Brief introduction of 1,1-Dioxo-isothiazolidine

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Practical Synthesis of Sultams via Sulfonamide Dianion Alkylation: Application to the Synthesis of Chiral Sultams

(Equation presented) A practical synthesis of sultams was developed via intramolecular sulfonamide dianion alkylation. This method has been applied toward the synthesis of chiral sultams, which are synthetically valuable as chiral auxiliaries.

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Total synthesis of the polyene macrolide dermostatin A

Herein we provide full details of studies which culminated in the first total synthesis of the polyene macrolide dermostatin A, confirming our earlier stereochemical assignment. A highly convergent synthesis was developed, featuring the cyanohydrin acetonide method for polyol construction and a Stille approach to polyene introduction. The strategies and tactics developed en route should be of value for the preparation of other members of the polyene macrolide class, as well as analogs of the dermostatins.

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Past, present, and future of antifungal drug development

Fungi are eukaryotic, single cell or multicellular organisms which cause a wide range of human diseases ranging from superficial skin to invasive life-threatening infections. Over the last couple of decades the incidence of life-threatening fungal infections has increased seriously as the patients of AIDS, cancer, organ transplant and immune-compromised population have increased. Though a significant progress has been made in the discovery of antifungal agents in the form of polyenes, azoles and allylamines yet the antifungal therapy poses severe challenge because of the side effects, narrow spectrum of activity and recently development resistance among patients against the present antifungals. This chapter deals with the current antifungal agents, their spectrum of activity, mode of action, limitations, current challenges in antifungal therapy, and new avenues for future developments.

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Chemical modification of PVA with four, five and seven heterocyclic compounds and study anticancer activity

Schiff bases [1]a,b were prepared from the reaction of 2-amino-5-mercapto-1,3,4-thiadiazole with aromatic aldehydes. In the present study a series of some four, five-and seven-membered heterocyclic compounds have been synthesized by the reaction of schiff bases [1]a,b with thioglycolic acid, chloroacetyl chloride, sodium azide or various anhydrides to give thiazolidinone [2]a, azetidinone [6]b, tetrazole [7]b and 1,3-oxazepine derivatives [14-16]b respectively, then compounds[2]a, [6,7]b and[14-16]b were reacted with Na2CO3 of distilled water as a solvent, then of ClCH2COOH was added to produce [3]a, [8,9]band[17-19]b. The compounds [3]a, [8,9]b and [17-19]b reacted with SOCl2 in the presence of Benzene to producing the compounds [4]a, [10,11]b and [20-22]b. Chemical modification of Poly(vinyl alcohol) were obtained by reaction of PVA with compounds [4]a, [10,11]b and [20-22]b using the Dimethyl formamide to produce compounds [5]a,[12,13]b and [23-25]b. The structure of the synthesized compounds were set by their analytical and spectral data such as, FTIR spectra,1H-NMR., UV-Vis Spectroscopy and Elemental analysis (CHNS). Finally study antibacterial activity screened via two types of bacteria. Anticancer activity also examined for all modifier polyvinyl alcohol.

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Diastereoselective additions of titanium enolates from N-glycolyl thiazolidinethiones to acetals

The stereochemical outcome of the Lewis acid-mediated glycolate addition of the titanium enolates from protected N-hydroxyacetyl-4-isopropyl-1,3- thiazolidine-2-thiones to dimethyl and dibenzyl acetals depends on the hydroxyl protecting group. Particularly, the pivaloyl protected glycolate derivative provides the reluctant anti adducts in high yields and diastereomeric ratios, which can be isolated and further converted in enantiomerically pure form to beta-methoxy or beta-benzyloxy alpha-pivaloyloxy carbonyl fragments in a straightforward manner.

