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7 data found. 1 - 7 listed

Published online: 2nd February, 2023

Paper | Regular issue | Prepress
DOI: 10.3987/COM-22-14801
■ Design, Synthesis, and Biological Evaluation of New Di-arylimidazole-quinazolinone Hybrid

Parsa Moghimirad, Shahin Boumi, Seyed Nasser Ostad, Maliheh Barazandeh Tehrani,* and Mohsen Amini*

*Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran14176, Iran

Abstract

The aim of this study is synthesis of new diarylimidazole-quinazolinone hybrid derivatives to target two binding sites of tubulin, an attractive target for design of anticancer drugs. In this report, the location of the accessible space of active site was determined by comparing the crystal structure of different inhibitors in tubulin structure. The docking and molecular dynamic simulations were used to confirm the position and stability of designed compounds. Thirteen new compounds were synthesized and their cytotoxicity were studied on three types of cancerous cell lines. Some of the synthesized compounds showed remarkable anti-proliferative activity in cell culture study.

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Published online: 2nd February, 2023

Review | Regular issue | Prepress
DOI: 10.3987/REV-23-1002
■ Utility of 6-Aminouracils for Building Substituted and Heteroannulated Pyrimidines: A Comprehensive Review

Magdy A. Ibrahim, Zeinab Hussain,* Nasser M. El-Gohary, Yassin A. Gabr, Hassan A. Allimony, and Al-Shimaa Badran

*Department of Chemistry, Faculty of Education, Ain Shams University, Roxy, 11711, Cairo-Egypt

Abstract

6-Aminouracils are very useful intermediates for building different categories of heterocyclic compounds. 6-Aminouracils are electron rich compounds due to the presence of free amino group which can initiate interactions with electron deficient centres or activate the nearby C-5 position to start the reaction followed by cyclization in most cases. The present review summarizes the different reactions developed for the synthesis of substituted and annulated pyrimidines. A diversity of substituted pyrimidines was prepared directly from reactions of 6-aminouracils with some electrophilic reagents, meanwhile formation of fused pyrimidines were
achieved by reaction of 6-aminouracils with a variety of reagents such as aromatic and aliphatic aldehydes, acyclic and cyclic methylene ketones, cyclic enols, alkynes, iminium salts and a diversity of other reagents.

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Published online: 26th January, 2023

Review | Regular issue | Prepress
DOI: 10.3987/REV-22-998
■ 3-[2-Oxo-2H-chromen-3(6)(8)-YL]-1-aryl/heteroaryl-1H-pyrazole-4-carbaldehydes: Synthesis, Reactions and Applications

Ayat K. Alsolimani, Mohammed A. Assiri, and Tarik E. Ali*

*Department of Chemistry, Faculty of Education, Ain Shams University, Roxy, Cairo, Egypt

Abstract

The chemistry of 3-(2-oxo-2H-chromen-3(6)(8)-yl)-1-aryl/heteroaryl-1H-pyrazole-4-carbaldehydes has gained increased interest in both synthetic organic and biological fields, since a large number of developments in the use of such compounds seem to be of considerable value. This review describes all the available synthetic methods for diverse 3-(2-oxo-2H-chromen-3(6)(8)-yl)-1-aryl/ heteroaryl-1H-pyrazole-4-carbaldehydes in the literature survey. It also summarizes thier chemical behaviors as building blocks towards a variety of chemical reagents to construct related compounds as well as their biological applications.

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Published online: 26th January, 2023

Short Paper | Regular issue | Prepress
DOI: 10.3987/COM-22-14799
■ A New Compound Embeloside A with Hypoglycemic Potential from the Fruits of Embelia Oblongifolia Hemsl.

