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Heterocyclic compounds containing nitrogen and sulfur, processes for their preparation and pharmaceutical compositions thereof

The invention relates to nitrogen- and sulfur–containing heterocyclic compounds of the formula (I), wherein, Ar represents an optionally mono- or polysubstituted aryl or heteroaryl group;, R1 represents a carbonyl or (C2 6alkenyl)–carbonyl group;, R2 represents a hydrogen atom, or a C1 6alkyl, phenyl or phenyl(C1 4alkyl) group;, R3 represents a hydrogen atom or a (C1 6 alkoxy)carbonyl group;, R4 and R5, which may be the same or different, represent a hydrogen atom or a C1 6alkyl group;, R6 represents a hydrogen atom or a C1 6alkyl group or halophenyl group;, m is 0 or 1; and, n is 1 or 2,with the proviso that R2 is a hydrogen atom when m is 0, and acid addition salts of the compounds of formula (I) and pharmaceutical compositions thereof. The invention also relates to processes for the preparation of these compounds. The compounds of formula (I) show a significant cerebral antihypoxic activity.

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Awesome and Easy Science Experiments about (R)-2-Oxothiazolidine-4-carboxylic acid

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Electric Literature of 19771-63-2, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.19771-63-2, Name is (R)-2-Oxothiazolidine-4-carboxylic acid, molecular formula is C4H5NO3S. In a Article£¬once mentioned of 19771-63-2

A practical synthesis of (+)-biotin from L-cysteine

alpha-Amino aldehyde 4, which is readily derived from L-cysteine through cyclization and elaboration of the carboxy group, was subjected to the Strecker reaction, which, via sodium bisulfite adduct 16, afforded alpha-amino nitrile 5 with high diastereose-lectivity (syn/anti = 11:1) and in high yield. Amide 6, derived from 5, was converted to thiolactone 8, a key intermediate in the synthesis of (+)-biotin (1), by a novel S,N-carbonyl migration and cyclization reaction. The Fukuyama coupling reaction of 8 with the zinc reagent 21, which has an ester group, in the presence of a heterogeneous Pd/ C catalyst allowed the efficient installation of the 4-carboxybutyl chain to provide 9. Compound 9 was hydrogenated and the protecting groups removed to furnish 1 in 10 steps and in 34 % overall yield from L-cysteine.

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New dimensions in the field of antimalarial research against malaria resurgence

Malaria is a life threatening disease caused by microscopic parasites called Plasmodium that are transmitted to human beings by mosquitoes. Single celled Eukaryotic plasmodium parasite is responsible to cause malaria in human beings and is transmitted by bite of Anopheles species mosquitoes. Resurgence of malaria towards the end of 20th Century is due to failure of its eradication completely. Parasite recurrence occurs due to high densities of parasite, low immunity and non opimized drug concentration. The ineffective eradications strategies were due to indefinable complex life cycle of Plasmodium and emergence of drugs resistant strains of Plasmodium falciparum (Pf) including Artemisinin and Artemisinin based combination therapy (ACT). The vector of the disease i.e. mosquitoes became resistive towards Pyrethroids, which are only class of insecticides recommended for vector control. Artemisinin based combination therapy gained acceptance as an effective approach to counter the spread of disease resistance to chloroquine, sulfadoxine, pyrimethamine and other anti malarial drugs. Understanding the underlying molecular basis of the pathogenesis led to the development of some new diagnostic, drugs and insecticides. Reports on the use of new combination therapies reduced the burden of disease worldwide. Some of the new combination therapies are in clinical stage of development that have efficacy against drug resistant parasites and the potential to use in single dose regimens to improve compliance. The current review represents the recent anti-malarial research carried out globally especially in the class of synthesis of small molecule and natural product derivatives as potent anti-malarial drugs. The review also covers the advancement in the anti-malarial vaccine development although goal for vaccine development still remains elusive.

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Synthesis, characterization, antibacterial and antiepileptic studies of some novel thiazolidinone derivatives

In the quest of finding new drug leads with potential antibacterial and antiepileptic activities, synthesis of thiazolidinone derivatives 6(a?c) is reported which are obtained from 5-(4-chlorobenzylidine)-3-[4-(7-chloroquinoline-4-ylamino]propyl)-2-imino-thiazolidin-4-one derivatives by applying appropriate synthetic route. These compounds 6(a?c) were evaluated for antibacterial and antiepileptic activities. Compound 6a having good lipophilicity is found to be most active.

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Anti-diabetic and anti-hyperlipidemic effects of 2-[(Trimethylsilyl)-oxy]-, trimethylsilyl ester isolated from Pericampylus glaucus in diabetic rats

The purpose of the present study was to isolate and identify 2-[(trimethylsilyl)-oxy]-, trimethylsilyl ester compound from Pericampylus glaucus and to evaluate their effects on blood glucose and lipid profiles in diabetic rats. The isolation and identification of compound 2-[(trimethylsilyl)-oxy]-, trimethylsilyl ester was undertaken through column chromatography followed by GCMS and1HNMR. The anti-hyperglycemic effect of isolated compound was carried out against STZ-induced diabetic rats. GC followed by MS and1HNMR indicate the presence of compound 2-[(trimethylsilyl)-oxy]-, trimethylsilyl ester in sample. The weight was 234, retention time 2.99, and total area was 1015482. The compound significantly (P < 0.01) reduced blood glucose level in hyperglycemic rats as matched to control. The attenuation on blood glucose level with 2-[(trimethylsilyl)-oxy]-, trimethylsilyl ester were non-significant (P > 0.05) up to 4 h that became significant (P < 0.01) at 24 h as matched to diabetic group. A significant (P < 0.001) attenuation in levels of cholesterol, triglycerides, LDL and significant (P < 0.01) increased in HDL was noted in 2-[(trimethylsilyl)-oxy]-, trimethylsilyl ester treated group. The findings of this study indicate that isolated compound Pericampylus glaucus compound 2-[(trimethylsilyl)-oxy]-, trimethylsilyl ester has significant attenuation effect on blood glucose and lipid profiles. I hope this article can help some friends in scientific research. I am very proud of our efforts over the past few months and hope to 2682-49-7, help many people in the next few years.Formula: C3H5NOS

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The important role of 76186-04-4

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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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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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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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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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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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