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Isoxazole?a potent pharmacophore

Isoxazole is an azole with an oxygen atom next to the nitrogen. Isoxazole rings are found in some natural products, such as ibotenic acid and also found in a number of drugs, including COX-2 inhibitor valdecoxib. Furoxan, a nitric oxide donor is containing isoxazolyl group and found in many beta-lactamase resistant antibiotics, such as cloxacillin, dicloxacillin and flucloxacillin. The synthetic androgenic steroid danazol also has an isoxazole ring. The substituted isoxazoles are well developed in literature to possess significant biological activities. The disubstituted and trisubstituted isoxazoles have been reported to exhibit broad range of biological activities such as antimicrobial activity, analgesic activity, anti-inflammatory activity, antioxidant activity, anticancer activity, CNS (central nervous system) activity, antitubercular activity and miscellaneous activities like GABA (gamma-amino butyric acid) agonistic activity, inhibitory activity, antihypertensive activity, and glutamate transporter activity. The present review summarizes up to date information of various biological activities of isoxazole analogs.

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Sulfur containing acridine derivatives in preclinical studies with cancer cell lines

Background: The possible use of acridines as anticancer agents was first considered in the 1920?s. Since then, a large number of acridine drugs have been tested as antitumour agents, including compounds containing sulphur on the acridine chromophore. In this review, we will discuss recent studies which have investigated the anticancer activity of this class of acridine derivatives. Methods: We present the results both of our own decade-long research and also of existing research literature into the anticancer activity of acridine derivatives containing sulphur. The evidence of specific tumor-cell killing properties displayed by these compounds suggest the potential of using such molecules as anticancer therapeutics. Results: During the last decade, a number of acridine analogs have been developed by modifying the position and the nature of the substituent on the acridine core. In this paper, we published results on the anticancer activity of acridine derivatives containing sulfur (acridine thioureas, acridine thiazolidine/thiazoidinone, and acridine thiosemicarbazones/ thiosemicarbazides). In cancer chemotherapy, the mechanism of the drugs is complex, although the study of the anticancer activity of acridines has yielded exciting results. Conclusion: In this review we have summarized recent literature on the anticancer activity of acridine derivatives containing sulfur. A considerable amount of published data suggests that these compounds exhibit promising anticancer activity against selected cancer cell lines. The obtained results can be helpful in the development of new pharmaceutical agents.

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Highly Enantioselective Claisen-Type Acylation and Dieckmann Annulation

Enantioselective Claisen condensation reactions between various esters 1a-f and 3-acyl-4(S)-IPTT 2a,b employing lithium isopropylcyclohexylamide and HMPA gave acylated products 3a-j in 29-77percent yield and in 22-97percent ee.Asymmetric Dieckmann-type annulation of 4a with KH in DMF followed by methanolysis afforded bicyclic beta-keto methyl ester 6a in 69percent overall yield and in 96percent ee.

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Awesome Chemistry Experiments For 1,1-Dioxo-isothiazolidine

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COMPOUNDS AND METHODS FOR ANTIVIRAL TREATMENT

Compounds and pharmaceutically acceptable salts and esters and compositions thereof, for treating viral infections are provided. The compounds and compositions are useful for treating Pneumovirinae virus infections. The compounds, compositions, and methods provided are particularly useful for the treatment of Human respiratory syncytial virus infections

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Extended knowledge of 2-Cyanoimino-1,3-thiazolidine

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An antibiotic anticancer activity method for the preparation of compounds (by machine translation)

An antibiotic anticancer active compound preparation method, comprising: cooling the ice, compound HRB-1365-0 : C4H6N2 S2, compound HRB-1365-1 : C2H7NS, and water, stirring reaction in alkaline conditions, filtration to obtain white solid, that is, for the compound HRB-1365-2 : C4H5N3S; under ice cooling, compound HRB-1365-2 : C4H5N3S, compound HRB-1365-1 : C2H7NS, triethylamine, stirring reaction in the methanol, after the completion of reaction, methanol concentrated under reduced pressure, the residue is washed with water, filtered, to obtain yellow solid is the compound HRB-1365: C6H9N3 S2; compound HRB-1365: C6H9N3 S2 of ethanol solution under stirring in the ice bath to cool down, to the drying to obtain the hydrogen chloride gas is introduced, after the saturation, continuing to stir, filtering and drying the obtained product. (by machine translation)

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Simple exploration of (R)-Ethyl thiazolidine-4-carboxylate hydrochloride

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Chiral ferrocenylthiazolidines, new ligands for palladium complexes

The reaction of ferrocene with methyl or ethyl esters of L-cysteine in the presence of paraformaldehyde is studied. This process yields the optically pure derivatives: methyl or ethyl (R)-3-(ferrocenylmethyl)thiazolidine-4-carboxylates (1a or 1b), together with the corresponding N,N-bisthiazolidine derivatives (2a or 2b). When the reaction was carried out using the ethyl ester of L-cysteine, small amounts (ca. 9%) of the 1,1′-disubstituted ferrocene derivative (3b) were also isolated. The reactivity of compounds 1 versus palladium(II) species is studied, and has allowed us to isolate and characterise: [Pd(eta3-C3H5)Br(1a)] (4a) and [Pd(eta3-C3H5)Br(1b)] (4b), in which the ferrocenyl ligand behaves as a monodentate S-donor group. Compounds 4 evolve in the presence of dimethylsulfoxide to produce: [Pd(eta1-C3H5)Br(1)(dmso)] (5) in which the palladium(II) is bound to the terminal carbon of the C3H5 group. The reactivity of ligands 1 with Na2[PdCl4] is also reported and has allowed us to isolate the dinuclear compounds [Pd2Cl4(mu-1a)2] (6a) and [Pd2Cl4(mu-1b)2] (6b)] in which the thiazolidine behaves as a bridging (N,S) donor group.

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Synthesis of Methyl and Ethyl 3-Alkylthiazolidine-4(R)-carboxylates and Their Roots Inhibition of the Growth of Brassica campestris

Methyl and ethyl 3-alkylthiazolidine-4(R)-carboxylates (1-6 and 7-12), which were newly synthesized, inhibited growth of the roots of Brassica campestris L. subsp. rapa Hook fil. et Anders.Of the methyl esters, methyl 3-methylthiazolidine-4(R)-carboxylate (2) was the strongest inhibitor.Of the ethyl esters, ethyl 3-methylthiazolidine-4(R)-carboxylate (8) was the strongest inhibitor.The chlorophyll concentration in the cotyledons of plants treated with any of the compounds, except for 7, was decreased.

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Using human neural progenitor cell models to conduct large-scale drug screens for neurological and psychiatric diseases

High-throughput drug screen (HTS) has become a viable approach for new treatment discovery in human diseases. Advances in gene editing technology and human pluripotent stem cell differentiation techniques have expanded the capability of HTS to identify potential treatments for human diseases of the central nervous system. Here, we describe techniques to use a human patient-derived neural progenitor cell luciferase reporter line to screen a large small molecule library.

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A FACILE SYNTHESIS OF 2-OXO-THIAZOLIDINES OF BIOLOGICAL INTEREST.

A facile procedure for the preparation in good yield of L-2-oxothiazolidine-4-carboxylic acid and other 2-oxothiazolidines of biological interest is described, involving reaction of suitable aminothiols with 1,1′-carbonyldiimidazole in an organic solvent.

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PYRIDAZINONE COMPOUNDS

The invention is directed to pyridazinone compounds and pharmaceutical compositions containing such compounds that are useful in treating infections by hepatitis C virus

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