Synthesis and evaluation of anticonvulsant and antidepressant activities of 7-alkyl-7H-tetrazolo[1,5-g]purine derivatives

Wang, Shi‐Ben; Deng, Xian‐Qing; Liu, Dachuan; Zhang, Hongjian; Quan, Zhe‐Shan

doi:10.1007/s00044-014-1030-0

Cited by 14 publications

(5 citation statements)

References 21 publications

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“…Wang et al synthesized seventeen 7‐alkyl‐7H‐tetrazolo[1,5‐g]purine derivatives ( 13a–q ) and evaluated their anticonvulsant and antidepressant behaviors in animal models [108]. Compared to the reference drug carbamazepine, compound 13h (Figure 17) was found to be the most efficient with a median effective dose (ED 50 ) of 28.9 mg/kg and a protective index value of 15.8.…”

Section: Recent Developments Of Pyrimidine Derivatives (2016–2021)mentioning

confidence: 99%

An insight on medicinal attributes of pyrimidine scaffold: An updated review

Vyas

Sahu

Pathania

et al. 2022

Journal of Heterocyclic Chem

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Pyrimidine itself or in different fused forms is an important chemical motif for every step of cell life. Alongside, it exists as a key pharmacophoric part in thiamine, alloxan, orotic acid, and other isoforms of nucleotide bases. It has emerged as a privileged scaffold in medicinal chemistry due to its various possible structural and pharmacological attributes. In a number of clinically used chemical agents, pyrimidine or its fused/clubbed form with other moieties act as a key pharmacophore. Structure activity relationship (SAR) studies of the explored derivatives demonstrated that slight modifications with various substitutions on the pyrimidine rings can deviate biological activity to a large extent. 2-Pyrimidone and 2,4-pyrimidione derivatives are largely explored by a number of research groups for various pharmacological targets and due to their similarity to nucleotide bases, it has a great impact on the biological profile of these molecules. The current review focuses on describing the recent advancements (2015 onward) in the development of pyrimidine-based biologically active molecules along with drug candidates under different clinical trials. The aim of this review is to provide structural features associated with pyrimidine along with their SAR studies, which are believed to be valuable for the scientists working on the development of pyrimidine-based small molecules in the aforementioned disease conditions. We believe that the results of this research will help to provide a structural idea that may be used in the design and development of new pyrimidine-based small molecules that target a variety of receptors or enzymes.

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Section: Recent Developments Of Pyrimidine Derivatives (2016–2021)mentioning

confidence: 99%

An insight on medicinal attributes of pyrimidine scaffold: An updated review

Vyas

Sahu

Pathania

et al. 2022

Journal of Heterocyclic Chem

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show abstract

“…For many years, these purine scaffolds have been exploited as terminal fragments with the long-chain aryl piperazines (LCAPs) for the design and development of novel purine-based antidepressants [ 122 ]. Purine derivatives possess diverse pharmacological activities [ 123 , 124 ], and recent findings show that purine clubbed piperazine derivatives display promising antidepressant profile [ 124 - 126 ].…”

Section: Various Classes Of Multi-target Directed Ligands Against Dep...mentioning

confidence: 99%

“…1,3-Dimethyl-purine-2,6-dione scaffold showed good binding affinities towards the 5-HT 1A , 5-HT 2A , 5-HT 7 and 5-HT 6 [ 124 ] receptors. LCAPs have been reported to possess good binding affinities for 5-HT 1A , 5-HT 2A, 5-HT 7 and 5-HT 6 receptors [ 127 - 129 ].…”

Section: Various Classes Of Multi-target Directed Ligands Against Dep...mentioning

confidence: 99%

Design Strategies, Chemistry and Therapeutic Insights of Multi-target Directed Ligands as Antidepressant Agents

Singh

Bhatia

Kumar

et al. 2022

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: Depression is one of the major disorders of the central nervous system worldwide and causes disability and functional impairment. According to the World Health Organization, around 265 million people worldwide are affected by depression. Currently marketed antidepressant drugs take weeks or even months to show anticipated clinical efficacy but remain ineffective in treating suicidal thoughts and cognitive impairment. Due to its multifactorial complexity, single-target drugs did not always produce satisfactory results and lacks the desired level of therapeutic efficacy. Recent literature reports revealed improved therapeutic potential of multi-target directed ligands due to their synergistic potency and better safety. Medicinal chemists have gone to great extents for the design of multi-target ligands by generating structural hybrids of different key pharmacophores with improved binding affinities and potency towards different receptors or enzymes. This article compiled the design strategies of recently published multi-target directed ligands as antidepressant agents. Their biological evaluation, structural-activity relationships, mechanistic and in silico studies were also described. This article will be highly useful for the researchers to design and develop multi-target ligands as antidepressants with high potency and therapeutic efficacy.

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“…Phthalazine and benzo[g]phthalazine derivatives [1] are nitrogen heterocyclic compounds that showed various biological activities, such as antimicrobial, [2] anti-inflammatory, [3] anticonvulsant, [4] leishmanicidal, [5] antibacterial, [6] and anticancer [7] [8] and inhibitory effect to parasites. [9,10] Also, they act as ligands for a variety of transition metals which have been used in chemosensor materials.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Antimicrobial Evaluation of New 5-Amino-2,3-dihydrophthalazine-1,4-dione Derivatives

Ewies

El‐Hussieny²,

El‐Sayed

et al. 2021

Egypt. J. Chem.

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5-Amino-2,3-dihydrophthalazine-1,4-dione (Luminol 1) reacted with some organophosphorus reagents such as phosphonium ylides, trialkyl phosphites, and tris(dialkylamino)phosphines to afford the corresponding olefinic products 5a-e, alkoxy-, and dialkylamino derivatives of Luminol 6a-e. 4-Thioxo-3,4-dihydrophthalazin-1(2H)-one derivative 7 was synthesized from the reaction of Luminol (1) with thiating Lawesson and Japanese reagents. Structures of the synthesized compounds were clarified based on their elemental and spectroscopic analyses. The synthesized compounds were evaluated for their antimicrobial activity against some bacterial and fungal strains.

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Synthesis and evaluation of anticonvulsant and antidepressant activities of 7-alkyl-7H-tetrazolo[1,5-g]purine derivatives

Cited by 14 publications

References 21 publications

An insight on medicinal attributes of pyrimidine scaffold: An updated review

An insight on medicinal attributes of pyrimidine scaffold: An updated review

Design Strategies, Chemistry and Therapeutic Insights of Multi-target Directed Ligands as Antidepressant Agents

Synthesis and Antimicrobial Evaluation of New 5-Amino-2,3-dihydrophthalazine-1,4-dione Derivatives

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