- Diazinium salts with dihydroxyacetophenone skeleton: Syntheses and antimicrobial activity
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Herein we report a feasible study concerning syntheses, structure and antimicrobial activity of some new diazinium salts with dihydroxyacetophenone skeleton. A fast, general, environmentally friendly, and facile method for preparation of diazinium salts under microwave and ultrasounds irradiation is presented. Antimicrobial tests prove that some diazine compounds have a remarkable activity against different microorganisms (germs and fungi), the pyrimidine derivatives being more active. Correlations between structure and antimicrobial activity are reported.
- Balan, Ana Maria,Florea, Ondina,Moldoveanu, Costel,Zbancioc, Gheorghita,Iurea, Dorina,Mangalagiu, Ionel I.
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- Imidazolylacetophenone oxime-based multifunctional neuroprotective agents: Discovery and structure-activity relationships
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Alzheimer's disease (AD) possesses a complex pathogenetic mechanism. Nowadays, multitarget agents are considered to have potential in effectively treating AD via triggering molecules in functionally complementary pathways at the same time. Here, based on the screening (～1400 compounds) against neuroinflammation, an imidazolylacetophenone oxime ether (IOE) was discovered as a novel hit. In order to obtain SARs, a series of imidazolylacetophenone oxime derivatives were constructed, and their C=N bonds were confirmed as the Z configuration by single crystals. These derivatives exhibited potential multifunctional neuroprotective effects including anti-neuroin?ammatory, antioxidative damage, metal-chelating, inhibition of acetylcholinesterase (AChE) properties. Among these derivatives, compound 12i displayed the most potent inhibitory activity against nitric oxide (NO) production with EC50 value of 0.57 μM 12i can dose-dependently suppress the expression of iNOS and COX-2 but not change the expression of HO-1 protein. Moreover, 12i exhibited evidently neuroprotective effects on H2O2-induced PC12 cells damage and ferroptosis without cytotoxicity at 10 μM, as well as selectively metal chelating properties via chelating Cu2+. In addition, 12i showed a mixed-type inhibitory effect on AChE in vitro. The structure-activity relationships (SARs) analysis indicated that dioxolane groups on benzene ring and rigid oxime ester can improve the activity. Parallel artificial membrane permeation assay (PAMPA) also verified that 12i can overcome the blood-brain barrier (BBB). Overall, this is the ?rst report on imidazolylacetophenone oxime-based multifunctional neuroprotective effects, suggesting that this type of compounds might be novel multifunctional agents against AD.
- Ren, Bo,Guo, Cong,Liu, Run-Ze,Bian, Zhao-Yuan,Liu, Rong-Chun,Huang, Lan-Fang,Tang, Jiang-Jiang
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- Preparation method of isoproterenol hydrochloride
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The invention relates to the technical field of raw material medicine synthesis, in particular to a preparation method of isoproterenol hydrochloride. According to the preparation method, water, N, N-dimethylformamide or an aqueous solution of N, N-dimethylformamide is used as a solvent, borohydride is used as a reducing agent to carry out reduction reaction on isopropyladrenolone or salt thereof, the reaction conditions are mild, compared with a conventional hydrogenation reduction process, the production safety is remarkably improved, the production cost is greatly reduced, the usage amount of borohydride is small, and the environmental protection is improved to a certain extent. The product obtained by the preparation method is very high in purity, is suitable for industrial production of isoprenaline hydrochloride as a medicine raw material medicine product, and can effectively avoid toxic and side effects caused by impurities.
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Paragraph 0008; 0029-0032
(2021/05/01)
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- Acetophenone oxime ester imidazole derivative as well as preparation method and application thereof
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The invention relates to the technical field of acetophenone oxime ester imidazole derivatives. The invention designs a series of novel (E)-1 - (2, 2 -dimethyl benzo [d] [1, 3] dioxol -5 - base) -2 - (1H - imidazol -1 -yl) -1 -ketoxime ester imidazole derivatives and further explores the interaction between the molecular structure and the inhibitory activity of the compound for LPS-induced neuroinflammation, and Developed new drugs for's disease provide experimental and theoretical basis.
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Paragraph 0032-0037; 0094-0098; 0109-0113
(2021/09/26)
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- Production process of adrenal glands
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The invention discloses a production technology for carbazochrome. The production technology comprises the following steps: 1) synthesizing chloracetyl catechol; 2) synthesizing corticosterone hydrochloride; 3) synthesizing adrenaline; and 4) synthesizing the carbazochrome. The production technology for the carbazochrome, disclosed by the invention, has the advantages of simple preparation method,few steps and easiness for operation and control; and an obtained product has good color and luster, good quality, high purity and high yield, can be directly used for production and utilization andhas very good practicability.
