A Review on Biological Properties and Synthetic Methodologies of the Diarylpentadienones

2020 ◽  
Vol 20 ◽  
Author(s):  
Maryam Aisyah Abdullah ◽  
Siti Munirah Mohd Faudzi ◽  
Nadiah Mad Nasir
Keyword(s):  
Biological Properties ◽  
Review Article ◽  
High Potential ◽  
One Pot ◽  
One Pot Synthesis ◽  
Structure Activity ◽  
Synthetic Methodologies ◽  
Relationship Of ◽  
Effective Drugs ◽  
Enhanced Stability

Abstract:: Medicinal chemists have continuously shown interest in new curcuminoid derivatives, the diarylpentadienones, owing to their enhanced stability feature and easy preparation using a one-pot synthesis. Thus far, methods such as Claisen-Schmidt condensation and Julia-Kocienski olefination have been utilised for the synthesis of these compounds. Diarylpentadienones possess a high potential as a chemical source for designing and developing new and effective drugs for the treatment of diseases, including inflammation, cancer, and malaria. In brief, this review article focuses on the broad pharmacological applications and the summary of the structure-activity relationship of molecules which can be employed to further explore the structure of diarylpentadienone. The current methodological developments towards the synthesis of diarylpentadienones are also discussed.

scholarly journals Synthesis, Antiprotozoal Activity, and Cheminformatic Analysis of 2-Phenyl-2H-Indazole Derivatives

Molecules ◽  
2021 ◽  
Vol 26 (8) ◽  
pp. 2145
Author(s):  
Karen Rodríguez-Villar ◽  
Lilián Yépez-Mulia ◽  
Miguel Cortés-Gines ◽  
Jacobo David Aguilera-Perdomo ◽  
Edgar A. Quintana-Salazar ◽  
...  
Keyword(s):  
Phenyl Ring ◽  
Medicinal Chemistry ◽  
Structural Features ◽  
Pharmacological Properties ◽  
Antiprotozoal Activity ◽  
One Pot ◽  
Biological Assays ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
Synthetic Methodologies

Indazole is an important scaffold in medicinal chemistry. At present, the progress on synthetic methodologies has allowed the preparation of several new indazole derivatives with interesting pharmacological properties. Particularly, the antiprotozoal activity of indazole derivatives have been recently reported. Herein, a series of 22 indazole derivatives was synthesized and studied as antiprotozoals. The 2-phenyl-2H-indazole scaffold was accessed by a one-pot procedure, which includes a combination of ultrasound synthesis under neat conditions as well as Cadogan’s cyclization. Moreover, some compounds were derivatized to have an appropriate set to provide structure-activity relationships (SAR) information. Whereas the antiprotozoal activity of six of these compounds against E. histolytica, G. intestinalis, and T. vaginalis had been previously reported, the activity of the additional 16 compounds was evaluated against these same protozoa. The biological assays revealed structural features that favor the antiprotozoal activity against the three protozoans tested, e.g., electron withdrawing groups at the 2-phenyl ring. It is important to mention that the indazole derivatives possess strong antiprotozoal activity and are also characterized by a continuous SAR.

scholarly journals Polyelectrolytes Tailored Enzyme Cascades with Enhanced Stability and Activity for One‐pot Synthesis

ChemCatChem ◽  
2018 ◽  
Vol 10 (23) ◽  
pp. 5391-5396 ◽  
Author(s):  
Zheyu Wang ◽  
Junqian Wang ◽  
Gong Chen ◽  
Weina Xu ◽  
Zhongwang Fu ◽  
...  
Keyword(s):  
One Pot ◽  
One Pot Synthesis ◽  
Enzyme Cascades ◽  
Enhanced Stability

Developed one-pot synthesis of dual-color CdSe quantum dots for white light-emitting diode application

2018 ◽  
Vol 6 (12) ◽  
pp. 3089-3096 ◽  
Author(s):  
Sheng Dai ◽  
Cyuan-Bin Siao ◽  
Shu-Ru Chung ◽  
Kuan-Wen Wang ◽  
Xiaoqing Pan
Keyword(s):  
Quantum Dots ◽  
White Light ◽  
Light Emitting Diode ◽  
Cdse Quantum Dots ◽  
Cdse Qds ◽  
One Pot ◽  
Synthetic Process ◽  
Light Emitting ◽  
One Pot Synthesis ◽  
Enhanced Stability

The size and fraction of red and green CdSe QDs can be controlled precisely during the synthetic process, thus manifesting remarkably enhanced stability.

scholarly journals One-pot synthesis, anti-tumor evaluation and structure–activity relationships of novel 25-OCH3-PPD derivatives

MedChemComm ◽  
2017 ◽  
Vol 8 (9) ◽  
pp. 1845-1849 ◽  
Author(s):  
Fan-Zhi Qu ◽  
Chen Zhao ◽  
Jia-Qing Cao ◽  
Yan Zhang ◽  
Yu-Qing Zhao
Keyword(s):  
Panax Ginseng ◽  
Synthetic Method ◽  
Lead Compound ◽  
One Pot ◽  
Structure Activity Relationships ◽  
One Pot Synthesis ◽  
Structure Activity

Based on the fact that 25-OCH3-PPD, a natural ginsengenin isolated from the leaves of Panax ginseng, is a promising lead compound, novel 25-OCH3-PPD derivatives were synthesized to find more potent anti-tumor agents by a simple and facile synthetic method.

Indazole as a Privileged Scaffold: The Derivatives and their Therapeutic Applications

2020 ◽  
Vol 20 ◽  
Author(s):  
Jinling Qin ◽  
Weyland Cheng ◽  
Yong-Tao Duan ◽  
Hua Yang ◽  
Yongfang Yao
Keyword(s):  
Biological Activities ◽  
Biological Properties ◽  
Vital Role ◽  
Drug Molecules ◽  
Structure Activity ◽  
Privileged Scaffold ◽  
Future Direction ◽  
Relationship Of ◽  
Anti Hiv ◽  
Clinical Drug

Background: Heterocyclic compounds, also called heterocycles, are a major class of organic chemicalcompound that plays a vital role in the metabolism of all living cells. The heterocyclic compound, indazole, has attracted more attention in recent years and is widely present in numerous commercially available drugs. Indazole-containing derivatives, representing one of the most important heterocycles in drug molecules, are endowed with a broad range of biological properties. Methods: A literature search was conducted in PubMed, Google Scholar and Web of Science regarding articles related to indazole and its therapeutic application. Results: The mechanism and structure-activity relationship of indazole and its derivatives were described. Based on their versatile biological activities, the compounds were divided into six groups: anti-inflammatory, antibacterial, anti-HIV, antiarrhythmic, antifungal and antitumour. At least 43 indazole-based therapeutic agents were found to be used in clinical application or clinical trials. Conclusion: This review is a guide for pharmacologists who are in search of valid preclinical/clinical drug compoundswhere the progress of approved marketed drugs containing indazole scaffold is examined from 1966 to the present day. Future direction involves more diverse bioactive moieties with indazole scaffold and greater insights into its mechanism.

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