Novel 8-(furan-2-yl)-3-substituted thiazolo [5,4-e][1,2,4] triazolo[1,5-c] pyrimidine-2(3H)-thione derivatives as potential adenosine A2A receptor antagonists

Mishra, Chandra Bhushan; Barodia, Sandeep Kumar; Prakash, Amresh; Kumar, J.B. Senthil; Luthra, Pratibha Mehta

doi:10.1016/j.bmc.2010.02.048

Cited by 28 publications

(10 citation statements)

References 30 publications

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“…Check the effects on the model of treatments already established for parkinsonism 22 1982 and 2020 (Kiselev et al, 2019;Ardayfio et al, 2010;Fink-Jensen et al, 2011;Goudet et al, 2012;González-Lugo et al, 2010;Ionov & Pushinskaya, 2013;Klein & Schmidt, 2003;Meissner et al, 2011;Ionov et al, 2012b;De Ryck & Teitelbaum, 1984;Sanberg et al, 1988;Wardas Pietraszek & Dziedzicka-Wasylewska, 2003;Tonelli et al, 2017;Mishra et al, 2010;Tysnes & Storstein, 2017;Hodgson et al, 2009;Moo-Puc et al, 2003;Nade et al, 2015;McAllister, 1996;Himori et al, 1994;Kobayashi, 1997;Pires et al, 2005) Explore the effects of potential new treatments for parkinsonism 149 1981 and 2020 (Trevitt et al, 2009;Maj et al, 1990;Juszkiewicz et al, 1994;Juszkiewicz et al, 1995;Mandhane et al, 1997;Konieczny et al, 1999;Jagtap & Inamdar, 2001;Ossowska et al, 2001;Breysse et al, 2002;Moo-Puc et al, 2003;Ossowska et al, 2003;Rukoyatkina et al, 2003;Wardas et al, 2003;Tanganelli et al, 2004;Ossowska et al, 2005;…”

Section: First and Last Year Of Publication Referencesmentioning

confidence: 99%

Haloperidol‐induced catalepsy as an animal model for parkinsonism: A systematic review of experimental studies

Waku

Magalhães

Alves

et al. 2021

Eur J of Neuroscience

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Several useful animal models for parkinsonism have been developed so far. Haloperidol‐induced catalepsy is often used as a rodent model for the study of motor impairments observed in Parkinson's disease and related disorders and for the screening of potential antiparkinsonian compounds. The objective of this systematic review is to identify publications that used the haloperidol‐induced catalepsy model for parkinsonism and to explore the methodological characteristics and the main questions addressed in these studies. A careful systematic search of the literature was carried out by accessing articles in three different databases: Web of Science, PubMed and SCOPUS. The selection and inclusion of studies were performed based on the abstract and, subsequently, on full‐text analysis. Data extraction included the objective of the study, study design and outcome of interest. Two hundred and fifty‐five articles were included in the review. Publication years ranged from 1981 to 2020. Most studies used the model to explore the effects of potential treatments for parkinsonism. Although the methodological characteristics used are quite varied, most studies used Wistar rats as experimental subjects. The most frequent dose of haloperidol used was 1.0 mg/kg, and the horizontal bar test was the most used to assess catalepsy. The data presented here provide a framework for an evidence‐based approach to the design of preclinical research on parkinsonism using the haloperidol‐induced catalepsy model. This model has been used routinely and successfully and is likely to continue to play a critical role in the ongoing search for the next generation of therapeutic interventions for parkinsonism.

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Section: First and Last Year Of Publication Referencesmentioning

confidence: 99%

Haloperidol‐induced catalepsy as an animal model for parkinsonism: A systematic review of experimental studies

Waku

Magalhães

Alves

et al. 2021

Eur J of Neuroscience

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“…Very recently, benzofurans [74], 7-imino-2-thioxo-thiazolo[4,5- d ]pyrimidines [75] (e.g. 61 ) and the related thiazolotriazolopyrimidinethiones [76] (e.g. 62 ) have been described as new potent A 2A -selective AR antagonists.…”

Section: Adenosine Receptor Antagonistsmentioning

confidence: 99%

Recent developments in adenosine receptor ligands and their potential as novel drugs

