Schiff bases of isatin with aminothiazole, its N-mannich bases and Spiro isatin derivatives were synthesized. Their chemical structures were confirmed by Infrared, 1H-Nuclear Magnetic Resonance data and elemental analysis. Antimicrobial evaluation was performed by the agar diffusion method against four pathogenic bacteria and two pathogenic fungi. Anti-inflammatory activity was tested by carragenin-induced rat paw edema and compounds were evaluated for analgesic action by the acetic acid-induced writhing method; Compounds Aa, Ab and A5, A6 were found to be active against bacteria and fungi. The compounds A3, A6, Aa and Ab showed anti-inflammatory activity, having a percentage protection value of 34.69, 32.65, 38.77 and 36.73 as compared with that of indomethacin, with % protection of 46.93. Similarly, the compounds Aa, Ab and A6 showed analgesic activity, with % protection of 67.51, 64.78 and 49.81 as compared with the standard with % protection of 79.56.
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http://dx.doi.org/10.4103/0975-1483.63164 | DOI Listing |
J Contemp Dent Pract
May 2024
Department of Pediatric and Preventive Dentistry, Saveetha Dental College and Hospital, Saveetha Institute of Medical and Technical Sciences, Saveetha University, Chennai, Tamil Nadu, India.
Aim And Objectives: To characterize and analyze the structural presentation of a new denture base copolymer with a spiro-acetal cross-linker at 10 and 20 wt.% concentrations by nuclear magnetic resonance (NMR) and field emission scanning electron microscopy-energy-dispersive X-ray (FESEM-EDX) spectroscopies. Also, to evaluate the glass transition temperature (T) of the new copolymer.
View Article and Find Full Text PDFAngew Chem Int Ed Engl
October 2024
Department of Chemistry, Aarhus University, 8000, Aarhus C, Denmark.
The substituted tetrahydrofuran core is a structural motif in many biologically active and natural compounds. However, the scarcity of enantioselective methods developed towards its synthesis makes this field challenging and attractive to explore. Herein, the first Brønsted-base catalyzed enantioselective (3+2) annulation of donor-acceptor cyclopropanes with aldehydes and ketones affording enantioenriched 2,3,5-substituted tetrahydrofurans is reported.
View Article and Find Full Text PDFJ Org Chem
March 2024
Saint Petersburg State University, Saint Petersburg 199034, Russian Federation.
Herein, we report the study of the thermally promoted reaction of 3-diazotetramic acids with imines as a rapid route to a novel spiro heterocyclic scaffold, spiro bis-β-lactams (2,6-diazaspiro[3.3]heptane-1,5-diones). The transformation proceeds via metal-free microwave-assisted Wolff rearrangement of the diazo reagent followed by Staudinger [2+2] cycloaddition of the heterocyclic ketenes with Shiff bases.
View Article and Find Full Text PDFMol Divers
December 2024
Department of Chemistry, National Institute of Technology Warangal, Hanamkonda, Telangana, 506004, India.
The development of anti-tuberculosis (anti-TB) drugs has become a challenging task in medicinal chemistry. This is because Mycobacterium tuberculosis (TB), the pathogen that causes tuberculosis, has an increasing number of drug-resistant strains, and existing medication therapies are not very effective. This resistance significantly demands new anti-TB drug profiles.
View Article and Find Full Text PDFNat Prod Res
August 2024
Department of Chemistry, College of Science, University of Baghdad, Baghdad, Iraq.
Spiro-5-nitro isatino aza-β-lactams were produced by a [2 + 2] cycloaddition of 5-nitro isatin Schiff bases [1-5] with different aromatic isocyanate and thioisocyanate. 1HNMR and 13CNMR as well as FTIR spectroscopies, were used to identify the structures of the obtained compounds. These spiro-5-nitro isatin aza- β-lactams interest to us due to their potential antioxidant and anticancer properties.
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