Design and synthesis of some substituted thiazolo[3,2-a]pyrimidine derivatives of potential biological activities

Moty, Samia G. Abdel; Hussein, Mostafa A.; Aziz, Salah A. Abdel; Abou-Salim, Mahrous A.

doi:10.1016/j.jsps.2013.12.016

Cited by 34 publications

(5 citation statements)

References 19 publications

(28 reference statements)

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“…They have been reported to inhibit specific enzymes, such as AChE [5], cell division cycle (Cdc) 25B phosphatase [6], casein kinase 2 [7], YycG histidine kinase [8], 2-methylerythritol 2,4-cyclodiphosphate synthase (IspF) proteins from Mycobacterium tuberculosis , Plasmodium falciparum , and Arabidopsis thaliana [9], and xanthine oxidase [10]. While the precise biological targets remain to be elucidated in some cases, thiazolo[3,2- a ]pyrimidines have widely been reported to possess anti-cancer [11], anti-inflammatory and analgesic [12,13,14,15], anti-microbial, antibiofilm, antioxidant, DNA cleavage [8,16,17,18,19,20], antiviral [21,22], anti-Parkinsonian [23], antidiabetic [24], antihypertensive, and inotropic [25] activities. Other possible applications include their use as antimalarials and inhibitors of HIV reverse transcriptase [9,26], as well as antagonists of the 5-HT2 serotonin receptor, with potential interest for the treatment of depression [27,28].…”

Section: Introductionmentioning

confidence: 99%

Synthesis, Crystal Structure, and Biological Evaluation of Fused Thiazolo[3,2-a]Pyrimidines as New Acetylcholinesterase Inhibitors

et al. 2019

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A new series of thiazolo[3,2-a]pyrimidine bromide salt derivatives 7a–d were synthesized from 3,4-dihydropyrimidinethione precursors. The target compounds were fully characterized by 1D- and 2D-NMR, high resolution ESI-MS/MS and single crystal X-ray diffraction analysis, which confirmed a regioselective 5H cyclization of the dihydropyrimidinethiones. All target compounds were evaluated in vitro as human acetylcholinesterase (hAChE) inhibitors via an Ellman-based colorimetric assay and showed good inhibition activities (better than 70% at 10 µM and IC50 values in the 1 µM range). Molecular docking simulations for all target products into hAChE were performed and confirmed strong binding to the enzyme. These results provide a promising and new starting point to improve acetylcholinesterase inhibitors and explore novel treatment options against Alzheimer’s disease.

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Section: Introductionmentioning

confidence: 99%

Synthesis, Crystal Structure, and Biological Evaluation of Fused Thiazolo[3,2-a]Pyrimidines as New Acetylcholinesterase Inhibitors

et al. 2019

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“…Pneumothorax then occur after bullae rupture. Many scholars hold based on research that the mechanism described above belong to one-way valve mechanism; third, for a small number of patients, lung tumor tissue and visceral pleura can have direct invasion (ATTARI et al, 2016;ABDEL et al, 2016). In this study, there were 1900 patients having lung cancer with distal visceral pleura rupture.…”

Section: Discussionmentioning

confidence: 85%

Application of VATS in Diagnosis and Treatment of Lung Cancer Complicated with Pneumothorax

Lv¹,

Zhao²,

Zhang³

et al. 2018

Biosci. J.

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ABSTRACT:The paper aims to explore clinical symptoms and complication characteristic of lung cancer complicated with pneumothorax, analyze clinical diagnostic value of VATS, and elaborate on specific clinical programs and significance. To investigate diagnosis and therapeutic value of VATS for lung cancer complicated with pneumothorax, 1900 cases of patients with lung cancer complicated with pneumothorax were randomly selected as research objects to be treated with VATS, and then analysis of their clinical data was done. The clinical data showed that many patients were not clearly diagnosed before operation. In VATS operation, lung tumor tissue was removed and then immediately frozen and sliced. Appropriate surgical approach was chosen based on specific circumstances of patients. As can be known from the results, 1000 cases were treated with wedge resection of lung tumor under thoracoscopy, 900 cases were treated with assisted small incision surgery under thoracoscopy. 1400 cases of lung metastasis were treated with pleural friction fixation. All the operations were successful, with pathology being clearly diagnosed. After surgery, 8 patients had mild air leakage, which could be heal without special treatment. There was no perioperative death. The above analysis shows that VATS can clearly diagnose peripheral lung tumor, and fundamentally cure pneumothorax and lung cancer, which is thus recommended in clinic.

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“…Composite soil samples were air dried, passed through a 2-mm sieve, and manually cleaned of any visible plant tissues for laboratory analysis. Soil organic carbon content and soil total nitrogen content were determined by an element analyzer (Vario EL III), and soil total phosphorous content (Moty et al, 2016) was analyzed by using the molybdenum blue colorimetric method with a UV/visible spectrophotometer after H2SO4-H2O2 digestion (UV-2550; Shimadzu, Kyoto, Japan).…”

Section: Methodsmentioning

confidence: 99%

Fine-Root Turnover, Litterfall, and Soil Microbial Community of Three Mixed Coniferous–Deciduous Forests Dominated by Korean Pine (Pinus koraiensis) Along a Latitudinal Gradient

Yang

Wang

et al. 2019

Front. Plant Sci.

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Carbon dynamics in forests and in particular in soils are of primary importance in the context of climate change. A better understanding of the drivers controlling carbon storage is needed to improve climate mitigation strategies. Carbon storage is the result of a balance between inputs and outputs. Carbon inputs in the soil come from plant residues and root exudates, which are further transformed by microorganisms and stored in the long term. Here, we measured litter and fine-root production in three mixed forests dominated by Pinus koraiensis along a latitudinal gradient and performed a litterbag experiment to better understand the driving factors of decomposition. We found that over the three sites litter production was controlled by climatic factors, soil properties, and forest stand characteristics, whereas decay rates were mainly controlled by microbial community structure and soil stoichiometry. For fine roots, production differed among sites, and higher production was consistently observed in the top soil layers compared to deep soil, although the root distribution along the soil profile differed among sites. Fine-root decay rates were mainly controlled by fine-root stoichiometric characteristics. This article emphasizes the complexity of fine-root dynamics even for a single species. Environmental drivers impact on both production and decay, and we suggest performing manipulative field experiments to better identify the mechanisms involved in soil carbon cycling.

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Design and synthesis of some substituted thiazolo[3,2-a]pyrimidine derivatives of potential biological activities

Cited by 34 publications

References 19 publications

Synthesis, Crystal Structure, and Biological Evaluation of Fused Thiazolo[3,2-a]Pyrimidines as New Acetylcholinesterase Inhibitors

Synthesis, Crystal Structure, and Biological Evaluation of Fused Thiazolo[3,2-a]Pyrimidines as New Acetylcholinesterase Inhibitors

Application of VATS in Diagnosis and Treatment of Lung Cancer Complicated with Pneumothorax

Fine-Root Turnover, Litterfall, and Soil Microbial Community of Three Mixed Coniferous–Deciduous Forests Dominated by Korean Pine (Pinus koraiensis) Along a Latitudinal Gradient

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