scholarly journals Synthesis and Preliminary Biological Evaluation of 1,3,5-Triazine Amino Acid Derivatives to Study Their MAO Inhibitors

Molecules ◽  
2015 ◽  
Vol 20 (9) ◽  
pp. 15976-15988 ◽  
Author(s):  
Sherine Khattab ◽  
Hosam Khalil ◽  
Adnan Bekhit ◽  
Mohamed El-Rahman ◽  
Ayman El-Faham ◽  
...  
Keyword(s):  
Amino Acid ◽  
Biological Evaluation ◽  
Amino Acid Derivatives ◽  
Mao Inhibitors

scholarly journals Synthesis and Biological Evaluation of Novel Phenylpropenoyl-amino Acid Derivatives

2019 ◽  
Vol 39 (7) ◽  
pp. 1953
Author(s):  
Sufan Gao ◽  
Yanchun Zhang ◽  
Jiaming Li ◽  
Bin Zhang ◽  
Yu Yang ◽  
...  
Keyword(s):  
Amino Acid ◽  
Biological Evaluation ◽  
Amino Acid Derivatives ◽  
Synthesis And Biological Evaluation

scholarly journals Synthesis of Novel Baicalein Amino Acid Derivatives and Biological Evaluation as Neuroprotective Agents

Molecules ◽  
2019 ◽  
Vol 24 (20) ◽  
pp. 3647 ◽  
Author(s):  
Xiaohui Jia ◽  
Menglu Jia ◽  
Yuqin Yang ◽  
Di Wang ◽  
Fei Zhou ◽  
...  
Keyword(s):  
Amino Acid ◽  
High Resolution Mass Spectrometry ◽  
Neuroprotective Effect ◽  
Biological Evaluation ◽  
Neuroprotective Activity ◽  
Amino Acid Derivatives ◽  
H9c2 Cell ◽  
Butyl Hydroperoxide ◽  
Tert Butyl ◽  
Tert Butyl Hydroperoxide

Baicalein, a famously effective component of the traditional Chinese medicine Rhizoma Huang Qin (Scutellaria altissima L.), has been proved to have potent neuroprotection and anti-platelet aggregation effects with few side effects. Meanwhile, recent studies have revealed that the introduction of amino acid to baicalein could improve its neuroprotective activity. In the present study, a series of novel baicalein amino acid derivatives were designed, synthesized, and screened for their neuroprotective effect against tert-butyl, hydroperoxide-induced, SH-SY5Y neurotoxicity cells and toxicity on the normal H9C2 cell line by standard methylthiazol tetrazolium (MTT) assay. In addition, all of the newly synthesized compounds were characterized by 1H-NMR, 13C-NMR, and high resolution mass spectrometry (HR-MS). The results showed that most of the compounds provided more potent neuroprotection than baicalein, and were equivalent to the positive drug edaravin. They showed no obvious cytotoxicity on normal H9C2 cells. Notably, the most active compound 8 displayed the highest protective effect (50% effective concentration (EC50) = 4.31 μM) against tert-butyl, hydroperoxide-induced, SH-SY5Y neurotoxicity cells, which was much better than the baicalein (EC50 = 24.77 μM) and edaravin (EC50 = 5.62 μM). Further research on the chick chorioallantoic membrane (CAM) model indicated that compound 8 could significantly increase angiogenesis, which might promote neurovascular proliferation. The detection of apoptosis analysis showed that compound 8 could dramatically alleviate morphological manifestations of cell damage. Moreover, the benzyloxycarbonyl (cbz)-protected baicalein amino acid derivatives showed better neuroprotective activity than the t-Butyloxy carbonyl (boc)-protected derivatives.

Synthesis and Biological Evaluation of SeCF3‐Substituted α‐Amino Acid Derivatives

ChemMedChem ◽  
2021 ◽  
Author(s):  
Zhou-Zhou Han ◽  
Tao Dong ◽  
Xiao-Xia Ming ◽  
Fu Kuang ◽  
Cheng-Pan Zhang
Keyword(s):  
Amino Acid ◽  
Biological Evaluation ◽  
Amino Acid Derivatives ◽  
Synthesis And Biological Evaluation

scholarly journals Design, Synthesis and Biological Evaluation of Diosgenin-Amino Acid Derivatives with Dual Functions of Neuroprotection and Angiogenesis

Molecules ◽  
2019 ◽  
Vol 24 (22) ◽  
pp. 4025 ◽  
Author(s):  
Desheng Cai ◽  
Jinchai Qi ◽  
Yuqin Yang ◽  
Wenxi Zhang ◽  
Fei Zhou ◽  
...  
Keyword(s):  
Amino Acid ◽  
Cell Line ◽  
Chorioallantoic Membrane ◽  
Biological Evaluation ◽  
Amino Acid Derivatives ◽  
H9c2 Cell ◽  
Protecting Group ◽  
Neuroprotective Effects ◽  
Wide Range ◽  
Dual Functions

Diosgenin, a natural product with steroidal structure, has a wide range of clinical applications in China. It also shows great potential in the treatment of blood clots and nerve damage. To enhance the bioavailability as well as efficacy of diosgenin, eighteen diosgenin-amino acid derivatives were designed and synthesized. The neuroprotective effects of these compounds were evaluated by SH-SY5Y cell line and the biosafety was evaluated by H9c2 cell line. The results displayed that part of the derivatives’ activities (EC50 < 20 μM) were higher than positive control edaravone (EC50 = 21.60 ± 3.04 μM), among which, DG-15 (EC50 = 6.86 ± 0.69 μM) exhibited the best neuroprotection. Meanwhile, biosafety evaluation showed that DG-15 had no cytotoxicity on H9c2 cell lines. Interestingly, combined neuroprotective and cytotoxic results, part of the derivatives without their protecting group were superior to compounds with protecting group. Subsequently, Giemsa staining and DAPI (4′,6-diamidino-2-phenylindole) staining indicated that DG-15 had a protective effect on damaged SH-SY5Y cells by reducing apoptosis. Moreover, DG-15 showed a higher role in promoting angiogenesis at high concentrations (4 mg/mL) on the chorioallantoic membrane model. This finding displayed that DG-15 had dual functions of neuroprotection and angiogenesis, which provided further insight into designing agent for the application in treatment of ischemic stroke.

Synthesis and evaluation of quinazoline amino acid derivatives as mono amine oxidase (MAO) inhibitors

2015 ◽  
Vol 23 (13) ◽  
pp. 3574-3585 ◽  
Author(s):  
Sherine Nabil Khattab ◽  
Nesreen Saied Haiba ◽  
Ahmed Mosaad Asal ◽  
Adnan A. Bekhit ◽  
Adel Amer ◽  
...  
Keyword(s):  
Amino Acid ◽  
Amine Oxidase ◽  
Amino Acid Derivatives ◽  
Mao Inhibitors

Biological evaluation of new [18F]F-labeled synthetic amino acid derivatives as oncologic radiotracers

2016 ◽  
Vol 59 (10) ◽  
pp. 404-410 ◽  
Author(s):  
Yeseulmi Kim ◽  
Sang Ju Lee ◽  
Cheol-Min Yook ◽  
Seung Jun Oh ◽  
Jin-Sook Ryu ◽  
...  
Keyword(s):  
Amino Acid ◽  
Biological Evaluation ◽  
Amino Acid Derivatives ◽  
Synthetic Amino Acid
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