Recent progress in the total synthesis of pyrrole-containing natural products (2011-2020)

Author(s):  
Nidhi Singh ◽  
Snigdha Singh ◽  
Sahil Kohli ◽  
Aarushi Singh ◽  
Hannah Asiki ◽  
...  

Natural products have long served as a rich resource for drug discovery in the treatment of illnesses and chronic diseases. Among many families exhibiting fascinating structural complexity and impressive bioactivity,...

Symmetry ◽  
2021 ◽  
Vol 13 (4) ◽  
pp. 720
Author(s):  
Satomi Niwayama

Symmetric organic compounds are generally obtained inexpensively, and therefore they can be attractive building blocks for the total synthesis of various pharmaceuticals and natural products. The drawback is that discriminating the identical functional groups in the symmetric compounds is difficult. Water is the most environmentally benign and inexpensive solvent. However, successful organic reactions in water are rather limited due to the hydrophobicity of organic compounds in general. Therefore, desymmetrization reactions in aqueous media are expected to offer versatile strategies for the synthesis of a variety of significant organic compounds. This review focuses on the recent progress of desymmetrization reactions of symmetric organic compounds in aqueous media without utilizing enzymes.


Author(s):  
Beatriz de las Heras Polo

Natural products have historically contributed to drug discovery as a source of bioactive molecules, due to their great diversity and structural complexity. They have provided “lead” molecules for the development of drugs in different therapeutic areas, with a very prominent representation in the treatment of pain and inflammation, coagulation disorders, metabolic disorders, as well as in the treatment of cancer and infectious diseases. In recent decades there has been a paradigm shift in drug discovery strategies that has allowed the identification of new active natural products in therapeutic targets. Combinatorial Chemistry and biological tests (High Throughput Screening), together with the development of computational techniques, have contributed decisively to the design and optimization of libraries of natural product derivatives based on their biological activity. In parallel, technological advances in the field of Omics sciences and in data processing lead to a multidimensional approach in the drug discovery process. These powerful tools will allow the analysis of the pharmacological potential of natural products and their derivatives for the conversion of these molecules to active products with low toxicity. In the Precision Medicine era, natural products continue to be molecules with great potential in pharmaceutical development, since, unlike other therapeutic strategies, they have a favorable cost-benefit ratio, which will allow their future use in this discipline.


2013 ◽  
Vol 8 (7) ◽  
pp. 1934578X1300800 ◽  
Author(s):  
Takuya Imaoka ◽  
Makoto Iwata ◽  
Takafumi Akimoto ◽  
Kazuo Nagasawa

Oroidin derived pyrrole imidazole marine alkaloids (PIAs) are attractive targets for synthetic organic chemists because of their structural complexity and diversity as well as their interesting biological activities. A number of efforts have been carried out to develop strategies for the synthesis of these natural products. Members of PIAs ( eg., 2-7) which contain tetracyclic ring systems possessing characteristic cyclic guanidine or urea moieties show significant biological activities including anticancer activity and agonistic activity against the adrenoceptor. In this review investigations of the total synthesis of the representative tetracyclic PIAs dibromophakellin (2) and dibromophakellstatin (3) are described.


2011 ◽  
Vol 2011 ◽  
pp. 1-7 ◽  
Author(s):  
Xiao-hua Cai ◽  
Bing Xie ◽  
Hui Guo

The first cyclopenta[b]benzofuran derivative, rocaglamide, from Aglaia elliptifolia, was found to exhibit considerable insecticidal activities and excellent potential as a therapeutic agent candidate in cancer chemotherapy; the genus Aglaia has been subjected to further investigation. Both the structural complexity of rocaglamide and its significant activity make it an attractive synthetic target. Stereoselective synthesis of the dense substitution pattern of these targets is a formidable synthetic challenge: the molecules bear five contiguous stereocenters and cis aryl groups on adjacent carbons. In past years of effort, only a handful of completed total syntheses have been reported, evidence of the difficulties associated with the synthesis of rocaglate natural products. The advance on total synthesis of rocaglamide was mainly reviewed from intramolecular cyclization and biomimetic cycloaddition approach.


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