A series of carbamimidothioic acid phenylmethyl ester salts and their N,N'-tetramethyl derivatives were synthesized, many of which exert an interesting inhibiting action on Gram-positive and Gram-negative bacteria and also on fungi. This activity is noteworthy in view of the large number of strains antagonized; the (3,4,5-trichlorophenyl) methyl ester chloride of carbamimidothioic acid appeared to be the best term of the series. The possible influence on this activity of decomposition kinetics to the corresponding mercapto-derivatives was investigated and compared with that of a series of N,N'-tetramethyl derivatives of previously studied carbamimidothioic acid phenyl ester salts.
Download full-text PDF |
Source |
|---|
Publication Analysis
Top Keywords
Similar Publications
Absinthin, an agonist of the bitter taste receptor hTAS2R46, uncovers an ER-to-mitochondria Ca-shuttling event.
J Biol Chem
August 2019
Department of Health Sciences, School of Medicine, University of Piemonte Orientale, Via Solaroli, 17-28100 Novara, Italy. Electronic address:
Type 2 taste receptors (TAS2R) are G protein-coupled receptors first described in the gustatory system, but have also been shown to have extraoral localizations, including airway smooth muscle (ASM) cells, in which TAS2R have been reported to induce relaxation. TAS2R46 is an unexplored subtype that responds to its highly specific agonist absinthin. Here, we first demonstrate that, unlike other bitter-taste receptor agonists, absinthin alone (1 μm) in ASM cells does not induce Ca signals but reduces histamine-induced cytosolic Ca increases.
View Article and Find Full Text PDFCytotoxicity of the Urokinase-Plasminogen Activator Inhibitor Carbamimidothioic Acid (4-Boronophenyl) Methyl Ester Hydrobromide (BC-11) on Triple-Negative MDA-MB231 Breast Cancer Cells.
Molecules
May 2015
Dipartimento di Scienze e Tecnologie Biologiche, Chimiche e Farmaceutiche (STEBICEF), Edificio 16, Università di Palermo, Viale delle Scienze, 90128 Palermo, Italy.
BC-11 is an easily synthesized simple thiouronium-substituted phenylboronic acid, which has been shown to be cytotoxic on triple negative MDA-MB231 breast cancer cells by inducing a perturbation of cell cycle when administered at a concentration equal to its ED50 at 72 h (117 μM). Exposure of cells to BC-11, either pre-absorbed with a soluble preparation of the N-terminal fragment of urokinase-plasminogen activator (uPa), or in co-treatment with two different EGFR inhibitors, indicated that: (i) BC-11 acts via binding to the N-terminus of the enzyme where uPa- and EGF receptor-recognizing sites are present, thereby abrogating the growth-sustaining effect resulting from receptor binding; and (ii) the co-presence of the EGFR inhibitor PD153035 potentiates BC-11's cytotoxicity. Exposure of cells to a higher concentration of BC-11 corresponding to its ED75 at 72 h (250 μM) caused additional impairment of mitochondrial activity, the production of reactive oxygen species and promotion of apoptosis.
View Article and Find Full Text PDFSynthesis and anticancer activity of some novel trifluoromethylquinolines carrying a biologically active benzenesulfonamide moiety.
Eur J Med Chem
November 2013
Pharmacognosy Department, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi Arabia.
Several trifluoromethylquinoline derivatives containing a biologically active benzenesulfonamide moiety 2-14, 16, urea derivatives 15, 17, 4-isothiocyanate 18 and the corresponding carbamimidothioic acid derivatives 19-30, were synthesized from the strategic starting material 4-chloro-7-trifluoromethylquinoline 1. The structures of the newly synthesized compounds were elucidated on the basis of elemental and spectral analyses. All the prepared compounds were evaluated for their in vitro anticancer activity against various cancer cell lines.
View Article and Find Full Text PDFSomatic depolarization enhances GABA release in cerebellar interneurons via a calcium/protein kinase C pathway.
J Neurosci
April 2011
Laboratoire de Physiologie Cérébrale, Centre National de la Recherche Scientifique and Université Paris Descartes, 75006 Paris, France.
In cortical and hippocampal neurons, tonic somatic depolarization is partially transmitted to synaptic terminals, where it enhances transmitter release. It is not known to what extent such "analog signaling" applies to other mammalian neurons, and available evidence concerning underlying mechanisms is fragmentary and partially controversial. In this work, we investigate the presence of analog signaling in molecular layer interneurons of the rat cerebellum.
View Article and Find Full Text PDFReactivity toward cysteine of antimicrobial carbamimidothioic acid phenylalkylesters salts.
Boll Chim Farm
July 1991
Dipartimento di Scienze Farmaceutiche, University of Modena, Italy.
The rates of reaction toward cysteine of a series of carbamimidothioic acid phenylmethylesters halides were investigated in phosphate buffer pH 7.4 at 37 degrees C under pseudo-first-order conditions. The reaction involves nucleophilic attack of cysteine on the C-S bond of isothiouronium mojety and corresponding benzenemethanethiols were detected as product of the reaction.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!