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Paragraph 0028-0030
(2021/11/15)
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- A three-step, gram-scale synthesis of hydroxytyrosol, hydroxytyrosol acetate, and 3,4-dihydroxyphenylglycol
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Hydroxytyrosol and two other polyphenols of olive tree, hydroxytyrosol acetate and 3,4-dihydroxyphenylglycol, are known for a wide range of beneficial activities in human health and prevention from diseases. The inability to isolate high, pure amounts of these natural compounds and the difficult and laborious procedures for the synthesis of them led us to describe herein an efficient, easy, cheap, and scaling up synthetic procedure, from catechol, via microwave irradiation.
- Kalampaliki, Amalia D.,Giannouli, Vassiliki,Skaltsounis, Alexios-Leandros,Kostakis, Ioannis K.
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- Preparation method of 3,4-dihydroxy-2'-chloroacetophenone
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The invention belongs to the field of chemical synthesis, and particularly relates to a preparation method of 3,4-dihydroxy-2'-chloroacetophenone. Catechol is used as an initial raw material to reactwith chloroacetic acid in thionyl chloride to obtain a mixture containing 3,4-dihydroxy-2'-chloroacetophenone; after the reaction is finished, a certain amount of water is added for a quenching reaction; and then recrystallizing is directly carried out to obtain a product with puritiy of 99% or above. The technological process has a simple reaction and post-treatment operation, and the product hashigh quality and can meet use requirements without the need of further purification. The process is green, environment friendly, safe, reliable, economical and practical, and is very suitable for industrial production.
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Paragraph 0034-0039
(2019/12/31)
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- PROCESS FOR PREPARATION OF ISOPROTERENOL HYDROCHLORIDE
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The present invention provides a process for preparation of isoproterenol hydrochloride (1a) comprising catalytic hydrogenation of 3',4'-dihydroxy-2-(isopropylamino)-acetophenone hydrochloride (5a) in presence of an ion exchange resin, to provide isoproterenol hydrochloride (1a).
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Page/Page column 8
(2018/07/31)
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- Cascade Trisulfur Radical Anion (S3?-) Addition/Electron Detosylation Process for the Synthesis of 1,2,3-Thiadiazoles and Isothiazoles
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Trisulfur radical anion (S3?-) mediated reactions with in situ formed azoalkenes and α,β-usaturated N-sulfonylimines for the construction of 1,2,3-thiadiazoles and isothiazoles has been developed. S3?- is in situ generated from potassium sulfide in DMF. These two approaches provide a new, safe, and simple way to construct 4-subsituted 1,2,3-thiadiazoles, 5-subsituted 1,2,3-thiadiazoles, and isothiazole in good yields. The reactions include the formation of the new C-S and N-S bonds via S3?- addition and electron detosylation under mild conditions.
- Liu, Bei-Bei,Bai, Hui-Wen,Liu, Huan,Wang, Shun-Yi,Ji, Shun-Jun
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p. 10281 - 10288
(2018/07/25)
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- Synthesis and in-vitro evaluation of 2-amino-4-arylthiazole as inhibitor of 3D polymerase against foot-and-mouth disease (FMD)
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Foot-and-mouth disease (FMD) is a highly contagious vesicular disease of livestock caused by a highly variable RNA virus, foot-and-mouth disease virus (FMDV). One of the targets to suppress expansion of and to control FMD is 3D polymerase (FMDV 3Dpol). In this study, 2-amino-4-arylthiazole derivatives were synthesized and evaluated for their inhibitory activity against FMDV 3Dpol. Among them, compound 20i exhibited the most potent functional inhibition (IC50 = 0.39μM) of FMDV 3D polymerase and compound 24a (EC50=13.09 μM) showed more potent antiviral activity than ribavirin (EC50=1367 μM) and T1105 (EC50=347 μM) with IBRS-2 cells infected by the FMDV O/SKR/2010 strain.
- Jeong, Kwi-Wan,Lee, Jung-Hun,Park, Sun-Mi,Choi, Joo-Hyung,Jeong, Dae-Youn,Choi, Dong-Hwa,Nam, Yeonju,Park, Jong-Hyeon,Lee, Kwang-Nyeong,Kim, Su-Mi,Ku, Jin-Mo
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p. 387 - 397
(2015/09/01)
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- Discovery and characterization of novel imidazopyridine derivative CHEQ-2 as a potent CDC25 inhibitor and promising anticancer drug candidate
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Cell division cycle (CDC) 25 proteins are key phosphatases regulating cell cycle transition and proliferation via the interactions with CDK/Cyclin complexes. Overexpression of CDC25 proteins is frequently observed in cancer and is related to aggressiveness, high-grade tumors and poor prognosis. Thus, inhibiting CDC25 activity in cancer treatment appears a good therapeutic strategy. In this article, refinement of the initial hit XDW-1 by synthesis and screening of a focused compound library led to the identification of a novel set of imidazopyridine derivatives as potent CDC25 inhibitors. Among them, the most potent molecule was CHEQ-2, which could efficiently inhibit the activities of CDC25A/B enzymes as well as the proliferation of various different types of cancer cell lines in vitro assay. Moreover, CHEQ-2 triggered S-phase cell cycle arrest in MCF-7, HepG2 and HT-29 cell lines, accompanied by generation of ROS, mitochondrial dysfunction and apoptosis. Besides, oral administration of CHEQ-2 (10 mg/kg) significantly inhibited xenografted human liver tumor growth in nude mice, while demonstrated extremely low toxicity (LD50 > 2000 mg/kg). These findings make CHEQ-2 a good starting point for further investigation and structure modification.
