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      Prescribed drugs containing nitrogen heterocycles: an overview

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      Author(s): ,
      Publication date (Electronic, pub):
      Publication date (Electronic, collection):
      Journal: RSC Advances
      Publisher: The Royal Society of Chemistry

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          Abstract

          Heteroatoms as well as heterocyclic scaffolds are frequently present as the common cores in a plethora of active pharmaceuticals natural products. Statistically, more than 85% of all biologically active compounds are heterocycles or comprise a heterocycle and most frequently, nitrogen heterocycles as a backbone in their complex structures. These facts disclose and emphasize the vital role of heterocycles in modern drug design and drug discovery. In this review, we try to present a comprehensive overview of top prescribed drugs containing nitrogen heterocycles, describing their pharmacological properties, medical applications and their selected synthetic pathways. It is worth mentioning that the reported examples are actually limited to current top selling drugs, being or containing N-heterocycles and their synthetic information has been extracted from both scientific journals and the wider patent literature.

          Abstract

          In this review, we try to present a comprehensive overview on top prescribed drugs containing nitrogen heterocycles, describing their pharmacological properties, medical applications and their selected synthetic pathways.

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          Analysis of the structural diversity, substitution patterns, and frequency of nitrogen heterocycles among U.S. FDA approved pharmaceuticals.

          Edon Vitaku, David Smith, Jon Njardarson (2014)
          Nitrogen heterocycles are among the most significant structural components of pharmaceuticals. Analysis of our database of U.S. FDA approved drugs reveals that 59% of unique small-molecule drugs contain a nitrogen heterocycle. In this review we report on the top 25 most commonly utilized nitrogen heterocycles found in pharmaceuticals. The main part of our analysis is divided into seven sections: (1) three- and four-membered heterocycles, (2) five-, (3) six-, and (4) seven- and eight-membered heterocycles, as well as (5) fused, (6) bridged bicyclic, and (7) macrocyclic nitrogen heterocycles. Each section reveals the top nitrogen heterocyclic structures and their relative impact for that ring type. For the most commonly used nitrogen heterocycles, we report detailed substitution patterns, highlight common architectural cores, and discuss unusual or rare structures.
          Article 0 comments Cited 705 times – based on 0 reviews     Review now
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            European guideline for the diagnosis and treatment of insomnia

            Elisabeth Hertenstein, Colin Espie, Jason Ellis … (2017)
            This European guideline for the diagnosis and treatment of insomnia was developed by a task force of the European Sleep Research Society, with the aim of providing clinical recommendations for the management of adult patients with insomnia. The guideline is based on a systematic review of relevant meta-analyses published till June 2016. The target audience for this guideline includes all clinicians involved in the management of insomnia, and the target patient population includes adults with chronic insomnia disorder. The GRADE (Grading of Recommendations Assessment, Development and Evaluation) system was used to grade the evidence and guide recommendations. The diagnostic procedure for insomnia, and its co-morbidities, should include a clinical interview consisting of a sleep history (sleep habits, sleep environment, work schedules, circadian factors), the use of sleep questionnaires and sleep diaries, questions about somatic and mental health, a physical examination and additional measures if indicated (i.e. blood tests, electrocardiogram, electroencephalogram; strong recommendation, moderate- to high-quality evidence). Polysomnography can be used to evaluate other sleep disorders if suspected (i.e. periodic limb movement disorder, sleep-related breathing disorders), in treatment-resistant insomnia, for professional at-risk populations and when substantial sleep state misperception is suspected (strong recommendation, high-quality evidence). Cognitive behavioural therapy for insomnia is recommended as the first-line treatment for chronic insomnia in adults of any age (strong recommendation, high-quality evidence). A pharmacological intervention can be offered if cognitive behavioural therapy for insomnia is not sufficiently effective or not available. Benzodiazepines, benzodiazepine receptor agonists and some antidepressants are effective in the short-term treatment of insomnia (≤4 weeks; weak recommendation, moderate-quality evidence). Antihistamines, antipsychotics, melatonin and phytotherapeutics are not recommended for insomnia treatment (strong to weak recommendations, low- to very-low-quality evidence). Light therapy and exercise need to be further evaluated to judge their usefulness in the treatment of insomnia (weak recommendation, low-quality evidence). Complementary and alternative treatments (e.g. homeopathy, acupuncture) are not recommended for insomnia treatment (weak recommendation, very-low-quality evidence).
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              Management of Chronic Insomnia Disorder in Adults: A Clinical Practice Guideline From the American College of Physicians.

              Amir Qaseem, Devan Kansagara, Mary Forciea … (2016)
              The American College of Physicians (ACP) developed this guideline to present the evidence and provide clinical recommendations on the management of chronic insomnia disorder in adults.
              Article 0 comments Cited 371 times – based on 0 reviews     Review now
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                Author and article information

                Journal
                Journal ID (nlm-ta): RSC Adv
                Journal ID (iso-abbrev): RSC Adv
                Journal ID (publisher-id): RA
                Journal ID (coden): RSCACL
                Title: RSC Advances
                Publisher: The Royal Society of Chemistry
                ISSN (Electronic): 2046-2069
                Publication date (Electronic, pub): 15 December 2020
                Publication date (Electronic, collection): 9 December 2020
                Publication date PMC-release: 15 December 2020
                Volume: 10
                Issue: 72
                Pages: 44247-44311
                Affiliations
                [a] Department of Chemistry, School of Science, Alzahra University PO Box 1993891176, Vanak Tehran Iran mmh1331@ 123456yahoo.com mmheravi@ 123456alzahra.ac.ir +98 21 88041344 +98 21 88044051
                Author information
                https://orcid.org/0000-0003-2978-1157
                Article
                Publisher ID: d0ra09198g
                DOI: 10.1039/d0ra09198g
                PMC ID: 9092475
                PubMed ID: 35557843
                SO-VID: ca390769-4f88-422e-97a4-fca9301b837f
                Copyright © This journal is © The Royal Society of Chemistry
                History
                Date received : 28 October 2020
                Date accepted : 23 November 2020
                Page count
                Pages: 65
                Funding
                Funded by: Alzahra University, doi 10.13039/501100012310;
                Award ID: Unassigned
                Funded by: Iran National Science Foundation, doi 10.13039/501100003968;
                Award ID: Unassigned
                Categories
                Subject: Chemistry
                Custom metadata
                pubstatus Paginated Article

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