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  • medicinal
  • Modern drug discovery involves the identification of screening hits, medicinal chemistry and optimization of those hits to increase the affinity, selectivity (to reduce the potential of side effects), efficacy/potency, metabolic stability (to increase the half-life), and oral bioavailability. (wikipedia.org)
  • This made for the beginning of the modern era in pharmacology, as pure chemicals, instead of crude extracts of medicinal plants, became the standard drugs. (wikipedia.org)
  • The SSRIs are the most significant class of antidepressants marketed in recent years and make one of the major medicinal discoveries of the last few decades. (wikipedia.org)
  • An initial success was achieved when medicinal chemists set out in search of the ideal SSRI with the chemical synthesis of zimelidine (figure 1) from the antihistamine drug brompheniramine, which exhibited selective inhibition of 5-HT re-uptake with minimal inhibition of norepinephrine (NE) re-uptake. (wikipedia.org)
  • compounds
  • Examples of drug compounds isolated from crude preparations are morphine, the active agent in opium, and digoxin, a heart stimulant originating from Digitalis lanata. (wikipedia.org)
  • The Community for Open Antimicrobial Drug Discovery (CO-ADD) is a not-for-profit initiative created in 2015 reaching out to chemists in academia and research organisations who have compounds that were not designed as antibiotics and would not otherwise be screened for antimicrobial activity. (wikipedia.org)
  • These academic compounds are screened against a key panel of drug-resistant bacterial strains -superbugs. (wikipedia.org)
  • rational drug d
  • The strategy behind rational drug design is to develop a new drug that is capable of affecting a specific biological target, or in this case a special neural site of action (uptake pumps, receptors), while trying to avoid effects on other site of actions. (wikipedia.org)
  • inhibitors
  • Monoamine oxidase inhibitors (MAOIs) and tricyclic antidepressants (TCAs) were the first drugs to be developed for the treatment of depression, dating back to the early 1950s. (wikipedia.org)
  • novel
  • All the data and resources generated by the community are openly shared through a web based portal called Sysborg 2.0 specifically designed for this purpose The project has a healthcare model that blends together the policies of patenting and open source research, aiming to make novel drugs available as generic drugs, without Intellectual Property restrictions, and thus ensure affordability and accessibility. (wikipedia.org)
  • Multi-drug resistant microbes are a serious health treat, and exploration of novel chemical diversity is essential to find new antibiotics. (wikipedia.org)
  • Examples
  • Examples of GABAA PAMs include alcohol (ethanol), benzodiazepines such as diazepam (Valium) and alprazolam (Xanax), Z-drugs such as zolpidem (Ambien) and the barbiturate drugs. (wikipedia.org)
  • selective
  • Because of their undesirable adverse-effect profile and high potential for toxicity, due to their non-selective pharmacological effects, strict regiments were for taking the drugs which limited their use. (wikipedia.org)
  • LY-341,495 and MGS-0039 are drugs that act as a selective antagonist blocking both of the group II metabotropic glutamate receptors, mGluR2 and mGluR3. (wikipedia.org)
  • Strategies
  • Introduction of fluoxetine to the market is hailed as a miracle drug for the treatment of depression because it had fewer adverse effects, simpler dosing strategies and greater margin of safety when overdoses were consumed and thus it had better adherence, compared to the older antidepressants (TCAs and MAOIs). (wikipedia.org)
  • predict
  • Molecular docking is one of the most frequently used methods in structure-based drug design, due to its ability to predict the binding-conformation of small molecule ligands to the appropriate target binding site. (wikipedia.org)
  • adverse
  • Because of this, researchers looked for other alternatives with similar effectiveness but fewer adverse effects e.g. drugs that did not cause cardiac conduction abnormalities in overdoses or had the tendency to cause seizures, which led to the discovery of the SSRI drugs. (wikipedia.org)
  • biological
  • The idea that the effect of a drug in the human body is mediated by specific interactions of the drug molecule with biological macromolecules, (proteins or nucleic acids in most cases) led scientists to the conclusion that individual chemicals are required for the biological activity of the drug. (wikipedia.org)
  • platform
  • The CRDD web portal provides computer resources related to drug discovery on a single platform. (wikipedia.org)
  • CO-ADD is a community-driven solution to the superbug crisis problem providing chemists with: an open access antimicrobial drug discovery platform a low-barrier access to free antimicrobial screening a program to uncover and test chemical diversity sitting on chemists' shelves a communal knowledge base for antimicrobial discovery Resistance of bacteria to commonly used antibiotics is increasing and contributes significantly to patient morbidity and mortality. (wikipedia.org)