Müller

Jacobson

2011

Biochimica et Biophysica Acta (BBA) - Biomembranes

397

461

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Medicinal chemical approaches have been applied to all four of the adenosine receptor (AR) subtypes (A1, A2A, A2B, and A3) to create selective agonists and antagonists for each. The most recent class of selective AR ligands to be reported is the class of A2BAR agonists. The availability of these selective ligands has facilitated research on therapeutic applications of modulating the ARs and in some cases has provided clinical candidates. Prodrug approaches have been developed which improve the bioavailability of the drugs, reduce side-effects, and/or may lead to site-selective effects. The A2A agonist regadenoson (Lexiscan®), a diagnostic drug for myocardial perfusion imaging, is the first selective AR agonist to be approved. Other selective agonists and antagonists are or were undergoing clinical trials for a broad range of indications, including capadenoson and tecadenoson (A1 agonists) for atrial fibrillation, or paroxysmal supraventricular tachycardia, respectively, apadenoson and binodenoson (A2A agonists) for myocardial perfusion imaging, preladenant (A2A antagonist) for the treatment of Parkinson’s disease, and CF101 and CF102 (A3 agonists) for inflammatory diseases and cancer, respectively. This article is part of a Special Issue entitled: “Adenosine Receptors”.

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“…Nevertheless, we recently demonstrated the importance of the pyrazole portion of the PTP nucleus in modulating selectivity . Other examples of PTP‐related A 2A antagonists resulted from the substitution of the pyrazole ring with a thiazole, such as in the thiazolo[5,4‐e][1,2,4]triazolo[1,5‐c]pyrimidine derivative labeled as PTTP ( 27 , Fig. ).…”

Section: Medicinal Chemistry Of A2a Antagonistsmentioning

confidence: 99%

History and Perspectives of A_2AAdenosine Receptor Antagonists as Potential Therapeutic Agents

Preti

Baraldi

Moorman³

et al. 2015

Med. Res. Rev.

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Growing evidence emphasizes that the purine nucleoside adenosine plays an active role as a local regulator in different pathologies. Adenosine is a ubiquitous nucleoside involved in various physiological and pathological functions by stimulating A1 , A2A , A2B , and A3 adenosine receptors (ARs). At the present time, the role of A2A ARs is well known in physiological conditions and in a variety of pathologies, including inflammatory tissue damage and neurodegenerative disorders. In particular, the use of selective A2A antagonists has been reported to be potentially useful in the treatment of Parkinson's disease (PD). In this review, A2A AR signal transduction pathways, together with an analysis of the structure-activity relationships of A2A antagonists, and their corresponding pharmacological roles and therapeutic potential have been presented. The initial results from an emerging polypharmacological approach are also analyzed. This approach is based on the optimization of the affinity and/or functional activity of the examined compounds toward multiple targets, such as A1 /A2A ARs and monoamine oxidase-B (MAO-B), both closely implicated in the pathogenesis of PD.

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Novel 8-(furan-2-yl)-3-substituted thiazolo [5,4-e][1,2,4] triazolo[1,5-c] pyrimidine-2(3H)-thione derivatives as potential adenosine A2A receptor antagonists

Cited by 28 publications

References 30 publications

Haloperidol‐induced catalepsy as an animal model for parkinsonism: A systematic review of experimental studies

Haloperidol‐induced catalepsy as an animal model for parkinsonism: A systematic review of experimental studies

Recent developments in adenosine receptor ligands and their potential as novel drugs

History and Perspectives of A_2AAdenosine Receptor Antagonists as Potential Therapeutic Agents

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Novel 8-(furan-2-yl)-3-substituted thiazolo [5,4-e][1,2,4] triazolo[1,5-c] pyrimidine-2(3H)-thione derivatives as potential adenosine A2A receptor antagonists

Cited by 28 publications

References 30 publications

Haloperidol‐induced catalepsy as an animal model for parkinsonism: A systematic review of experimental studies

Haloperidol‐induced catalepsy as an animal model for parkinsonism: A systematic review of experimental studies

Recent developments in adenosine receptor ligands and their potential as novel drugs

History and Perspectives of A2AAdenosine Receptor Antagonists as Potential Therapeutic Agents

Contact Info

Product

Resources

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History and Perspectives of A_2AAdenosine Receptor Antagonists as Potential Therapeutic Agents