Ying Xu, Yuqi Sun, Bing Liu, Ning Chen, Yingjie Liu, Dongxue Wang, Lei Yu,* and Haifeng Wang*

*School of Pharmacy, Harbin University of Commerce, Harbin, 150076, China

Abstract

A total of eleven compounds were isolated from the ripe and dried fruits of Embelia oblongifolia Hemsl. Compound 1 was a new one named embeloside A, in addition, compounds 2-4, 6 and 10 were isolated from this genus for the first time. Their molecular structures were elucidated by 1D/2D NMR spectroscopic analysis, HR-ESI-MS spectral data and charged aerosol detector (CAD). Further, hypoglycemic activity evaluation showed that compound 1 could reduce the fasting blood glucose levels in diabetic rats. Therefore, the results suggest that compound 1 might provide a theoretical basis for the development of potential hypoglycemic drugs. The discovery of compounds 1-11 might provide experimental guidance for the further development of Embelia oblongifolia Hemsl.

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Published online: 24th January, 2023

Short Paper | Regular issue | Prepress
DOI: 10.3987/COM-22-14794
■ Selective Synthesis of 2,2-Diamino-4,4,6,6-tetrakis(aryloxy)cyclotriphosphazenes N3P3-2,2-(NH2)2-4,4,6,6-(ArO)4

Manabu Kuroboshi,* Fumiya Nakamura, and Hideo Tanaka

*Graduate School of Natural Science and Technology, Okayama University, Tsushima-naka 3-1-1, Kita-ku, Okayama, Japan

Abstract

To synthesize cyclotriphosphazene derivatives having multi-functional groups, aryloxylation of 2,2-diamimo-4,4,6,6-tetrachlorocyclotriphosphazene 2 was examined. A mixture of gem-disubstituted N3P3(NH2)2(ArO)2Cl2 9gem, tri-substituted N3P3(NH2)2(ArO)3Cl 10, and tetra-substituted N3P3(NH2)2(ArO)4 11 was obtained, especially 11 was obtained selectively when excess amount (6 equiv.) of ArONa was used. On the other hand, mono-substituted N3P3(NH2)2(ArO)Cl3 8 and non-gem-di-substituted N3P3(NH2)2(ArO)2Cl2 9non-gem-cis and 9non-gem-trans were not detected.

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Published online: 25th October, 2022

Review | Regular issue | Prepress
DOI: 10.3987/REV-22-992
■ Recent Advances in the Synthesis of 1,2,4-Triazolo[3,4-b][1,3,4]thiadiazole Compounds: A Mini-Review

Jin Luo,* Puqing Chen, and Chonghu Song

*Analytical and Testing Center, Jiangxi Normal University, Nanchang, Jiangxi 330022, China

Abstract

1,2,4-Triazolo[3,4-b][1,3,4]thiadiazoles are important sulphur- and nitrogen-containing fused heterocycles that can act as promising scaffolds exhibiting outstanding biological activities. Herein, we focused on the major synthetic pathways and methodologies for the synthesis of 1,2,4-triazolo[3,4-b][1,3,4]thiadiazole compounds in an attempt to facilitate the discovery of unique 1,2,4-triazolo[3,4-b]-[1,3,4]thiadiazole derivatives with improved biological activities.

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Published online: 7th October, 2022

Review | Regular issue | Prepress
DOI: 10.3987/REV-22-993
■ Hydroxychloroquine: Chemistry and Medicinal Applications

Nidhi Yadav, Yogesh Kumar Tyagi,* and Ram Singh*

*Department of Applied Chemistry, Delhi Technological University, Delhi - 110042, India

Abstract

Hydroxychloroquine (HCQ) is a molecule from the 4-aminoquinoline family which is utilized for the treatment of many diseases. This is one of the essential drugs, as per WHO. HCQ has been an anti-malarial drug and is also used for the treatment of autoimmune and rheumatic diseases. This molecule is repurposed for many types of diseases, either alone or in combination with other drugs. This review article discusses its synthetic methodologies and approved applications along with repurposed studies. This article covers HCQ applications in anti-cancer activity, anti-rheumatic activity, epigenetic activity, systemic lupus erythematosus, and COVID-19.

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7 data found. 1 - 7 listed