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Disclosed are prodrugs as follows:(I) a prodrug of the formula where A is a sulfur or a selenium, and R is a mono- di- or oligo-saccharide;(II) a prodrug of the formula where A is sulfur or selenium, R? is a sugar, or =O, and the R? groups are hydrogen, alkyl, alkoxy, carboxy;(III) a conjugate of an antioxidant vitamin and a thiolamine or selenolamine;(IV) a prodrug of the formula where A is sulfur or selenium, and R? is a sugar, or an alkyl or aryl group, or =O, and R? is an alkoxy, or an amine group;(V) a prodrug of the formula R is COOH or H, and R? is a sugar or =O.

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A self-immolative gamma-aminopropylsulfonate linker was investigated for use in the development of prodrugs that are reactive to various chemical or biological stimuli. To demonstrate their utility, a leucine-conjugated prodrug of 5-chloroquinolin-8-ol (5-Cl-8-HQ), which is a potent inhibitor against aminopeptidase from Aeromonas proteolytica (AAP), was synthesized. The sulfonate prodrug was considerably stable under physiological conditions, with only enzyme-mediated hydrolysis of leucine triggering the subsequent intramolecular cyclization to simultaneously release 5-Cl-8-HQ and form gamma-sultam. It was also confirmed that this gamma-aminopropylsulfonate linker was applicable for prodrugs of not only 8-HQ derivatives but also other drugs bearing a phenolic hydroxy group.

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Cancer is the second leading cause of death worldwide. There is always a huge demand for novel anticancer drugs and diverse new natural or synthetic compounds are developed continuously by scientists. Presently, a large number of drugs in clinical practice have showed pervasive side effect and multidrug resistance. Sulfonyl or sulfonamide hybrids became one of the most attractive subjects due to their broad spectrum of pharmacological activities. Sulfonyl hybrids were broadly explored for their anticancer activities and it was found that they possess minimum side effect along with multi-drug resistance activity. This review describes the most recent applications of sulfonyl hybrid analogues in anticancer drug discovery and further discusses the mechanistic insights, structure-activity relationships and molecular docking studies for the potent derivatives.

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The invention provides an inner sulfonamide compounds and their preparation method. The invention of the specific method is catalyst C, sulfonamide B, oxidizing agent D reaction in an organic solvent is added, after the separation and purification, to obtain an internal sulfonamide compound E, […] detection after the reaction is finished, then adding the oxidizing agent after the reaction F, inlet separation and purification, to obtain in the sulfonyl imide compound G. The method the catalyst needed is cheap and easy to obtain, low toxicity of the iron complex. When using the sulfonamide H when, through according to the above method after the reaction, and then adding the other additional oxidizing agent F under the condition of, one-pot synthesis in the realization of the sulfonyl imide compound. In the preparation of the sulfonamide and in the sulfonyl imide compound widely used in pharmaceutical chemistry, materials chemistry and the field of organic synthesis. (by machine translation)

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In the modern scenario, the quinolone scaffold has emerged as a very potent motif considering its clinical significance. Quinolones possess wide range of pharmacological activities such as anticancer, antibacterial, antifungal, antiprotozoal, antiviral, anti-inflammatory, carbonic anhydrase inhibitory and diuretic activity etc. The versatile synthetic approaches have been successfully applied and several of the resulted synthesized compounds exhibit fascinating biological activities in numerous fields. This has prompted to discover quinolone-based analogues among the researchers due to its great diversity in biological activities. In the past few years, various new, efficient and convenient synthetic approaches (including green chemistry and microwave-assisted synthesis) have been designed and developed to synthesize diverse quinolone-based scaffolds which represent a growing area of interest in academic and industry as well as to explore their biological activities. In this review, an attempt has been made by the authors to summarize (1) One of the most comprehensive listings of quinolone-based drugs or agents in the market or under various stages of clinical development; (2) Recent advances in the synthetic strategies for quinolone derivatives as well as their biological implications including insight of mechanistic studies. (3) Further, the biological data is correlated with structure-activity relationship studies to provide an insight into the rational design of more active agents.

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Infectious tropical diseases such as malaria, tuberculosis, and the so-called neglected tropical diseases are causing tremendous suffering to millions of people and huge impact on national economies, seriously worsening life conditions in the poorest parts of the world, where these diseases are endemic. Despite the existence of drugs for most of these diseases, they are far from adequate. Lack of efficacy, toxicity, and emergence of pathogen resistance are among the most important flaws of currently available drugs. Thus, apart from improving prevention and vector control measures, there is an urgent need for developing new efficacious, safe, and inexpensive drugs that desirably feature novel chemotypes. Multicomponent reactions (MCRs), where three or more reactants are combined in a one-pot reaction, constitute a very powerful tool for such endeavors, inasmuch as they enable a very rapid access to structurally diverse, usually complex scaffolds, shortening the synthesis of the novel drugs and, hence, lowering production costs, and affording original chemotypes. In this chapter, we provide an overview of the application of different types of MCRs to drug discovery against infectious tropical diseases, with particular emphasis on how structural complexity and molecular diversity can be readily introduced through their use.

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This application relates to compounds of Formula (I) or pharmaceutically acceptable salts or stereoisomers thereof, which modulate the activity of adenosine receptors, such as subtypes A2A and A2B receptors, and are useful in the treatment of diseases related to the activity of adenosine receptors including, for example, cancer, inflammatory diseases, cardiovascular diseases, and neurodegenerative diseases.

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Various substituted thiazolidin-2-ones were synthesized from the corresponding thiazolidine-2-thiones with bromoethanol in ethanol with sodium ethoxide as a base. The optimal reaction conditions and mechanism were reinvestigated in detail. The bioassay indicated that (S)-4-isobutyl and (S)-4-benzylthiazolidin-2-ones show certain inhibitive activities against Candida albicans and Escherichia coli. Supplemental materials are available for this article. Go to the publisher’s online edition of Phosphorus, Sulfur, and Silicon and the Related Elements to view the free supplemental file.

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A ketonic heterocyclic compound having at least two heteroatoms in the ring is prepared by reacting a difunctional compound having the general formula STR1 in which R1, R2, R3 and R4 are members of the group consisting of aliphatic, aromatic, cycloaliphatic and heterocyclic hydrocarbons which may contain functional groups selected from –OH, –OR5, –COOH, –COOR5, –CN, –Cl, –Br, –I, –F, and –CO–R5, wherein R5 is an aliphatic, aromatic, cycloaliphatic or heterocyclic hydrocarbon; X is oxygen or sulphur; Y is sulphur or nitrogen; n is an integer ranging from 1 to 3, or zero; R6 is a hydrogen or a hydrocarbon radical included in the above definition of R1 R2 R3 and R4 ; and m is the valence of Y, with carbon monoxide and oxygen in the presence of a catalyst selected from selenium, selenium compounds and complexes of copper, in the temperature range of from room temperature to 80 C and in the pressure range of from 1 to 10 atmospheres.

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New Advances in Chemical Research, May 2021. SDS of cas: 5908-62-3, Having gained chemical understanding at molecular level, chemistry graduates may choose to apply this knowledge in almost unlimited ways, as it can be used to analyze all matter and therefore our entire environment. 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 novel compounds having general formula (I), wherein R1 to R4, A, W, Q and Y are as described herein, compositions including the compounds and methods of using the compounds.

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