  • design
  • Characterisation of the binding behaviour plays an important role in rational design of drugs as well as to elucidate fundamental biochemical processes. (wikipedia.org)
  • community
  • CDD Public - a free database for fostering open collaboration containing over 3 million molecules accessible to everyone in the drug discovery community at large. (wikipedia.org)
  • Table
  • Since then the number of drugs in the SSRI class has become bigger and they are now six (fluoxetine, paroxetine, citalopram, escitalopram, sertraline and fluvoxamine), as demonstrated in table 1. (wikipedia.org)
  • Table 1 SSRI drugs used to treat depression. (wikipedia.org)
  • The following is a table with drugs organized by year of discovery. (wikipedia.org)
  • series
  • The discovery of leptin also is documented in a series of books including Fat: Fighting the Obesity Epidemic by Robert Pool, The Hungry Gene by Ellen Ruppel Shell, and Rethinking Thin: The New Science of Weight Loss and the Myths and Realities of Dieting by Gina Kolata. (wikipedia.org)
  • public
  • Discovering drugs that may be a commercial success, or a public health success, involves a complex interaction between investors, industry, academia, patent laws, regulatory exclusivity, marketing and the need to balance secrecy with communication. (wikipedia.org)
  • New drugs being developed will be in public domain. (wikipedia.org)
  • health
  • On World Health Day 2011, themed 'combating antimicrobial resistance', WHO issued an international call for concerted action to halt the spread of antimicrobial resistance, launching a six-point policy package, recommended for governments, which sets out the measures governments and their national partners need to combat drug resistance. (wikipedia.org)
  • role
  • SSRIs were the first drugs to establish beyond doubt a pathophysiological role for 5-HT in affective illnesses and in the broad spectrum of anxiety disorders. (wikipedia.org)
  • significant
  • Because these drugs have already passed significant safety tests, the risk of failure is reduced and, if pharmaceuticals are found to be effective in Alzheimer's patients, they can be brought more rapidly to market. (wikipedia.org)
  • serve
  • Although barbiturates fell out of favor, they continue to serve as a short-acting anesthetic and anti-epileptic drugs. (wikipedia.org)
  • medicinal chemistry
  • Modern drug discovery involves the identification of screening hits, medicinal chemistry and optimization of those hits to increase the affinity, selectivity (to reduce the potential of side effects), efficacy/potency, metabolic stability (to increase the half-life), and oral bioavailability. (wikipedia.org)
  • The Drug Discovery Series covers all aspects of drug discovery and medicinal chemistry and contains over sixty books published since 2010. (rsc.org)
  • Dr Stevan Djuric is head of the global AbbVie Medicinal Chemistry Leadership Team at Abbott and is also responsible for the Discovery Chemistry and Technology organization within their Discovery organization and chemistry outsourcing activities. (smi-online.co.uk)
  • Network with industry experts, gain insight into the latest technological developments and how these are being utilised within the pharmaceutical industry, discuss the potential of novel drug modalities, the use of AI in drug discovery and the latest medicinal chemistry techniques and how these can be brought into the commercial market. (smi-online.co.uk)
  • Discuss latest advances in medicinal chemistry techniques and how these can be implemented in the commercial space of drug discovery. (smi-online.co.uk)
  • assays
  • Expert authors have developed and utilized these in vitro assays to achieve "drug-like" characteristics in addition to efficacy properties and good safety profiles of drug candidates. (springer.com)
  • Drug Discovery and Evaluation:Pharmacological Assays bridges this gap by comprehensively covering the pharmacological methods that have been utilized successfully for more than a hundred years as well as the latest technologies. (springer.com)
  • The 3rd edition of this successful reference book contains an updated selection of the most frequently used assays for reliably detecting the pharmacological effects of potential drugs. (springer.com)
  • The Penn Center for Molecular Discovery (PCMD) is one of nine centers participating in the NIH Molecular Libraries Screening Centers Network (MLSCN) to screen the NIH repository for biological activity in assays submitted by scientists around the country. (upenn.edu)
  • Pharmaceuticals
  • Because these drugs have already passed significant safety tests, the risk of failure is reduced and, if pharmaceuticals are found to be effective in Alzheimer's patients, they can be brought more rapidly to market. (wikipedia.org)
  • biotech
  • This provocative meeting is intended to bring together all those concerned about drug discovery (academia, industry, biotech, funders, charities and patient groups) to openly debate the bottlenecks that are hindering innovation and generation of tangible results. (rsc.org)
  • molecule
