Novel pseudonucleosides with benzylamino group on 5'-position (4) were synthesized by using the microwave-assisted one-pot tandem Staudinger/aza-Wittig/reduction reaction in good yields of 55.2-71.7%. The deacetylation of 4 afforded compounds 5. HIV-1 reverse transcriptase (RT) inhibitory and antitumor activities were preliminarily evaluated with 5. The results showed that the new pseudonucleosides (5) could effectively inhibit HIV-1 RT activity, but no antitumor activity.
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http://dx.doi.org/10.1016/j.bmcl.2010.10.054 | DOI Listing |
ChemistryOpen
January 2025
Discipline of Pharmaceutical Sciences, Catalysis and Peptide Research Unit, University of KwaZulu-Natal, Durban, 4000, South Africa.
An efficient microwave-assisted synthesis route for novel oxazolidinone analogues has been developed. The general synthesis of these compounds began with an L-proline-mediated three-component Mannich reaction between commercially available 3-fluoro-4-morpholinoaniline, aqueous formaldehyde and α-hydroxyacetone. This was followed by a one-step cyclisation to form the core structure of oxazolidinone antibiotics which was subsequently derivatized.
View Article and Find Full Text PDFChem Biodivers
January 2025
Department of Pharmaceutical Chemistry, MM College of Pharmacy, Maharishi Markandeshwar (Deemed to be University), Ambala, India.
Quinolone antibiotics are a crucial class of synthetic antibacterial agents, widely utilized due to their broad spectrum of antibacterial activity. Due to the development of antimicrobial resistance, the potency of quinolone drugs decreased. Many conventional methods have been developed to elevate amination rate and to improve yield.
View Article and Find Full Text PDFCurr Top Med Chem
January 2025
Department of Pharmaceutical Chemistry, JSS College of Pharmacy, JSS Academy of Higher Education & Research (JSS AHER), Mysuru, Karnataka, India.
Background: Several chemical studies described the physiological efficacy of 1,4- dihydropyridines (DHPs). DHPs bind to specific sites on the α1 subunit of L-type calcium channels, where they demonstrate a more pronounced inhibition of Ca2+ influx in vascular smooth muscle compared to myocardial tissue. This selective inhibition is the basis for their preferential vasodilatory action on peripheral and coronary arteries, a characteristic that underlies their therapeutic utility in managing hypertension and angina.
View Article and Find Full Text PDFOrg Lett
January 2025
Department of Chemistry, Indian Institute of Technology Hyderabad, Kandi 502 284, Sangareddy District, Telangana, India.
This study demonstrates quick access to heteroatom-embodied complex fused polycyclic frameworks through a palladium-catalyzed domino process facilitated by microwave-assisted crossover annulation of -alkynylarylhalides and dihydrobenzofurans derivatives. The overall success of this process lies in the careful design of dihydrobenzofuran precursors that direct the initial palladium-mediated annulation step to proceed in a highly regioselective manner to furnish a single regioisomeric product. Notably, this one-pot method has witnessed good substrate scope and has furnished products with excellent yields.
View Article and Find Full Text PDFRSC Adv
December 2024
Bioorganic Laboratory, Department of Chemistry, University of Delhi Delhi-110007 India
A synthesis of a small library of fluorescent 1,4-dihydropyridine nucleoside analogues has been successfully carried out under solvent-free conditions a one-pot three-component Hantzsch condensation reaction. The process involved a Ba(NO) catalyzed solvent-free reaction between 3',5'-di--acetyl-5-formyl-2'-deoxyuridine, differently substituted β-keto ester and ammonium acetate under microwave irradiation. This facile methodology yielded the desired products with very high yields (86-96%) under solvent-free reaction conditions in a short reaction time, which was followed by a simple workup.
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