Synthesis, characterization and in vitro antimicrobial activity of novel fused pyrazolo[3,4-c]pyridazine, pyrazolo[3,4-d]pyrimidine, thieno[3,2-c]pyrazole and pyrazolo[3′,4′:4,5]thieno[2,3-d]pyrimidine derivatives

Reheim, Mohamed Ahmed Mahmoud Abdel; Baker, Safaa M.

doi:10.1186/s13065-017-0339-4

Cited by 25 publications

(7 citation statements)

References 27 publications

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“…Abdel Reheim et al 79 reported that the reaction of diphenylpyrazolone 149 with cyanoacetic hydrazide and elemental sulfur in DMF containing a catalytic amount of piperidine yielded 5-amino-1,3-diphenyl-1Hthieno[3,2-c]pyrazole-6-carbohydrazide (150) (Scheme 45).…”

Section: Scheme 44mentioning

confidence: 99%

A concise review on synthesis, reactions and biological importance of thienopyrazoles

Zaki¹,

Saber²,

El‐Dean³

et al. 2020

Arkivoc

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Pyrazoles are five membered heterocycles constitute a higly significant class of compounds in organic synthesis. Nowadays, pyrazoles and condensed pyrazoles have attracted substantial attention of the scientists owing to their excellent pharmacological and agrochemical properties. Pyrazole derivatives exhibit a wide range of pharmacological effects such as: anticancer, antioxidant, anti-inflammatory, antipyretic, analgesic, antimicrobial, antidepressant, antiviral, antihypertensive, anti-glaucoma, anti-tubercular, sodium channel blocker, anxiolytic, neuroprotective and anti-diabetic activities. This review casts light on recent methodologies for the synthesis and reactions of thienopyrazole moiety. This follow-up may encourage scientists to create new routes towards the thienopyrazole nucleus with important biological activity.

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Section: Scheme 44mentioning

confidence: 99%

A concise review on synthesis, reactions and biological importance of thienopyrazoles

Zaki¹,

Saber²,

El‐Dean³

et al. 2020

Arkivoc

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“…After the publication of this work [ 1 ] it was noticed that on page 3 of the article beginning in the paragraph—‘Hydrazide 14 is used as a key producer…’ the compound—“Not ethyl- N ′-5-amino-1,3-diphenyl-1 H -thieno[3,2- c ]pyrazole-6-carbonylformohydrazonate” should be deleted. Also on page 10 of the PDF beginning in paragraph—‘Synthesis of 5-amino-…’ the compound—“Not ethyl- N ′-5-amino-1,3-diphenyl-1 H -thieno[3,2- c ]pyrazole-6-carbonylformohydrazonate” should be deleted.…”

Section: Correction To: Chemistry Central Journal (2017) 11:112 1011mentioning

confidence: 99%

Correction to: Synthesis, characterization and in vitro antimicrobial activity of novel fused pyrazolo[3,4-c]pyridazine, pyrazolo[3,4-d]pyrimidine, thieno[3,2-c] pyrazole and pyrazolo[3′,4′:4,5]thieno[2,3-d]pyrimidine derivatives

Reheim

Baker

2017

Chemistry Central Journal

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“…Celecoxib and lonazolac are used as anti-inflammatory drugs, fipronil acts as an insecticide, dipyrone is a promising analgesic and antipyretic molecule [ 8 ], and sildenafil is used for erectile dysfunction treatment, all of these drugs are pyrazole based compounds [ 9 ]. Fused-pyrazoles have been found to exhibit several biological properties like anti-inflammatory [ 10 ], anti-viral [ 11 ], anti-tumor [ 12 ], anti-microbial [ 13 ], and antiprotozoal [ 14 ]. In addition, many fused-pyrazoles have shown significant anti-human immunodeficiency virus (HIV) properties [ 15 ].…”

Section: Introductionmentioning

confidence: 99%

Inhibition of Glioma Cell Growth and Apoptosis Induction through Targeting Wnt10B Expression by Pyrazolo[4,3-c]pyridine-4-one

Zhu

Peng

et al. 2020

Med Sci Monit

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Background Gliomas are commonly diagnosed tumors in the central nervous system that have an elevated mortality rate. The present study evaluated pyrazolo[4,3-c]pyridine-4-one (PP-4-one) as an anti-proliferative agent against glioma cells and investigated the associated mechanism. Material/Methods The changes in cell growth were analyzed by Cell Counting Kit-8 (CCK-8) and apoptosis by flow cytometry using Annexin V-FITC staining kit. The FACSCalibur flow cytometer was used for analysis of DNA content and western blotting for protein expression. Results The PP-4-one treatment suppressed viability of U251, C6, and U87 cells significantly at a concentration of 0.25 μM. At a concentration of 16 μM, PP-4-one treatment for 72 hours suppressed viability of U251, C6, and U87 cells to 24%, 21%, and 20%, respectively. Treatment with PP-4-one suppressed cyclic 3′,5′-adenosine monophosphate (cAMP) levels in U251 and C6 cells significantly ( P <0.05) depending on the concentration. The apoptotic cells were increased significantly ( P <0.05) by PP-4-one treatment in U251 and C6 cell cultures. A considerable enhancement in the proportion of U251 and C6 cells in the G0/G1 phase was recorded on incubation with PP-4-one. Treatment of U251 and C6 cells with PP-4-one markedly enhanced p21 expression relative to the control. The B-cell lymphoma (Bcl-2) level in PP-4-one treated U251 and C6 cells was markedly lower relative to the control cells. The Bax, caspase-3, and caspase-9 levels were elevated markedly by PP-4-one treatment in U251 and C6 cells. Conclusions This study demonstrated that PP-4-one has anti-proliferative potential for glioma cells via targeting cAMP and Bcl-2 levels. It also promoted glioma cell apoptosis through caspase activation and arrest of the cell cycle. Thus, PP-4-one may be used to develop drug candidates for the glioma treatment.

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Synthesis, characterization and in vitro antimicrobial activity of novel fused pyrazolo[3,4-c]pyridazine, pyrazolo[3,4-d]pyrimidine, thieno[3,2-c]pyrazole and pyrazolo[3′,4′:4,5]thieno[2,3-d]pyrimidine derivatives

Cited by 25 publications

References 27 publications

A concise review on synthesis, reactions and biological importance of thienopyrazoles

A concise review on synthesis, reactions and biological importance of thienopyrazoles

Correction to: Synthesis, characterization and in vitro antimicrobial activity of novel fused pyrazolo[3,4-c]pyridazine, pyrazolo[3,4-d]pyrimidine, thieno[3,2-c] pyrazole and pyrazolo[3′,4′:4,5]thieno[2,3-d]pyrimidine derivatives

Inhibition of Glioma Cell Growth and Apoptosis Induction through Targeting Wnt10B Expression by Pyrazolo[4,3-c]pyridine-4-one

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