCR drug discovery from the medicinal chemistry perspective.

Masahiko Fujioka Publication date: 2012/10/01
Chapter Five - Poly-NHC Complexes of Transition Metals: Recent Applications and New Trends

AbstractThe most significant recent developments in the chemistry of transition metal complexes with poly-N-heterocyclic carbene ligands (poly-NHCs) are reviewed herein. In particular, attention is focussed on the preparation of novel poly-NHCs, on their coordination chemistry toward transition metal centers, and on the applications of the resulting complexes, which nowadays range from catalysis to photophysics and medicinal chemistry. The goal is to highlight the most important recent achievements in this complex field and to give to the reader an overview on the broad chemistry of these compounds.

Andrea Biffis Publication date: 2015/01/01
Chapter 2 - Medicinal Chemistry: Definitions and Objectives, Drug Activity Phases, Drug Classification Systems

Publisher SummaryMedicinal chemistry remains a challenging science that provides profound satisfaction to its practitioners and focuses on the discovery, development, identification, and interpretation of the mode of action of biologically active compounds at the molecular level. It is concerned with this interaction, focusing on the organic and biochemical reactions of drug substances with their targets. This is one aspect of drug chemistry. Other important aspects are the synthesis and the analysis of drug substances. The role of medicinal chemistry in drug development is most prominent in the following three steps: discovery, optimization, and development. The way of a drug into the body, to its target(s), and out again can be broken down into three mechanistically distinct phases, the second and third being partly simultaneous. During drug development, all three phases are investigated interdependently because structural changes required for one phase must not abolish suitability i Read more...

Peter Imming Publication date: 2008/01/01
Drug Guru: A computer software program for drug design using medicinal chemistry rules

AbstractDrug Guru™ (drug generation using rules) is a new web-based computer software program for medicinal chemists that applies a set of transformations, that is, rules, to an input structure. The transformations correspond to medicinal chemistry design rules-of-thumb taken from the historical lore of drug discovery programs. The output of the program is a list of target analogs that can be evaluated for possible future synthesis. A discussion of the features of the program is followed by an example of the software applied to sildenafil (Viagra®) in generating ideas for target analogs for phosphodiesterase inhibition. Comparison with other computer-assisted drug design software is given.

Kent D. Stewart Publication date: 2006/10/15
Chapter 5 - Natural products: a continuing source of inspiration for the medicinal chemist

AbstractThe study of naturally occurring compounds has led to innumerable advances in pharmacology and medicine. For the medicinal chemist, a biologically active natural compound provides a useful template for designing novel molecules, which can be used to probe the mechanism of action of the parent compound, or to develop drugs with improved pharmacological profiles. The discipline of medicinal chemistry is therefore crucial to modern drug development. Developing countries are richly endowed with flora containing many useful natural products. Unfortunately, little effort has been made in these same countries to develop the expertise (in areas such as medicinal chemistry) required to mount a credible drug-development effort. The lack of expertise in modern drug-development methods has relegated most developing countries to the role of raw material supplier. To address this inadequacy, training programs in modern drug design and development should become an integral part of national po Read more...

S Mbua Ngale Efange Publication date: 2002/01/01
Benzoboroxoles: Synthesis and applications in medicinal chemistry

Highlights•Benzoboroxoles are cyclic boronic acid hemiesters that have gained prominence due to their excellent medicinal properties.•Tavaborole is a benzoboroxole that has been approved by the FDA for the treatment of onychomycosis.•Crisaborole is a benzoboroxole in clinical use for the treatment of atopic dermatitis.•Several other benzoboroxoles are under clinical trials for the treatment of a variety of diseases.•This review outlines the methods for the synthesis of benzoboroxoles and their applications in medicinal chemistry.

Gautam R. Mereddy Publication date: 2018/06/15
ReviewInteractions between proteins and Ru compounds of medicinal interest: A structural perspective

Highlights•Structures of adducts formed between Ru compounds and proteins are summarized.•The effect of Ru compound binding on the protein structure is discussed.•Recurrent features in the structures of Ru-protein adducts are highlighted.

Antonello Merlino Publication date: 2016/11/01
Back | Next (Page 1 of 12)
Advertisement
Join Copernicus Academic and get access to over 12 million papers authored by 7+ million academics.
Join for free!

Contact us