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Extended knowledge of 4-(4-((2,4-Dioxothiazolidin-5-ylidene)methyl)-2-methoxyphenoxy)-3-(trifluoromethyl)benzonitrile

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Synthetic Route of 1055361-35-7, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.1055361-35-7, Name is 4-(4-((2,4-Dioxothiazolidin-5-ylidene)methyl)-2-methoxyphenoxy)-3-(trifluoromethyl)benzonitrile, molecular formula is C19H11F3N2O4S. In a Article£¬once mentioned of 1055361-35-7

Synthetic Approaches to 5,7- and 5,8-Dimethoxyquinoline. Sonochemical Dehalogenation of Substituted 2,4-Dichloroquinolines. Use of the 2D COLOC Spectrum for the NMR Assignment of 5,8-Dimethoxyquinoline

Sonochemical dehalogenation of 2,4-dichloroquinoline is very facile.However, with 5,7-dimethoxy-2,4-dichloroquinoline the reaction proceeds stepwise to provide the title dimethoxyquinolines which cannot be prepared via the Skraup reaction.The 13C NMR chemical shift assignments for 5,8-dimethoxyquinoline are presented.These were made by utilising the coupling connectivities from the bridgehead carbons in the 2D COLOC spectrum. – Keywords.Sonochemistry; Quinolines; 13C NMR Spectroscopy; 2D COLOC spectrum.

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Molecular docking, molecular dynamics, and in silico prediction of the toxic potential of primaquine thiazolidinone derivatives

Primaquine thiazolidinone derivatives are proposed as promising antimalarial candidates to be tested as primaquine substitutes. Molecular docking and dynamics simulations were applied in the analogues-NQO2 complexes to understand their interactions, and also studied the toxic potential of these derivatives in a set of 16 target proteins. The results of our study suggest that the interactions of five thiazolidinone primaquine derivatives with NQO2 are stronger than the interaction of primaquine and NQO2. The analogue 5n-protein complex seems to be the most stable compared with the primaquine-protein complex. The analogues 5n and 5o are predicted to be in the same class of toxic potential as primaquine. Their interactions with the cytochrome P450 enzymes are also predicted to be weaker, indicating that a better activity/toxicity balance compared with primaquine may be reached.

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Synthesis of some new 1,3,4-oxadiazole derivatives and evaluation of their antibacterial effects

In the present study, some oxadiazole derivatives have been synthesized by incorporating azetidinyl and thiazolidinyl moieties at its 2-position such as 5-(p-methoxyphenyl)-[2-substitutedbenzylidenylimino]1,3,4- oxadiazole 2-6, 5-(p-methoxyphenyl)-[2-(3¡ä-chloro-2¡ä-oxo-4¡ä-substitutedaryl-1-azetidinyl)1,3,4-oxadiazole 7-11 and 5-(p-methoxyphenyl)-[2-(2¡ä-substitutedaryl-4¡ä-oxo-1¡ä,3¡ä-thiazolidin-3¡ä-yl)1,3,4-oxadiazole 12-16. The structure of these compounds have been elucidated by elemental analysis (C, H, N) and IR, 1H-NMR, Mass spectroscopic techniques. Further, these compounds were subjected to screening for antibacterial activities against different bacterial strains.

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Brief introduction of (S)-4-Isopropylthiazolidine-2-thione

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A versatile synthesis of various substituted taurines from vicinal amino alcohols and aziridines

Taurine and structurally diverse substituted taurines have been synthesized by peroxyformic acid, oxidation of the thiazolidine-2-thione intermediates generated from, vicinal amino alcohols or aziridines and carbon disulfide. The stereochemistry and mechanisms of the reactions are disscussed. The method is a salt-free and versatile route, convenient in terms of purification, and can be used to synthesize optically active substituted taurines.

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Synthesis and pharmacological studies of 1-(2-amino-1-(4-methoxyphenyl) ethyl) cyclohexanol analogs as potential microbial agents

A novel series of Schiff bases 4a?n was prepared from 2-hydrazinyl-N-(2-(1-hydroxycyclohexyl)-2-(4-methoxyphenyl) ethyl)acetamide. Thiazolidinone 5a?n derivatives were prepared from the reaction of Schiff base and thioglycolic acid. The structures of the synthesized compounds were assigned on the basis of elemental analysis, IR, 1H NMR, 13C NMR and Mass spectral data. All the compounds were screened against different strains of bacteria and fungi. These active compounds impelled us to study their antitubercular activity. Compounds 4b, 5a, 5b, 5d, 5e, 5f, 5k, 5l and 5n emerged as promising antimicrobials. It was also observed that the promising antimicrobials have proved to be better antituberculars. Compound 5k showed better antitubercular activity compared to Rifampicin.

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