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An efficient procedure has been proposed for the synthesis of linear and angular phenyl-substituted dibenzonaphthyridines from anilinoquinolines and benzoic acid in up to 85% yield using Eaton?s reagent (a solution of phosphorous pentoxide in methanesulfonic acid) as condensing agent instead of polyphosphoric acid which previously afforded less than 50% yield of the same compounds. Apart from benzoic acid, ethyl benzoate and benzoyl chloride can be used in the synthesis of dibenzonaphthyridines according to the proposed procedure, but the yields are lower.

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A two step synthesis of 2-alkynyl-4-arylquinolines has been accomplished via Pd/C-mediated regioselective C-2 alkynylation of 2,4-dichloroquinoline in water followed by Suzuki coupling at C-4 of the resulting 4-chloro derivative.

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Our Top Choice Compound: Thiazolidin-2-one

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As a part of our ongoing studies in developing new derivatives as antimicrobial agents we describe the synthesis of novel substituted 5-benzylideno-2-adamantylthiazol[3,2-b][1,2,4]triazol-6(5H)ones.The twenty-five newly synthesized compounds were tested for their antimicrobial and antifungal activity. All compounds have shown antibacterial properties with compounds 1?9 showing the lowest activity, followed by compounds 10?14 while compounds 15?25 the highest antibacterial activity. Specific compounds appeared to be more active than ampicillin in most studied strains and in some cases more active than streptomycin. Antifungal activity in most cases also was better than that of reference drugs ketoconazole and bifonazole. Elucidating the relation of molecular properties to antimicrobial activity as well as generation of pharmacophore model for antifungal activity of two fungal species Aspergillus fumigatus and Candida albicans were performed.

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We live in a world with complex diseases such as cancer which cannot be cured with one-compound one-target based therapeutic paradigm. This could be due to the involvement of multiple pathogenic mechanisms. One-compound-various-targets stratagem has become a prevailing research topic in anti-cancer drug discovery. The simultaneous interruption of two or more targets has improved the therapeutic efficacy as compared to the specific targeted based therapy. In this review, six types of dual targeting agents along with some interesting strategies used for their design and synthesis are discussed. Their pharmacology with various types of the molecular interactions within their specific targets has also been described. This assemblage will reveal the recent trends and insights in front of the scientific community working in dual inhibitors and help them in designing the next generation of multi-targeted anti-cancer agents.

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Background: Thienopyrimidine, triazole and thiazolidinone derivatives have recently gained attention due to their effective pharmacological activities. They show antioxidant, antitumor, antimicrobial, antiviral, anti-inflammatory and analgesic properties. Objective: Synthesis of new ethyl 2-amino-4-isopropyl-5-methylthiophene-3-carboxylate (2) was used as a starting material to produce 2-mercapto-methylthienopyrimidinone (3), (4) and 2- hydrazinyl-methylthienopyrimidinone (5), through high yields and evaluating anticancer activities. Methods: A series of novel Schiff?s bases (6-9) were produced after treatment of (5) with aldehydes. Triazolopyrimidinones (6a, 7a, 8a, 9a) were produced from cyclization of benzylidene (6-9) using Br2 / AcOH or dry pyridine /Ac2O. Thiazolidinones (6b, 7b, 8b, 9b) were synthesized from benzylidene (6-9) with mercaptoacetic acid. Results: All the compounds were synthesized in good yields (55-85%) in a regularly actual system under mild condition. The new compounds have been established by means of diverse spectroscopic ways as IR, NMR and MS. The newly synthesized compounds were evaluated for their antiproliferative activity against the breast MCF-7 carcinoma cell line. Compound (7) showed promising anticancer activity with IC50 of 6.9 muM, and 40.8% of antioxidant effect as DPPH inhibition. Molecular docking of (7) showed deltaG values of-20.54 kcal/ mol and -25.60 kcal/ mol. Molecular dynamics simulation of (7) in complex with PARP-1 revealed RMSD of 3.00 a. Conclusion: The QSAR study confirmed the presence of a relationship between anticancer activity and subdivided surface area descriptors with coefficient r2 = 0.98 with high predictive power.

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Optimization of a lead series of PI3Kdeltainhibitors based on a dihydroisobenzofuran core led to the identification of potent, orally bioavailable compound 19. Selectivity profiling of compound 19 showed similar potency for class III PI3K, Vps34, and PI3Kdelta, and compound 19 was not well-tolerated in a 7-day rat toxicity study. Structure-based design led to an improvement in selectivity for PI3Kdeltaover Vps34 and, a focus on oral phramacokinetics properties resulted in the discovery of compound 41, which showed improved toxicological outcomes at similar exposure levels to compound 19.