- Song, Yu'Ning,Lin, Xiaoqian,Kang, Dongwei,Li, Xiao,Zhan, Peng,Liu, Xinyong,Zhang, Qingzhu
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p. 293 - 307
(2014/06/24)
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- Synthesis and molecular structure of 1-(Pyrimidin-2-yl)-2-(4-aryl-1,3- thiazol-2-yl)hydrazines
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Reactions of some 2-hydrazinopyrimidine hydrochlorides with potassium thiocyanate gave 1-(pyrimidin- 2-yl)thiosemicarbazides which underwent Hantzsch condensation with aryl chloromethyl ketones to produce 1-(pyrimidin-2-yl)-2-(4- aryl-1,3-thiazol-2-yl)hydrazine hydrochlorides. The protonation was accompanied by mutually dependent tautomeric rearrangements of heterocyclic fragments. Pleiades Publishing, Ltd., 2011.
- Erkin,Krutikov
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experimental part
p. 1699 - 1704
(2011/12/03)
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- PROCESSES FOR THE PREPARATION OF EPINEPHRINE
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The invention relates to efficient and cost effective processes for the preparation of pure (-)- epinephrine. More particularly, it relates to processes for the resolution of racemic epinephrine.
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Page/Page column 6; 7
(2009/03/07)
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- PROCESS FOR THE PREPARATION OF HYDROXYTYROSOL
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Process for the preparation of hydroxytyrosol, characterized by reacting 4- chloroacetyl-catechol with a metal formate and formic acid in an aqueous solvent optionally containing a lower alkanol and catalytically hydrogenating the 4- hydroxyacetyl-catechol obtained in the presence of a precious metal, preferably on a carrier.
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Page/Page column 4-5
(2008/12/07)
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- Phenacylpyridiniothiocephalosporins
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An antibacterial 3-vic-dihydroxyaroylmethylpyridiniothiomethyl cephalosporin (I) and its salts represented by the following formula: STR1 (wherein, R1 is amino group or acylamino; R2 is hydrogen or methoxy; R3 is hydrogen atom or substituent; R4 is vic-dihydroxyaryl; R5 is straight or branched lower alkylene; R6 is hydrogen, a carboxy-protecting group or combined with Y a negative charge; X is --O--, --S-- or sulfinyl; and Y is a counter-ion of pyridinio or combined with R6 a negative charge), a disinfecting and treating method of bacterial infection using it, and synthetic methods thereof are provided.
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- Cephalosporin derivatives, and antibacterial agents
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A compound having the formula: STR1 wherein R is a straight chain or branched chain lower alkyl, cyclic lower alkyl, lower alkenyl (except for 1-carboxy-1-vinyl), lower alkynyl, aralkyl, phenyl or 2-pyrrolidon-3-yl group which may be substituted, and Q is STR2 (wherein R1 is a hydrogen atom or an acetyl group, R2 is a hydrogen atom, a carboxyl group or a carboxymethyl group, Y is a sulfur atom or an oxygen atom, Z is a sulfur atom, an oxygen atom or an imino group which may be substituted by a lower alkyl group); or a pharmaceutically acceptable salt, physiologically hydrolyzable ester or solvate thereof.
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- Pyridazine derivatives having a psychotropic action and compositions
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This invention relates to pyridazine derivatives substituted in the 4-position by a cyano group having psychotropic activity. It also relates to a process for the preparation of these products and their application as medicaments. STR1
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- N-(4-Substituted-thiazolyl)oxamic Acid Derivatives, a New Series of Potent, Orally Actve Antiallergy Agents
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A series of N-(4-substituted-thiazolyl)oxamic acid derivatives were synthesized and tested for antiallergy activity in the rat PCA model.These compounds were conveniently prepared by treatment of the appropriate acetophenone with thiourea and iodine or by reaction of the chloroacetylbenzene with thiourea to give the corresponding aminothiazoles; subsequent condensation with ethyloxalyl chloride gave the thiazolyloxamates.Many of the analogues showed a 50percent inhibition at oxamic acid ethanolamine salt (61, PRH-836-EA), has been selected for further pharmacological evaluation.
- Hargrave, Karl D.,Hess, Friedrich K.,Oliver, James T.
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p. 1158 - 1163
(2007/10/02)
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