  • The idea that the effect of a drug in the human body is mediated by specific interactions of the drug molecule with biological macromolecules, (proteins or nucleic acids in most cases) led scientists to the conclusion that individual chemicals are required for the biological activity of the drug. (wikipedia.org)
  • The rest of a cell's internal machinery has been depicted as floating awash in the cytoplasm, with proteins occasionally running into binding partners, substrates and small-molecule drugs. (nature.com)
  • Molecular docking is one of the most frequently used methods in structure-based drug design, due to its ability to predict the binding-conformation of small molecule ligands to the appropriate target binding site. (wikipedia.org)
  • pharmaceutical
  • Modern drug discovery is thus usually a capital-intensive process that involves large investments by pharmaceutical industry corporations as well as national governments (who provide grants and loan guarantees). (wikipedia.org)
  • Drug discovery is done by pharmaceutical companies, with research assistance from universities. (wikipedia.org)
  • The generic drugs will be taken up by pharmaceutical companies so that the drug will be commercialised at reasonable price. (wikipedia.org)
  • After initial ADDF funding, grantees have received commitments of over $2 billion in follow-on funding from government, pharmaceutical companies and venture capital firms to further advance drug research. (wikipedia.org)
  • rational
  • This will assist rational, fast and successful drug discovery. (smi-online.co.uk)
  • The strategy behind rational drug design is to develop a new drug that is capable of affecting a specific biological target, or in this case a special neural site of action (uptake pumps, receptors), while trying to avoid effects on other site of actions. (wikipedia.org)
  • Characterisation of the binding behaviour plays an important role in rational design of drugs as well as to elucidate fundamental biochemical processes. (wikipedia.org)
  • receptors
  • LY-341,495 and MGS-0039 are drugs that act as a selective antagonist blocking both of the group II metabotropic glutamate receptors, mGluR2 and mGluR3. (wikipedia.org)
  • The GABAA receptors have historically been a target of drug treatment research. (wikipedia.org)
  • academia
  • Discovering drugs that may be a commercial success, or a public health success, involves a complex interaction between investors, industry, academia, patent laws, regulatory exclusivity, marketing and the need to balance secrecy with communication. (wikipedia.org)
  • inhibition
  • An initial success was achieved when medicinal chemists set out in search of the ideal SSRI with the chemical synthesis of zimelidine (figure 1) from the antihistamine drug brompheniramine, which exhibited selective inhibition of 5-HT re-uptake with minimal inhibition of norepinephrine (NE) re-uptake. (wikipedia.org)
  • chemists
  • CO-ADD is a community-driven solution to the superbug crisis problem providing chemists with: an open access antimicrobial drug discovery platform a low-barrier access to free antimicrobial screening a program to uncover and test chemical diversity sitting on chemists' shelves a communal knowledge base for antimicrobial discovery Resistance of bacteria to commonly used antibiotics is increasing and contributes significantly to patient morbidity and mortality. (wikipedia.org)
  • effectiveness
  • Because of this, researchers looked for other alternatives with similar effectiveness but fewer adverse effects e.g. drugs that did not cause cardiac conduction abnormalities in overdoses or had the tendency to cause seizures, which led to the discovery of the SSRI drugs. (wikipedia.org)
  • Methods
  • Based at Stevenage, his group specialises in the application of molecular design, data analysis, predictive modelling and chemoinformatics methods to drug discovery. (smi-online.co.uk)
  • researchers
  • Our unique resources, dedicated researchers and international partners create an ideal context for drug discovery that drives our search for revolutionary new treatments. (edu.au)
  • resistance
  • On World Health Day 2011, themed 'combating antimicrobial resistance', WHO issued an international call for concerted action to halt the spread of antimicrobial resistance, launching a six-point policy package, recommended for governments, which sets out the measures governments and their national partners need to combat drug resistance. (wikipedia.org)
  • metabolism
  • This led to great success, such as the work of Gertrude Elion and George H. Hitchings on purine metabolism, the work of James Black on beta blockers and cimetidine, and the discovery of statins by Akira Endo. (wikipedia.org)
  • proteins
  • Transient liquid-like droplets made up of proteins and RNA are scattered throughout the cell - with potentially broad drug discovery implications. (nature.com)
  • gene
  • The discovery of leptin also is documented in a series of books including Fat: Fighting the Obesity Epidemic by Robert Pool, The Hungry Gene by Ellen Ruppel Shell, and Rethinking Thin: The New Science of Weight Loss and the Myths and Realities of Dieting by Gina Kolata. (wikipedia.org)