scholarly journals Synthesis of new derivatives of alepterolic acid via click chemistry

2021 ◽  
pp. 45-45
Author(s):  
Xin Jin ◽  
Jianguo Cao ◽  
Qingjie Zhao ◽  
Wang Qi ◽  
Hongmei Guo ◽  
...  
Keyword(s):  
Click Chemistry ◽  
Structural Modification ◽  
Folk Medicine ◽  
Functional Materials ◽  
Biological Evaluation ◽  
Reaction Conditions ◽  
Mass Spectral ◽  
The Common ◽  
Medicinal Activity ◽  
Derivatives Of

Alepterolic acid is a natural diterpenoid isolated from Aleuritopteris argentea (S.G. Gm?l.) F?e, a fern with potential medicinal activity, used in China as a folk medicine to regulate menstruation and prevent cancer. Nevertheless, there are few reports about the structural modification of this natural product. With the wide application of 1,2,3-triazole derivatives in medicines, pesticides, functional materials, the synthesis of 1,2,3-triazoles derivatives has attracted the attention of synthetic chemists. In this article, 23 new derivatives of alepterolic acid combined with 1,2,3-triazole were designed and synthesized by esterification and click chemistry reaction in a fast, conventional, and efficient way. All the products were obtained in good yields (72 to 97 %). The structure of these compounds was confirmed by 1H, 13C NMR, and mass spectral data. The use of the easily available reactants and the common reaction conditions furnish an efficient method for the synthesis of alepterolic acid derivatives. The preparation of these compounds would enable further biological evaluation in the future.

Synthesis and biological evaluation of fluorinated analogues of ripostatin A

2019 ◽  
Vol 17 (6) ◽  
pp. 1362-1364 ◽  
Author(s):  
Vladyslav Shenderman ◽  
Evgeny V. Prusov
Keyword(s):  
Click Chemistry ◽  
Biological Evaluation ◽  
Last Stage ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of

A last stage click-chemistry approach to synthesize the heterocycle-containing derivatives of fluorinated ripostatin A was developed.

scholarly journals Synthesis and biological evaluation of novel urea and thiourea derivatives of valacyclovir

2014 ◽  
Vol 79 (3) ◽  
pp. 283-289 ◽  
Author(s):  
Ramana Katla ◽  
Rasheed Syed ◽  
Madhava Golla ◽  
Adam Shaik ◽  
Raju Chamarthi
Keyword(s):  
Antioxidant Activity ◽  
Antiviral Activity ◽  
Elemental Analysis ◽  
Antioxidant Activities ◽  
Biological Evaluation ◽  
Thiourea Derivatives ◽  
Mass Spectral ◽  
High Yields ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of

A series of novel urea and thiourea derivatives of valacyclovir were efficiently synthesized in high yields and evaluated their antiviral activity. 2-((6-Amino-4-oxo-4,5-dihydro-1H-imidazo[4,5-c]pyridin-1-yl)methoxy)ethyl-2-amino-3-ethylbutanoate (valacyclovir) 1 is reacted with various aromatic isocyanates/thiocyanates 2 in the presence of N, N- dimethyl piperazine as a base in THF: pyridine (4:1) to obtain valacyclovir urea/thiourea derivatives 3(a-j). The structures of the title compounds 3(a-j) were confirmed by IR, NMR (1H, 13C), mass spectral and elemental analysis. The newly synthesized compounds were screened for their antiviral activity against Tobacco mosaic virus (TMV) and antioxidant activity was evaluated by DPPH, SOD and GST methods. The title compounds exhibited potent antiviral and good antioxidant activities.

scholarly journals MICROWAVE-ASSISTED SYNTHESIS, CHARACTERIZATION, AND BIOLOGICAL EVALUATION OF PHENYLACRYLAMIDE DERIVATIVES OF TRIAZOLES DERIVED FROM OXAZOLONES

2018 ◽  
Vol 11 (7) ◽  
pp. 285
Author(s):  
Venkat Swamy Puli ◽  
Vukoti Kiran Kumar ◽  
Venkata Reddy Regalla ◽  
Anindita Chatterjee
Keyword(s):  
Antioxidant Activities ◽  
Reaction Times ◽  
Biological Evaluation ◽  
Biologically Active ◽  
Spectral Studies ◽  
Microwave Assisted Synthesis ◽  
Microwave Technology ◽  
Mass Spectral ◽  
Microwave Assisted ◽  
Derivatives Of