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Provided are novel organic electroluminescent compounds and organic electroluminescent devices using the same. Since the organic electroluminescent compound exhibits good luminous efficiency and excellent life property compared to the existing material, it may be used to manufacture OLED devices having superior operation life and consuming less power due to improved power efficiency.

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The present invention relates to novel compounds of the general formula (I) STR1 wherein R means hydrogen or C1-4 alkyl group; and Y stands for cyano, trifluoromethyl, aryloxy or aryl(C1-4 alkyl)oxy group. The compounds according to the invention show a gastric acid secretion-inhibiting effect and therefore, they are useful for the treatment of gastric and duodenal ulcers. In addition, they exert a cytoprotective action against gastric laesions induced, e.g. by indomethacin or acid-containing alcohol.

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Abstract: Reaction of thiazolidin-2-cyanamide and substituted benzyl bromide compounds in acetonitrile at room temperature afforded the 3-(2?-substituted benzyl)thiazolidin-2-cyanamide derivatives 1?13 in good yields. Compounds 1?13 were characterized by proton nuclear magnetic resonance (1H NMR) and infrared spectroscopies, of which the structures of the isomeric o-, m-, and p-fluoro derivatives 4?6 were established by single crystal X-ray crystallography. Compound 4 crystallizes in the monoclinic space group P21/n, with a = 9.177(19), b = 8.551(18), c = 14.090(3) A, beta = 98.243(3), and Z = 4. The unit cell of 5 has a monoclinic P21/c symmetry with the cell parameters a = 9.289(2), b = 14.057(4), c = 8.574(2) A, beta = 100.350(3), and Z = 4. The unit cell of 6 also has a monoclinic P21/c symmetry with the cell parameters a = 9.333(4), b = 14.034(5), c = 8.508(3) A, beta = 99.15(5), and Z = 4. Graphic Abstract: A series of 3-(2?-substituted benzyl)thiazolidin-2-cyanamide derivatives were efficiently synthesized via the reaction of benzyl bromide compounds with thiazolidin-2-cyanamide, of which the structures of the isomeric o-, m-, and p-fluoro derivatives were characterized by X-ray crystallography. [Figure not available: see fulltext.]

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New Advances in Chemical Research, May 2021. COA of Formula: C3H7NO2S, Chemical engineers ensure the efficiency and safety of chemical processes, adapt the chemical make-up of products to meet environmental or economic needs, and apply new technologies to improve existing processes. In a document type is Patent, and a compound is mentioned, 5908-62-3, 1,1-Dioxo-isothiazolidine, introducing its new discovery.

The present invention provides a new use of a compound of formula (I) or a pharmaceutically acceptable salt or solvate salt thereof, wherein: G is selected from a group consisting of: phenyl, pyridyl, benzothiazolyl, indazolyl; p is an integer ranging from 0 to 5; R1 is independently selected from a group consisting of: halogen, hydroxyl, cyano, C1-4alkyl, haloC1-4alkyl, C1-4 alkoxy, haloC1-4alkoxy, C1-4alkanoyl; or corresponds to a group R5; R2 is hydrogen or C1-4 alkyl; R3 I s C1-4alkyl; R4 is hydrogen, or a phenyl group, a heterocyclyl group, a 5- or 6-membered heteroaromatic group, or a 8- to 11-membered bicyclic group, any of which groups is optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, C1-4alkanoyl; R5 is a moiety selected from the group consisting of: isoxazolyl, -CH2-N-pyrrolyl, 1,1-dioxido-2-isothiazolidinyl, thienyl, thiazolyl, pyridyl, 2-pyrrolidinonyl, and such a group is optionally substituted by one or two substituents selected from: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, C1-4alkanoyl; and when R1 is chlorine and p is 1, such R1 is not present in the ortho position with respect to the linking bond to the rest of the molecule; and when R1 corresponds to R5, p is 1; in the manufacture of a medicament for the treatment of a somatoform disorder such as body dysmorphic disorder or hyperchondriasis, bulimia nervosa, anorexia nervosa, binge eating, paraphilia and nonparaphilic sexual addictions, Sydeham’s chorea, torticollis, autism, a movement disorder including Tourette’s syndrome; and in the manufacture of a medicament for the treatment of premature ejaculation.

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