Studies on Some New Ru(III) Complexes Using aryl-azo Pentane- 2,4-dione and 2,6-bis (2'-Benzimidazolyl) Pyridine as Ligands: Synthesis, Spectroscopic, Luminescent, Electrochemical and Biological Activities

Some ruthenium(III) complexes with aryl-azo 2,4-pentanedione as co-ligands (L1H - L3H2) have been synthesized and characterized spectroscopically IR, 1H NMR, UV/Vis, ESR, conductimetric) along with elemental analysis and FAB-mass data. Their luminescent and redox properties have been studied. The antibacterial, anti-HIV and antitmnour activities have also been reported

Exploring new bio-active Ru(II) polypyridyl complexes through their interaction with DNA

660-663Complexes of multifunctional ligands 4- amino-3-hydrazino-5-mercapto- 1 ,2,4- triazole (L 1H2) and triazolo-2,4-pentanedione (L2H) with Ru(II)-2,2'bipyridyl have been prepared and characterized by IR, 1H NMR and UV/Vis spectral data in addition to their elemental analysis and FAB mass data. These have been allowed to interact with aqueous buffered solution of calf thymus DNA and the interaction has been monitored by UVNis-spectral data. Based on such interaction, the ligands and their Ru(II) complexes have been investigated for their cytotoxicity against various tumor cells and for anti - HVV (human immuno deficiency virus) activities

Binding of Ru(II) polypyridyl complexes with DNA

913-928In the present review salient features of ruthenium nucleic acid binding and factors governing the binding affinity with different forms of DNA are presented. Attempts are also made to explore the mode of binding through spectroscopic techniques and correlation of spectroscopic parameters in the presence and absence of DNA

Spectroscopic, luminescent, electrochemical and antibacterial activity of <span style="font-size:14.0pt;font-family:"Times New Roman";mso-fareast-font-family: "Times New Roman";mso-ansi-language:EN-US;mso-fareast-language:EN-US; mso-bidi-language:AR-SA">aryl/azolo 2,4-pentanediones and their Ru(II)-2,2'-bipyridyl complexes</span>

339-345Mononuclear and dinuclear Ru(II) 2,2'-bipyridyl complexes with some aryl/heterocyclic diazo 2,4-pentanediones have been synthesized and characterized by their elemental analyses and spectral (IR, UV/visible, 1H/13C NMR and FAB mass) data. Luminescent and electrochemical studies of the complexes are also reported. Antibacterial activity of the free ligands and their complexes evaluated against Pseudomonas aeruginosa has been correlated with the change in their absorbances in the presence and absence of the buffered aqueous solution of calf thymus DNA

Toward a Practical, Nonenzymatic Process for Investigational COVID-19 Antiviral Molnupiravir from Cytidine: Supply-Centered Synthesis

A scalable four-step synthesis of molnupiravir from cytidine is described herein. The attractiveness of this approach is its fully chemical nature involving inexpensive reagents and more environmentally friendly solvents such as water, isopropanol, acetonitrile, and acetone. Isolation and purification procedures are improved in comparison to our earlier study as all intermediates can be isolated via recrystallization. The key steps in the synthesis, namely, ester formation, hydroxyamination, and deprotection were carried out on a multigram scale to afford molnupiravir in 36-41% yield with an average purity of 98 wt % by qNMR and 99 area% by HPLC

Application of Chiral Transfer Reagents to Improve Stereoselectivity and Yields in the Synthesis of the Antituberculosis Drug Bedaquiline

Bedaquiline (BDQ) is an important drug for treating multidrug-resistant tuberculosis (MDR-TB), a worldwide disease that causes more than 1.6 million deaths yearly. The current synthetic strategy adopted by the manufacturers to assemble this molecule relies on a nucleophilic addition reaction of a quinoline fragment to a ketone, but it suffers from low conversion and no stereoselectivity, which subsequently increases the cost of manufacturing BDQ. The Medicines for All Institute (M4ALL) has developed a new reaction methodology to this process that not only allows high conversion of starting materials but also results in good diastereo- and enantioselectivity toward the desired BDQ stereoisomer. A variety of chiral lithium amides derived from amino acids were studied, and it was found that lithium (R)-2-(methoxymethyl)pyrrolidide, obtained from d-proline, results in high assay yield of the desired syn-diastereomer pair (82%) and with considerable stereocontrol (d.r. = 13.6:1, e.r. = 3.6:1, 56% ee), providing BDQ in up to a 64% assay yield before purification steps toward the final API. This represents a considerable improvement in the BDQ yield compared to previously reported conditions and could be critical to further lowering the cost of this life-saving drug