Objective: The aim of the present study is to synthesize novel phenylacrylamide derivatives as potent bioactive agents.Methods: Novel N-(3-(4H-1,2,4-triazol-4-ylamino)-3-oxo-1-arylidene prop-2-yl) benzimidic acids (7a-c) have been synthesized by the reaction of 4-(arylidene)-2-phenyloxazol-5(4H)-ones (5a-c) with 4-amino-1, 2, 4-triazole (6) in the presence of anhydrous sodium acetate in glacial acetic acid. Titled compounds (7a-c) were obtained in good yields using microwave technology which resulted in dramatic reductions in reaction times leading to the formation of phenylacrylamide derivatives (7a-c) at a faster rate.Results: The structures of the newly synthesized compounds were characterized by Fourier-transform infrared, 1H NMR, 13C NMR, and mass spectral studies. This method can be an efficient method for the synthesis of phenylacrylamide derivatives (7a-c).Conclusion: All the final compounds were screened for their antimicrobial and antioxidant activities and found to be biologically active. Among all the compounds, 7b was found to be potent antimicrobial and antioxidant.

scholarly journals Synthesis, characterization and study the biological evaluation of some Schiff base derivatives in the presence of lemon juice catalyst

2019 ◽  
Vol 9 (4) ◽  
pp. 4187-4192
Keyword(s):  
Nmr Spectra ◽  
Inhibitory Concentration ◽  
Antibacterial Activities ◽  
Biological Evaluation ◽  
Lemon Juice ◽  
Gram Negative Bacteria ◽  
13C Nmr Spectra ◽  
Reaction Conditions ◽  
Schiff Base Derivatives ◽  
Derivatives Of

In this project, we tried to synthesis derivatives of 4-(benzylidene) aminopyrimidine (I), (benzo[d]thiazol-2-ylimino) methylphenol (II), n-benzylideneazine (III) and n-benzylideneaniline (IV) with natural catalyst and solvent instead of chemical catalyst and solvent condition as green chemistry. The advantages of the use of natural catalyst without organic solvent are eco-friendly, affordable, very safe and easy reaction conditions. The synthesized product was characterized by melting point, IR, 1H NMR and 13C NMR spectra. All derivatives of 4-(benzylidene)aminopyrimidine (I) were tested against gram-positive and gram-negative bacteria by minimum inhibitory concentration (MIC) and disk diffusion methods for antibacterial activities.

Exploring the Chemistry and Therapeutic Potential of Triazoles: A Comprehensive Literature Review

2019 ◽  
Vol 19 (16) ◽  
pp. 1298-1368 ◽  
Author(s):  
Ankit Jain ◽  
Poonam Piplani
Keyword(s):  
Oxidative Stress ◽  
Drug Discovery ◽  
Literature Review ◽  
Structural Modification ◽  
Therapeutic Potential ◽  
Pharmacological Properties ◽  
Pharmacological Activities ◽  
Triazole Derivatives ◽  
Comprehensive Literature Review ◽  
The Common

: Triazole is a valuable platform in medicinal chemistry, possessing assorted pharmacological properties, which could play a major role in the common mechanisms associated with various disorders like cancer, infections, inflammation, convulsions, oxidative stress and neurodegeneration. Structural modification of this scaffold could be helpful in the generation of new therapeutically useful agents. Although research endeavors are moving towards the growth of synthetic analogs of triazole, there is still a lot of scope to achieve drug discovery break-through in this area. Upcoming therapeutic prospective of this moiety has captured the attention of medicinal chemists to synthesize novel triazole derivatives. The authors amalgamated the chemistry, synthetic strategies and detailed pharmacological activities of the triazole nucleus in the present review. Information regarding the marketed triazole derivatives has also been incorporated. The objective of the review is to provide insights to designing and synthesizing novel triazole derivatives with advanced and unexplored pharmacological implications.

Synthesis, Structural Studies and Biological Evaluation of Halogen Derivatives of 1,3-Disubstituted Thiourea

2017 ◽  
Vol 14 (6) ◽  
Author(s):  
Anna Bielenica ◽  
Karolina Stepien ◽  
Aleksandra Sawczenko ◽  
Tadeusz Lis ◽  
Anna E. Koziol ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Structural Studies ◽  
Derivatives Of

Design, Synthesis and Biological Evaluation of Novel Aminosaccharide Derivatives of Combretastatin A-4

2013 ◽  
Vol 10 (10) ◽  
pp. 935-941
Author(s):  
Yan Tang ◽  
Zhewei Tu ◽  
Jing Sun ◽  
Xiong Zhu ◽  
Kun Liu ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of

Synthesis and Cytotoxicity Assessment of Novel 7-O- and 14-O-Derivatives of Glaucocalyxin A

