Literature DB >> 28523114

Design of Phthalazinone Amide Histamine H1 Receptor Antagonists for Use in Rhinitis.

Panayiotis A Procopiou1, Alison J Ford1, Paul M Gore1, Brian E Looker1, Simon T Hodgson1, Duncan S Holmes1, Sadie Vile1, Kenneth L Clark1, Ken A Saunders1, Robert J Slack1, James E Rowedder1, Clarissa J Watts1.   

Abstract

The synthesis of potent amide-containing phthalazinone H1 histamine receptor antagonists is described. Three analogues 3e, 3g, and 9g were equipotent with azelastine and were longer-acting in vitro. Amide 3g had low oral bioavailability, low brain-penetration, high metabolic clearance, and long duration of action in vivo, and it was suitable for once-daily dosing intranasally, with a predicted dose for humans of approximately 0.5 mg per day.

Entities:  

Keywords:  Histamine H1 receptor antagonist; allergic rhinitis; once-daily dosing; phthalazinone; topical application

Year:  2017        PMID： 28523114      PMCID： PMC5430406          DOI： 10.1021/acsmedchemlett.7b00112

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.345


  17 in total

Review 1.  Measurement of [Ca2+] using the Fluorometric Imaging Plate Reader (FLIPR).

Authors:  E Sullivan; E M Tucker; I L Dale
Journal:  Methods Mol Biol       Date:  1999

Review 2.  Allergic rhinitis and its impact on asthma.

Authors:  J Bousquet; P Van Cauwenberge; N Khaltaev
Journal:  J Allergy Clin Immunol       Date:  2001-11       Impact factor: 10.793

Review 3.  Histamine and H1-antihistamines: celebrating a century of progress.

Authors:  F Estelle R Simons; Keith J Simons
Journal:  J Allergy Clin Immunol       Date:  2011-10-27       Impact factor: 10.793

4.  Discovery of 4-substituted-8-(2-hydroxy-2-phenyl-cyclohexyl)-2,8-diaza-spiro[4.5]decan-1-one as a novel class of highly selective GlyT1 inhibitors with improved metabolic stability.

Authors:  Daniela Alberati; Dominik Hainzl; Synèse Jolidon; Eva A Krafft; Anke Kurt; Axel Maier; Emmanuel Pinard; Andrew W Thomas; Daniel Zimmerli
Journal:  Bioorg Med Chem Lett       Date:  2006-06-06       Impact factor: 2.823

Review 5.  Review of azelastine nasal spray in the treatment of allergic and non-allergic rhinitis.

Authors:  Christina Lee; Jonathan Corren
Journal:  Expert Opin Pharmacother       Date:  2007-04       Impact factor: 3.889

Review 6.  Selecting the optimal oral antihistamine for patients with allergic rhinitis.

Authors:  Jeffrey M Lehman; Michael S Blaiss
Journal:  Drugs       Date:  2006       Impact factor: 9.546

Review 7.  Allergic rhinitis: an update on disease, present treatments and future prospects.

Authors:  Sanjay N Mandhane; Jigar H Shah; Rajamannar Thennati
Journal:  Int Immunopharmacol       Date:  2011-07-23       Impact factor: 4.932

Review 8.  Allergic rhinitis.

Authors:  Alexander N Greiner; Peter W Hellings; Guiseppina Rotiroti; Glenis K Scadding
Journal:  Lancet       Date:  2011-07-23       Impact factor: 79.321

Review 9.  Azelastine hydrochloride: a review of pharmacology, pharmacokinetics, clinical efficacy and tolerability.

Authors:  Jonathan A Bernstein
Journal:  Curr Med Res Opin       Date:  2007-10       Impact factor: 2.580

10.  4-acyl-1-(4-aminoalkoxyphenyl)-2-ketopiperazines as a novel class of non-brain-penetrant histamine H3 receptor antagonists.

Authors:  Panayiotis A Procopiou; Rachael A Ancliff; Mark J Bamford; Christopher Browning; Helen Connor; Susannah Davies; Yvonne C Fogden; Simon T Hodgson; Duncan S Holmes; Brian E Looker; Karen M L Morriss; Christopher A Parr; Elizabeth A Pickup; Sanjeet S Sehmi; Gemma V White; Clarissa J Watts; David M Wilson; Michael D Woodrow
Journal:  J Med Chem       Date:  2007-12-06       Impact factor: 7.446
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  4 in total

1.  The Multidirectional Effect of Azelastine Hydrochloride on Cervical Cancer Cells.

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Journal:  Int J Mol Sci       Date:  2022-05-24       Impact factor: 6.208

2.  Amino- and polyaminophthalazin-1(2H)-ones: synthesis, coordination properties, and biological activity.

Authors:  Zbigniew Malinowski; Emilia Fornal; Agata Sumara; Renata Kontek; Karol Bukowski; Beata Pasternak; Dariusz Sroczyński; Joachim Kusz; Magdalena Małecka; Monika Nowak
Journal:  Beilstein J Org Chem       Date:  2021-02-25       Impact factor: 2.883

Review 3.  Synthesis of anti-allergic drugs.

Authors:  Shiyang Zhou; Gangliang Huang
Journal:  RSC Adv       Date:  2020-02-04       Impact factor: 4.036

4.  Turkish Guideline for Diagnosis and Treatment of Allergic Rhinitis (ART).

Authors:  Mustafa Cenk Ecevit; Müge Özcan; İlknur Haberal Can; Emel Çadallı Tatar; Serdar Özer; Erkan Esen; Doğan Atan; Sercan Göde; Çağdaş Elsürer; Aylin Eryılmaz; Berna Uslu Coşkun; Zahide Mine Yazıcı; Mehmet Emre Dinç; Fatih Özdoğan; Kıvanç Günhan; Nagihan Bilal; Arzu Yasemin Korkut; Fikret Kasapoğlu; Bilge Türk; Ela Araz Server; Özlem Önerci Çelebi; Tuğçe Şimşek; Rauf Oğuzhan Kum; Mustafa Kemal Adalı; Erdem Eren; Nesibe Gül Yüksel Aslıer; Tuba Bayındır; Aslı Çakır Çetin; Ayşe Enise Göker; Işıl Adadan Güvenç; Sabri Köseoğlu; Gül Soylu Özler; Ethem Şahin; Aslı Şahin Yılmaz; Ceren Güne; Gökçe Aksoy Yıldırım; Bülent Öca; Mehmet Durmuşoğlu; Yunus Kantekin; Süay Özmen; Gözde Orhan Kubat; Serap Köybaşı Şanal; Emine Elif Altuntaş; Adin Selçuk; Haşmet Yazıcı; Deniz Baklacı; Atılay Yaylacı; Deniz Hancı; Sedat Doğan; Vural Fidan; Kemal Uygur; Nesil Keleş; Cemal Cingi; Bülent Topuz; Salih Çanakçıoğlu; Metin Önerci
Journal:  Turk Arch Otorhinolaryngol       Date:  2021-05
  4 in total

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