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Oxadiazole derivative containing heterocyclic side chain, synthesis method and application thereof (by machine translation)

The invention discloses an oxadiazole derivative containing a heterocyclic side chain, a synthesis method and application, wherein the structure of the oxadiazole derivative is as shown in the formula I, wherein each substituent is defined in the specification and claims. The compound, provided by the invention, has strong IDO inhibiting activity, has good drug absorption potentiality, and has a good development prospect. (by machine translation)

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Synthesis and pharmacological evaluation of some 2-(4-isobutylphenyl)-N-(4-oxo-2-arylthiazolidin-3-yl) propanamides

Some derivatives of ibuprofen bearing 4H-thiazolidin-4-one moiety were synthesized from ibuprofen and studied for their pharmacological activities. Methyl ester of ibuprofen I was synthesized from ibuprofen and then converted to hydrazide II with the reaction of hydrazine hydrate. Hydrazide of ibuprofen then reacted with aromatic aldehydes in the presence of glacial acetic acid to yield the hydrazones III which on reaction with thioglycolic acid and dimethyl formamide in presence of catalytic amount of anhydrous zinc chloride furnished the title compounds IV. The structures of synthesized compounds were elucidated mainly by spectral evidence. All the synthesized title compounds were screened for their anti-inflammatory activity. Title compounds were also studied for their ulcerogenic potential. The compounds exhibited moderate to significant activities.

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2, 3-benzodiazepins (by machine translation)

What is described are BET protein-inhibitory, in particular BRD4-inhibitory 2,3-benzodiazepines of the general formula (I) in which R1a, R1b, R1c, R2, R3, R4, R5, A and X have the meanings given in the description, intermediates for preparing the compounds according to the invention, pharmaceutical compositions comprising the compounds according to the invention and their prophylactic and therapeutic use for hyperproliferative disorders, in particular for tumour disorders. Also described is the use of BET protein inhibitors for benign hyperplasias, atherosclerotic disorders, sepsis, autoimmune disorders, vascular disorders, viral infections, for neurodegenerative disorders, for inflammatory disorders, for atherosclerotic disorders and for the control of male fertility.

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Synthesis and aldose reductase inhibitory effect of some new hydrazinecarbothioamides and 4-thiazolidinones bearing an imidazo[2,1-b] thiazole moiety

Objectives: To synthesize and characterize 2-[[6-(4-bromophenyl)imidazo[2,1-b]thiazol-3-yl]acetyl]-N-alkyl/arylhydrazinecarbothioamide and 3-alkyl/aryl-2-[((6-(4-bromophenyl)imidazo[2,1-b]thiazol-3-yl)acetyl)hydrazono]-5-nonsubstituted/methyl-4-thiazolidinone derivatives and evaluate them for their aldose reductase (AR) inhibitory effect. Materials and Methods: 2-[[6-(4-bromophenyl)imidazo[2,1-b]thiazol-3-yl]acetyl]-N-alkyl/arylhydrazinecarbothioamides (3a-f) and 3-alkyl/aryl-2-[((6-(4-bromophenyl)imidazo[2,1-b]thiazol-3-yl)acetyl)hydrazono]-5-nonsubstituted/methyl-4-thiazolidinones (4a-j) were synthesized from 2-[6-(4-bromophenyl)imidazo[2,1-b]thiazole-3-yl]acetohydrazide (2). Their structures were elucidated by elemental analyses and spectroscopic data. The synthesized compounds were tested for their ability to inhibit rat kidney AR. Results: Among the synthesized compounds, 2-[[6-(4-bromophenyl)imidazo[2,1-b]thiazol-3-yl]acetyl]-N-benzoylhydrazinecarbothioamide (3d) showed the best AR inhibitory activity. Conclusion: The findings of this study indicate that the different derivatives of the compounds in this study may be considered interesting candidates for future research.

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Extracurricular laboratory:new discovery of 2-Cyanoimino-1,3-thiazolidine

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3-Cyano-2-(N-cyanoimino)thiazolidine (3-cyano-NCT): An efficient electrophilic cyanating agent for activated methylene compounds

We found that 3-cyano-2-(N-cyanoimino)thiazolidine (3-cyano-NCT) is a novel electrophilic cyanating agent. Various activated methylene compounds were cyanated in moderate to good yields.

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3-Phosphono-2-(N-cyanoimino)thiazolidine derivatives, new phosphorylating agents for alcohols

We have developed new phosphorylating agents, 3-phosphono-2-(N-cyanoimino)-thiazolidine derivatives (3-phosphono-NCTs), which were readily synthesized by phosphorylation of NCT, and transformed primary and secondary alcohols into phosphates in good yield. The transfer of three kinds of dialkylphosphono groups [(PhO)2P(O)-, (EtO)2P(O)-, (Cl3CCH2O)2P(O)-] proceeded in excellent yields. Selective phosphorylation of various alcohols was also accomplished.

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Amines having secondary aliphatic amino groups

The present invention relates to novel amides having secondary amino groups, a process for preparing them, adducts of these amines and their uses. The amides can be prepared in a simple way from readily available starting materials. They and their adducts have, in particular, a low viscosity and are suitable as constituent of polyurethane and polyurea compositions having excellent processability and high flexibility, and also as constituent of epoxy resin compositions, in particular coatings.

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Discover the magic of the 1,1-Dioxo-isothiazolidine

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Design of a series of bicyclic HIV-1 integrase inhibitors. Part 1: Selection of the scaffold

HIV integrase inhibitors based on a novel bicyclic pyrimidinone core is presented. Nine variations of the core scaffold are evaluated leading to optimization of the 6:6 core giving compound 48 with an EC50 of 3 nM against wild type HIV infected T-cells.

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PROCESS FOR PREPARING CYANIMINO-1,3-THIAZOLIDINES

The present invention relates to a process for preparing cyanimino-1,3-thiazolidines, which are important building blocks for the preparation of crop protection active ingredients and pharmaceuticals, by the following scheme: where A is an alkali metal and X represents an acid radical.

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Mesoionic sydnone: A review in their chemical and biological properties

Various literature sources have documented sydnones as important molecules with exclusive chemical properties and a wide spectrum of bioactivities. Sydnone can be defined as a five-membered pseudo-aromatic heterocyclic molecule. Classically, 1,2,3-oxadiazole forms the main skeleton of sydnone. The molecule has delocalized balanced positive and negative charges. The five annular atoms share the positive charge and the enolate-like exocyclic oxygen atom bears the negative charge. The hydrogen atom at the position C4 was proved to have acidic and nucleophilic functionalities making the sydnone ring reactive towards electrophilic reagents. These unique chemical features enable sydnones to interact with biomolecules resulting in important therapeutic effects like anticancer, antidiabetic, antimicrobial, antioxidant and anti-inflammatory. Consequently, we aim from the current article to review the available chemical and pharmacological information on sydnone and its derivatives.

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