Design and synthesis of novel thiophenecarbohydrazide, thienopyrazole and thienopyrimidine derivatives as antioxidant and antitumor agents

Abu‐Hashem, Ameen A.; Shehry, Mohamed F. El; Badria, Farid A.

doi:10.2478/v10007-010-0027-6

Cited by 86 publications

(63 citation statements)

References 18 publications

(13 reference statements)

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“…The viability of the cells determined by the microscopical examination using a hemocytometer and using trypan blue stain (stains only the dead cells). 24,25 …”

Section: Antioxidant Activity Screening Assay (Abts) Methodsmentioning

confidence: 99%

“…Negative control was run with MeOH/phosphate buffer (1:1) instead of test compound. 17,21,22,25 Bleomycin-dependent DNA damage…”

Section: Antioxidant Activity Screening Assay (Abts) Methodsmentioning

confidence: 99%

“…The assay was done according to Aeschlach 23,25 with minor modifications. The reaction mixture (0.5 mL) contained calf thymus DNA (0.5 mg/mL), bleomycin sulfate (0.05 mg/mL), MgCl 2 (5 mM), FeCl 3 (50 µM) and samples to be tested at different concentrations.…”

Section: Antioxidant Activity Screening Assay (Abts) Methodsmentioning

confidence: 99%

“…Erythrocyte hemolysis was mediated by peroxyl radicals in this assay system. 20,25 A 10% suspension of erythrocytes in phosphate buffered saline pH 7.4 (PBS) was added to the same volume of 200 mM AAPH solution in PBS containing samples to be tested at different concentrations. The reaction mixture was shaken gently while being incubated at 37 ºC for 2 h. The reaction mixture was then removed, diluted with eight volumes of PBS and centrifuged at 805´g for 10 min.…”

Section: Antioxidant Activity Screening Assay For Erythrocyte Hemolysismentioning

confidence: 99%

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Synthesis, Antioxidant, Antituomer Activities of Some New Thiazolopyrimidines, Pyrrolothiazolopyrimidines and Triazolopyrrolothiazolopyrimidines Derivatives

Abu‐Hashem

Youssef

Hussein

2011

J Chinese Chemical Soc

137

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Reaction of 6-amino-2-thiouracil 1 with ethyl bromoacetate yielded ethyl 2-(7-amino-2,5-dioxo-3,5-dihydro-2H-thiazolo[3,2-a]pyrimidin-6-yl)acetate 2. Reaction of 2 with sodium ethoxide afforded the pyrrolothiazolopyrimidine derivative 3. Compound 2 reacted with hydrazine hydrate to give 7-aminothiazolopyrimidine-carbohydrazide 4. The latter compound 4 reacted with carbon disulphide to form 7-amino-6-(oxadiazolylmethyl) thiazolopyrimidine 5. Compound 5 was heated in methanol to yield 9-thioxotriazolopyrrolothiazolopyrimidine 6. Also, the reaction of 3 with aromatic aldehydes afforded the diarylmethylenepyrrolothiazolopyrimidine derivatives 7a-c. The latter compounds 7a-c underwent cyclocondensation with hydroxylamine to give diaryldioxazolopyrrolothiazolopyrimidine derivatives 8a-c. The new prepared compounds were subjected for antioxidant and antituomer studies, some of these compounds exhibited promising activity.

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“…The viability of the cells determined by the microscopical examination using a hemocytometer and using trypan blue stain (stains only the dead cells). 24,25 …”

Section: Antioxidant Activity Screening Assay (Abts) Methodsmentioning

confidence: 99%

“…Negative control was run with MeOH/phosphate buffer (1:1) instead of test compound. 17,21,22,25 Bleomycin-dependent DNA damage…”

Section: Antioxidant Activity Screening Assay (Abts) Methodsmentioning

confidence: 99%

Section: Antioxidant Activity Screening Assay (Abts) Methodsmentioning

confidence: 99%

Section: Antioxidant Activity Screening Assay For Erythrocyte Hemolysismentioning

confidence: 99%

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Synthesis, Antioxidant, Antituomer Activities of Some New Thiazolopyrimidines, Pyrrolothiazolopyrimidines and Triazolopyrrolothiazolopyrimidines Derivatives

Abu‐Hashem

Youssef

Hussein

2011

J Chinese Chemical Soc

137

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“…A survey of the literature also reveals that substituted 2-aminothiophenes are potent and selective inhibitors of human leukocyte elastase (6), kinesin spindle protein (KPS) (7) and adenosine A1 receptor allosteric enhancers (8). Antifungal (9) and antitumor (10) properties have also been extensively described, resulting in marketed antifungal agents such as sertaconazole.…”

mentioning

confidence: 99%

Preliminary antifungal and cytotoxic evaluation of synthetic cycloalkyl[b]thiophene derivatives with PLS-DA analysis

Souza¹,

Oliveira²,

Aquino³

et al. 2012

Acta Pharmaceutica

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2-Aminothiophene derivatives are an important class of heterocycles found in several biologically active and natural compounds. This class of compounds has demonstrated a broad spectrum of activities and applications as pharmaceuticals and agrochemicals, dyes, biodiagnostics, and electronic and optoelectronic devices (1). -5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carbonitrile (2r), which inhibited more than 97 % growth of the three cell lines. The PLS discriminant analysis (PLS-DA) applied generated good exploratory and predictive results and showed that the descriptors having shape characteristics were strongly correlated with the biological data.

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Development of new Alzheimer's disease drug candidates using donepezil as a key model

Eissa

Kamel

Mohamed

et al. 2022

Archiv der Pharmazie

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Alzheimer's disease (AD) is one of the most prevalent geriatric diseases and a significant cause of high mortality. This crippling disorder is becoming more prevalent at an unprecedented rate, which has led to an increase in the financial cost of caring. It is a pathologically complicated, multifactorial disease characterized by β-amyloid precipitation, β-amyloid oligomer production, decrease in cholinergic function, and dysregulation of other neurotransmitter systems. Due to the pathogenic complexity of AD, multitarget drugs that can simultaneously alternate multiple biological targets may enhance the therapeutic efficacy. Donepezil (DNP) is the most potent approved drug for the treatment of AD. It has a remarkable effect on a number of AD-related processes, including cholinesterase activity, anti-Aβ aggregation, oxidative stress, and more. DNP resembles an excellent scaffold to be hybridized with other pharmacophoric moieties having biological activity against AD pathological factors. There have been significant attempts made to modify the structure of DNP to create new bioactive chemical entities with novel structural patterns. In this review, we highlight recent advances in the development of multiple-target DNP-hybridized models for the treatment of AD that can be used in the future in the rational design of new potential AD therapeutics. The design and development of new drug candidates for the treatment of AD using DNP as a molecular scaffold have also been reviewed and summarized.

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Design and synthesis of novel thiophenecarbohydrazide, thienopyrazole and thienopyrimidine derivatives as antioxidant and antitumor agents

Cited by 86 publications

References 18 publications

Synthesis, Antioxidant, Antituomer Activities of Some New Thiazolopyrimidines, Pyrrolothiazolopyrimidines and Triazolopyrrolothiazolopyrimidines Derivatives

Synthesis, Antioxidant, Antituomer Activities of Some New Thiazolopyrimidines, Pyrrolothiazolopyrimidines and Triazolopyrrolothiazolopyrimidines Derivatives

Preliminary antifungal and cytotoxic evaluation of synthetic cycloalkyl[b]thiophene derivatives with PLS-DA analysis

Development of new Alzheimer's disease drug candidates using donepezil as a key model

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