- Preparation method of clotrimazole
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The invention provides a preparation method of clotrimazole. The preparation method comprises the following steps: step 1, chlorinating (2-chlorphenyl) diphenyl methanol into (2-chlorphenyl) diphenylchloromethane; 2, subjecting (2-chlorphenyl) diphenyl chloromethane and imidazole to condensation to form clotrimazole; the total reaction flow formula is shown in the specification. The invention provides a preparation method of clotrimazole. The initial raw materials (2-chlorphenyl) diphenyl methanol and imidazole are easy to obtain and stable in performance; reaction condition mildness, a product which is unstable when meeting water and synthesized in step 1 does not need to be separated and purified, and can be applied directly in step 2, not only are the requirements on equipment and operation reduced, but also the risk of influencing the quality of the raw material medicine is reduced; the preparation method is simple in operation, short in process period, high in product purity andsuitable for industrial production, , in addition, the reaction solvent in the step 1 is also the reaction solvent in the step 2, emission of three wastes is reduced, and environmental protection is better facilitated.
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Paragraph 0027-0032; 0036-0041
(2020/07/28)
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- SURFACE ENHANCED RAMAN SPECTROSCOPY (SERS) COMPOUNDS AND METHODS OF THEIR PREPARATION
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A compound for detecting an analyte using Surface Enhanced Raman Spectroscopy (SERS) and a method of forming the compound is provided. The compound has Formula I: wherein W is selected from the group consisting of an optionally substituted aryl group and an optionally substituted heteroaryl group; each Y independently is NR1R2, wherein R1 and R2 are independently selected from the group consisting of H and C1-C6 alkyl, or R1 and R2 combine to form together with the nitrogen to which they are attached a heterocyclic group with 4 to 5 carbon atoms, is used to denote a single or a double bond, and Z is NH, NH2, NH—(C═O)—(CH2)n—SH, wherein n=1 to 10, or or a tautomer or stereoisomer thereof, or a salt thereof. A method and device for detecting an analyte using Surface Enhanced Raman Spectroscopy (SERS) is also provided.
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- COMBINATORIAL ROSAMINE LIBRARY AND USES THEREOF
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The present invention relates to a rosamine derivative compound, as described herein, having the following structure: Also disclosed are methods of making such compounds and for using them for detection and imaging.
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- Novel inhibitors of the gardos channel for the treatment of sickle cell disease
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Sickle cell disease (SCD) is a hereditary condition characterized by deformation of red blood cells (RBCs). This phenomenon is due to the presence of abnormal hemoglobin that polymerizes upon deoxygenation. This effect is exacerbated when dehydrated RBCs experience a loss of both water and potassium salts. One critical pathway for the regulation of potassium efflux from RBCs is the Gardos channel, a calcium-activated potassium channel. This paper describes the synthesis and biological evaluation of a series of potent inhibitors of the Gardos channel. The goal was to identify compounds that were potent and selective inhibitors of the channel but had improved pharmacokinetic properties compared to 1, Clotrimazole. Several triarylamides such as 10 and 21 were potent inhibitors of the Gardos channel (IC50 of 10 nM) and active in a mouse model of SCD. Compound 21 (ICA-17043) was advanced into phase 3 clinical trials for SCD.
- McNaughton-Smith, Grant A.,Burns, J. Ford,Stocker, Jonathan W.,Rigdon, Gregory C.,Creech, Christopher,Arlington, Susan,Shelton, Tara,De Franceschi, Lucia
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p. 976 - 982
(2008/12/20)
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- Non-peptide inhibition of T-lymphocyte activation and therapies related thereto
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Compounds, preparations and methods for immunosuppressive treatment of autoimmune disorders, graft rejection and/or graft/host disease. Therapeutically effective amounts of certain substituted triarylmethane compounds, such as 1-[(2-chlorophenyl)diphenylmethyl]-1H-pyrazole, are administered to mammalian patients to selectively inhibit the calcium-activated K + channel (IKCa1) in lymphocytes, monocytes, macrophages, platelets or endothelial cells without concomitant inhibition of P450-dependent enzyme systems, resulting in reduction of antigen-, cytokine-, or mitogen-induced calcium entry through store operated calcium channels in these cells, suppression of cytokine production by these cells, and inhibition of activation of these cells. Such inhibition of the Ca ++ activated K + channel (IKCa1) prevents the pre-Ca ++ stage of cell activation and thus causes immunosuppression and an anti-inflammatory response.
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- Tritylamino aromatic heterocycles and related carbinols as blockers of Ca2+-activated potassium ion channels underlying neuronal hyperpolarization
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A series of novel aromatic tritylamino heterocycles has been synthesized and the compounds have been tested in comparison with clotrimazole for their ability to inhibit the slow afterhyperpolarization current (SlAHP) in cultured rat hippocampal pyramidal neurones. Some analogues of the clotrimazole metabolite, 2-chlorophenyl-diphenyl methanol, having different chlorination substitution in the triphenyl group have also been examined. Two compounds in particular, 3-[(2-chlorophenyl)diphenylmethylamino]pyridine (3a, UCL 1880) and 2-tritylaminothiazole (6, UCL 2027), are of special interest; they are effective blockers of the SlAHP (IC50 = 1.1-1.2 μM) and are much more selective than clotrimazole since they have less effect on the high voltage-activated Ca2+ current.
- Zunszain, Patricia A.,Shah, Mala M.,Miscony, Zena,Javadzadeh-Tabatabaie, Mazyar,Haylett, Dennis G.,Ganellin, C. Robin
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p. 159 - 166
(2007/10/03)
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- Treatment of GLC1A glaucoma with non-steroidal glucocorticoid antagonists
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Compositions of non-steroidal glucocorticoid antagonists for treating GLC1A glaucoma and methods for their use are disclosed.
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- Synthesis and antifungal activity of a series of difluorotritylimidazoles
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1-[(2-Fluorophenyl)(4-fluorophenyl)phenylmethyl]-1H-imidazole (flutrimazole, UR-4056, CAS 119006-77-8) (15) was selected among a series of mono-, di- and trifluorotrityl-imidazole antifungal agents as the most potent fluorine containing analogue of clotrimazole.
- Bartroli,Alguero,Boncompte,Forn
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p. 832 - 835
(2007/10/02)
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