Design, synthesis, and evaluation of the anticonvulsant and antidepressant activities of pyrido[2,3-d]pyrimidine derivatives

Zhang, Hongjian; Wang, Shi‐Ben; Wen, Xiang; Li, Jin-Zi; Quan, Zhe‐Shan

doi:10.1007/s00044-016-1559-1

Cited by 36 publications

(17 citation statements)

References 26 publications

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“…By affecting the hydrogen bonding ability, polarity and lipophilicity of the molecules, the triazole moiety can improve the physicochemical properties, toxicology, pharmacokinetics and pharmacology of the compounds 11 , 12 . The synthetic moieties containing these molecular structures have been used extensively in the discovery of drugs due to their low occurrence in nature 13 .Meanwhile, on the basis of the literature, triazole and its derivatives have aroused enormous interest owing to their pharmaceutical and therapeutic applications, including their use as anticonvulsant 14–17 , antidepressant 18 , anticancer 19–23 , antiviral 24 , antimicrobial 25–33 , anti-acetylcholinesterase 34 , anti-inflammatory 35 , 36 , antioxidant 37–40 , antiparasitic 41–43 , and anti-diabetic drugs 44 . Their ability to produce various non-covalent interactions to improve solubility and binding to bimolecular targets may be the reason for this wide applicability 45 .…”

Section: Introductionmentioning

confidence: 99%

Application of triazoles in the structural modification of natural products

Guo

Zheng-ai

Shen

et al. 2021

Journal of Enzyme Inhibition and Medicinal Chemistry

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Nature products have been extensively used in the discovery and development of new drugs, as the most important source of drugs. The triazole ring is one of main pharmacophore of the nitrogen-containing heterocycles. Thus, a new class of triazole-containing natural product conjugates has been synthesised. These compounds reportedly exert anticancer, anti-inflammatory, antimicrobial, antiparasitic, antiviral, antioxidant, anti-Alzheimer, and enzyme inhibitory effects. This review summarises the research progress of triazole-containing natural product derivatives involved in medicinal chemistry in the past six years. This review provides insights and perspectives that will help scientists in the fields of organic synthesis, medicinal chemistry, phytochemistry, and pharmacology.

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Section: Introductionmentioning

confidence: 99%

Application of triazoles in the structural modification of natural products

Guo

Zheng-ai

Shen

et al. 2021

Journal of Enzyme Inhibition and Medicinal Chemistry

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“…34 ) were synthesized as anticonvulsant agents by Zhang et al. [ 142 , 143 ]. Based on the anticonvulsant and neurotoxicity screening data, compounds 157a and 157b showed wide margins of safety with PI value of >25.5 and > 26.0, and significant oral activity against MES-induced seizures in mice with an ED 50 of 88.0 and 94.6 mg/kg, respectively.…”

Section: Biological Activities Of 124-triazole Derivativesmentioning

confidence: 99%

An insight on medicinal attributes of 1,2,4-triazoles

Aggarwal

Sumran²

2020

European Journal of Medicinal Chemistry

214

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The present review aims to summarize the pharmacological profile of 1,2,4-triazole, one of the emerging privileged scaffold, as antifungal, antibacterial, anticancer, anticonvulsant, antituberculosis, antiviral, antiparasitic, analgesic and anti-inflammatory agents, etc. along with structure-activity relationship. The comprehensive compilation of work carried out in the last decade on 1,2,4-triazole nucleus will provide inevitable scope for researchers for the advancement of novel potential drug candidates having better efficacy and selectivity.

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“…Moreover, their structure-activity relationship (SAR) was investigated. Pyrido-pyrimidines have, for a long time, attracted the interests of both biological and synthetic researchers alike due to their various biological therapeutic properties such as anticonvulsant [14], antitumor [15], anti-proliferative [16], antifungal [17], adenosine kinase inhibition [18] and cytotoxic activities (Figure 1E-G) [19,20].…”

Section: Introductionmentioning

confidence: 99%

Synthesis and In Silico Docking of New Pyrazolo[4,3-e]pyrido[1,2-a]pyrimidine-based Cytotoxic Agents

Horchani

Heise

Hoenke

et al. 2021

IJMS

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To explore a new set of anticancer agents, a novel series of pyrazolo[4,3-e]pyrido[1,2-a]pyrimidine derivativeshave been designed and synthesized viacyclocondensation reactions of pyrazolo-enaminone with a series of arylidenemalononitriles; compound 5 was obtained from 5-amino-4-cyanopyrazole. The structures of the target compounds were investigated by spectral techniques and elemental analysis (IR, UV–Vis, 1H NMR, 13C NMR and ESI-MS). All compounds were evaluated for their in vitro cytotoxicity employing a panel of different human tumor cell lines, A375, HT29, MCF7, A2780, FaDu as well as non-malignant NIH 3T3 and HEK293 cells. It has been found that the pyrazolo-pyrido-pyrimidine analog bearing a 4-Br-phenyl moiety was the most active toward many cell lines with EC50 values ranging between 9.1 and 13.5 µM. Moreover, in silico docking studies of the latter with six anticancer drug targets, i.e., DHFR, VEGFR2, HER-2/neu, hCA-IX, CDK6 and LOX5, were also performed, in order to gain some insights into their putative mode of binding interaction and to estimate the free binding energy of this bioactive molecule.

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Design, synthesis, and evaluation of the anticonvulsant and antidepressant activities of pyrido[2,3-d]pyrimidine derivatives

Cited by 36 publications

References 26 publications

Application of triazoles in the structural modification of natural products

Application of triazoles in the structural modification of natural products

An insight on medicinal attributes of 1,2,4-triazoles

Synthesis and In Silico Docking of New Pyrazolo[4,3-e]pyrido[1,2-a]pyrimidine-based Cytotoxic Agents

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