2020 ◽  
Vol 20 (10) ◽  
pp. 1241-1249
Author(s):  
Hong-Chuan Liu ◽  
Li-Ming Qiao ◽  
Wei Zheng ◽  
Zhao-Bao Xiang ◽  
Hai-Sheng Chen ◽  
...  
Keyword(s):  
Acute Toxicity ◽  
Cell Lines ◽  
Cancer Cell ◽  
Human Cancer ◽  
Folk Medicine ◽  
A549 Cells ◽  
Cancer Cell Lines ◽  
Human Cancer Cell Lines ◽  
Derivatives Of

Background: Rabdosia japonica has been historically used in China as a popular folk medicine for the treatment of cancer, hepatitis, and gastricism. Glaucocalyxin A (GLA), an ent-kaurene diterpene isolated from Rabdosia japonica, is one of the main active ingredients showing potent inhibitory effects against several types of tumor cells. To the best of our knowledge, studies regarding the structural modification and Structure- Activity Relations (SAR) of this compound have not yet been reported. Objective: The aim of this study was to discover more potent derivatives of GLA and investigate their SAR and cytotoxicity mechanisms. Methods: Novel 7-O- and 14-O-derivatives of GLA were synthesized by condensation of acids or acyl chloride. The anti-tumor activities of these derivatives against various human cancer cell lines were evaluated in vitro by MTT assays. Apoptosis assays of compound 17 (7,14-diacylation product) were performed on A549 and HL-60 cells by flow cytometry and TUNNEL. The acute toxicity of this compound was tested on mice, at the dose of 300mg per kg body weight. Results: Seventeen novel 7-O- and 14-O-derivatives of GLA (1-17) were synthesized. These compounds showed potent cytotoxicity against the tested cancer cell lines, and almost all of them were found to be more cytotoxic than GLA and oridonin. Of the synthesized derivatives, compound 17 presented the greatest cytotoxicity, with IC50 values of 0.26μM and 1.10μM in HL-60 and CCRF-CEM cells, respectively. Furthermore, this compound induced weak apoptosis of A549 cells but showed great potential in stimulating the apoptosis of HL- 60 cells. Acute toxicity assays indicated that compound 17 is relatively safer. Conclusion: The results reported herein indicate that the synthesized GLA derivatives exhibited greater cytotoxicity against leukemia cells than against other types of tumors. In particular, 7,14-diacylation product of GLA was found to be an effective anti-tumor agent. However, the cytotoxicity mechanism of this product in A549 cells is expected to be different than that in other tumor cell lines. Further research is needed to confirm this hypothesis.

Hybridized Quinoline Derivatives as Anticancer Agents: Design, Synthesis, Biological Evaluation and Molecular Docking

2019 ◽  
Vol 19 (4) ◽  
pp. 439-452 ◽  
Author(s):  
Mohamed R. Selim ◽  
Medhat A. Zahran ◽  
Amany Belal ◽  
Moustafa S. Abusaif ◽  
Said A. Shedid ◽  
...  
Keyword(s):  
Cell Cycle ◽  
Anticancer Agents ◽  
Caspase 3 ◽  
Biological Evaluation ◽  
Tubulin Polymerization ◽  
Design Synthesis ◽  
Chemical Structures ◽  
M Phase ◽  
Induced Apoptosis ◽  
Derivatives Of

Objective: Conjugating quinolones with different bioactive pharmacophores to obtain potent anticancer active agents. Methods: Fused pyrazolopyrimidoquinolines 3a-d, Schiff bases 5, 6a-e, two hybridized systems: pyrazolochromenquinoline 7 and pyrazolothiazolidinquinoline 8, different substituted thiazoloquinolines 13-15 and thiazolo[3,2-a]pyridine derivatives 16a-c were synthesized. Their chemical structures were characterized through spectral and elemental analysis, cytotoxic activity on five cancer cell lines, caspase-3 activation, tubulin polymerization inhibition and cell cycle analysis were evaluated. Results: Four compounds 3b, 3d, 8 and 13 showed potent activity than doxorubicin on HCT116 and three compounds 3b, 3d and 8 on HEPG2. These promising derivatives showed increase in the level of caspase-3. The trifloromethylphenyl derivatives of pyrazolopyrimidoquinolines 3b and 3d showed considerable tubulin polymerization inhibitory activity. Both compounds arrested cell cycle at G2/M phase and induced apoptosis. Conclusion: Compounds 3b and 3d can be considered as promising anticancer active agents with 70% of colchicine activity on tubulin polymerization inhibition and represent hopeful leads that deserve further investigation and optimization.

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