A series of highly potent thiourea inhibitors of cytomegalovirus (CMV) with improved stability properties was prepared and evaluated. Compound 29 inhibited the virus in cultured HFF cells with IC50 of 0.2 nM.
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http://dx.doi.org/10.1016/j.bmcl.2004.04.093 | DOI Listing |
Bioorg Chem
January 2025
Department of Chemistry, Indian Institute of Technology Indore, Indore 453552 India; Department of Biosciences and Biomedical Engineering, Indian Institute of Technology Indore, Indore 453552 India. Electronic address:
Prostate cancer (PCa) has emerged to be the second leading cause of cancer-related deaths in men. Molecular imaging of PCa using targeted radiopharmaceuticals specifically to PCa cells promises accurate staging of primary disease, detection of localized and metastasized tumours, and helps predict the progression of the disease. Glutamate urea heterodimers have been popularly used as high-affinity small molecules in the binding pockets of popular and well-characterized PCa biomarker, prostate specific membrane antigen (PSMA).
View Article and Find Full Text PDFJ Exp Biol
January 2025
University of Guelph, 50 Stone Rd E, Guelph, N1G 2M7, Canada.
The timing of metamorphosis and settlement is critical for the survival and reproductive success of marine animals with biphasic life cycles. Thyroid hormones (THs) regulate developmental timing in diverse groups of chordates, including the regulation of metamorphosis in amphibians, teleosts, lancelets, tunicates, and lampreys. Recent evidence suggests a role for TH regulation of metamorphosis outside of the chordates, including echinoderms, annelids, and molluscs.
View Article and Find Full Text PDFVirusdisease
December 2024
Department of Molecular and Cellular Medicine, Institute of Liver and Biliary Sciences, D-1, Vasant Kunj, New Delhi, 110 070 India.
Unlabelled: Antivirals such as nucleotide analogs (NAs) are potent inhibitors of hepatitis B virus (HBV) replication. However, NAs fail to diminish the signaling and mitogenic activities of the transactivator HBx protein. Earlier we have shown that thiourea derivative IR-415 (DSA-00) targeted HBx to down-regulate its target viral and host genes.
View Article and Find Full Text PDFFuture Med Chem
December 2024
Department of Pharmacology and Toxicology, College of Pharmacy King Saud University, Riyadh, Saudi Arabia.
Aims: Current research work aims to synthesize hybrid compounds with a thiazole-thiazolidinone structure, as potent inhibitors of urease and α-glucosidase enzymes.
Materials And Methods: These compounds were characterize throughHNMR,CNMR and HREI-MS techniques. These compounds were also evaluated for their potential to inhibit urease and α-glucosidase enzymes for the treatment of urinary tract infections (UTIs) and diabetes treatments.
Heliyon
October 2024
Department of Chemistry, College of Science, Qassim University, Buraidah, 51452, Saudi Arabia.
Herein, a novel set of imidazo-isoxazole derivatives containing thiourea and urea scaffolds were synthesized, characterized (H NMR, C NMR, and elemental analysis). These compounds were biologically evaluated for their α-amylase and α-glucosidase inhibitory activity, identifying as the most active (IC 26.67 ± 1.
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