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The Prelude of Green Syntheses of Drugs and Natural Products
Published in Ahindra Nag, Greener Synthesis of Organic Compounds, Drugs and Natural Products, 2022
Leonardo Xochicale-Santana, C. C. Vidyasagar, Blanca M. Muñoz-Flores, Víctor M. Jiménez Pérez
C–C couplings have also benefited from this tool called mechanochemistry; this has made it possible to synthesize intermediates and/or structures of numerous pharmaceuticals and drug candidates in a more ecological way compared to their traditional synthesis. In this context, indazoles are part of several drugs of medicinal interest that have shown therapeutic applications such as anticancer drugs, contraceptives, and protein inhibitors such as HIF-1a (hypoxia-inducible factor 1 alpha subunit). In various articles, it has been described that the functionalization of the pyrazole ring is carried out by using metal catalysts such as Rh (III),29 Cu (I),30 or palladium catalysts31; however, these reagents tend to be very expensive, in addition to using reaction conditions that make them more tedious. In contrast, a recent report published in 2019 by Su describes a methodology for the functionalization of the pyrrazole ring by a C–H/C–H coupling by mechanical chemistry using a palladium catalyst and a low-cost oxidizing agent with good product yields and wide tolerance of functional groups (Scheme 15.11).32
Microwave-Assisted Transition Metal-Catalyzed Synthesis of Pharmaceutically Important Heterocycles
Published in Banik Bimal Krishna, Bandyopadhyay Debasish, Advances in Microwave Chemistry, 2018
Dipti Shukla, Priyank Purohit, Asit K. Chakraborti
The versatile biological and pharmacological activities established indazoles as an important pharmacophoric feature. Moustafa et al. reported a convenient synthesis of indazole derivatives [82]. The strategy involves the reductive cyclization of the Schiff base o-nitro-benzylidine amine 110 with PPh3 in the presence of molybdenum catalyst in toluene under microwave irradiation to form the indazole derivatives 111 (Scheme 9.40). In this reaction, PPh3 acts as the reducing agent. The protocol also works in conventional heating, but in the microwave heating condition, the reaction rate was 30 times faster than that of the conventional heating condition.
Five new cobalt(II) complexes based on indazole derivatives: synthesis, DNA binding and molecular docking study
Published in Journal of Coordination Chemistry, 2019
Bing-Fan Long, Qin Huang, Shu-Long Wang, Yan Mi, Meng-Fan Wang, Ting Xiong, Shu-Cong Zhang, Xian-Hong Yin, Fei-Long Hu
Among several transition metal complexes used as synthetic hydrolases, Co(II) complexes are better suited for the hydrolysis of DNA due to their strong Lewis acid and redox properties to produce reactive oxygen species that ultimately cleave DNA, yielding direct strand scission. The interaction of cobalt(II) transition metal complexes containing a planar heterocyclic aromatic ligand with molecular target DNA is of particular interest for understanding their cytotoxic activities, owing to their tunable coordination geometry, versatile redox and spectroscopic properties [3]. The investigation on cobalt complexes as cancer chemotherapeutic agents arises due to their ability of redox-dependent targeting the malignant tissue of solid tumors. But beyond that, the reports reveal that cytotoxic properties of metal complexes are strongly dependent on the nature of the ligands. Indazole and their derivatives display interesting biological properties and powerful pharmacological activities [4], such as antibacterial and antifungal activities. Several indazoles are found to exhibit significant levels of activity as HIV protease inhibitors [5], serotonin 5-HT1α, 5-HT2 and 5-HT3 receptor antagonists, and aldose reductase inhibitors [6]. The indazole derivatives are also known to exhibit diverse bioactivities such as anticonvulsant [7], antidiarrheal, antihistaminic [8], antidiabetic, cardioprotective [9], and anticancer. The metallic drug based on indazole derivatives may significantly enhance the cytotoxic properties. On the other hand, the chelating ligand or tethering two different components of biologically significant pharmacophore with different modes of action modulate or tune the various metallo-pharmaceuticals to yield a wider spectrum of effective regime of chemotherapeutic agents [10]. The optimized chelating agents contain phen and 2,2′-bipy, which bear π-electron deficiency and can be observed as excellent π-acceptors capable of stabilizing metal ions in lower oxidation state. Owing to their unusual electronic properties, diverse chemical reactivity and peculiar structures, metal complexes with phen/2,2′-bipy based ligand have gained much importance in molecular recognition and sensing DNA binding/cleavage. The phen ring enhanced co-planarity is beneficial for binding DNA. Attaching methyl group on the plane ligands will increase its solubility when it coordinated to the metal ions, which will optimize the interaction between complex and DNA.