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There are disclosed compounds of the formula, STR1 where n is 0, 1 or 2; A is STR2 where X in each occurrence is independently hydrogen, halogen, loweralkyl, hydroxy, nitro, loweralkoxy, amino, cyano, trifluoromethyl or methylthio; Y in each occurrence is independently hydrogen, halogen, loweralkyl, hydroxy, nitro, loweralkoxy, amino, cyano, trifluoromethyl or methylthio; m is 1 or 2; k is 1 or 2; R1 and R2 are independently hydrogen, loweralkyl, STR3 or aryl except that when R1 is STR4 or aryl, R2 is hydrogen, or alternatively R1 +R2 taken together with the carbon atom to which they are attached form a cyclopentane, cyclohexane, cycloheptane, pyran, thiopyran, indan or piperidine ring; R3 and R4 are independently hydrogen or loweralkyl, or alternatively R3 +R4 taken together with the carbon atom to which they are attached form a cyclopentane, cyclohexane, cycloheptane, pyran, thiopyran, pyrrolidine or piperidine ring, the term aryl signifying an unsubstituted phenyl group or a phenyl group substituted with 1, 2 or 3 substituents each of which being independently loweralkyl, loweralkoxy, hydroxy, halogen, loweralkylthio, cyano, amino or trifluoromethyl, which are useful as antipsychotic, analgesic, anticonvulsant and anxiolytic agents.

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Objective: Conjugating quinolones with different bioactive pharmacophores to obtain potent anticancer active agents. Methods: Fused pyrazolopyrimidoquinolines 3a-d, Schiff bases 5, 6a-e, two hybridized systems: pyrazolochromenquinoline 7 and pyrazolothiazolidinquinoline 8, different substituted thiazoloquinolines 13-15 and thiazolo[3,2-a]pyridine derivatives 16a-c were synthesized. Their chemical structures were characterized through spectral and elemental analysis, cytotoxic activity on five cancer cell lines, caspase-3 activation, tubulin polymerization inhibition and cell cycle analysis were evaluated. Results: Four compounds 3b, 3d, 8 and 13 showed potent activity than doxorubicin on HCT116 and three compounds 3b, 3d and 8 on HEPG2. These promising derivatives showed increase in the level of caspase-3. The trifloromethylphenyl derivatives of pyrazolopyrimidoquinolines 3b and 3d showed considerable tubulin polymerization inhibitory activity. Both compounds arrested cell cycle at G2/M phase and induced apoptosis. Conclusion: Compounds 3b and 3d can be considered as promising anticancer active agents with 70% of colchicine activity on tubulin polymerization inhibition and represent hopeful leads that deserve further investigation and optimization.

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Chemistry involves the study of all things, chemical manipulation – in order to better understand the way in which materials are structured, how they change and how they react in certain situations. In a patent, 76186-04-4, name is (S)-4-Isopropylthiazolidine-2-thione, introducing its new discovery. Related Products of 76186-04-4

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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Herein are provided, inter alia, compounds capable of modulating the level of activity of low molecular weight protein tyrosine phosphatase (LMPTP) and methods of using the same. In embodiments, the compound has a structure according to Formula (I-A).

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Reflux of equimolecular amounts 2-aminobenzylamine and isatins in acetic acid produced indolo[3,2-c]quinolin-6-ones in good yields. A proposed mechanism involving initial formation of a spiro compound is given. This isolable intermediate subsequently rearranges via a sequential isocyanate ring opening and a cyclisation process to a urea derivative which finally cyclized to the indolo[3,2-c]quinolin-6-ones. The urea derivative could be prepared separately and cyclized selectively to indolo[3,2-c]quinolin-6-one. Reaction of N-acetylisatin with 2-aminobenzylamine at room temperature yielded the 1,4-benzodiazepinone 3-(2-acetamidophenyl)-1,5-dihydro-1,4-benzodiazepin-2-one whereas its isomer 2(2-acetamidophenyl)-4,5-dihydro-1,4-benzodiazepin-3-one was obtained from 2-(2-acetylaminophenyl)-N-(2-aminobenzyl)-2-oxoacetamide in acetic acid at room temperature. The previously unknown linear isomer of indolo[3,2-c]quinolin-6-one, i.e. indolo[2,3-b]quinolin-11-one, has been prepared by thermal (260C) cyclization of methyl 2-phenylamino indole-3-carboxylate, which in turn was prepared in two steps from methyl indole-3-carboxylate.

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As a society publisher, everything we do is to support the scientific community – so you can trust us to always act in your best interests, and get your work the international recognition that it deserves.An article , which mentions name: (R)-2-Oxothiazolidine-4-carboxylic acid, molecular formula is C4H5NO3S. The compound – (R)-2-Oxothiazolidine-4-carboxylic acid played an important role in people’s production and life., name: (R)-2-Oxothiazolidine-4-carboxylic acid

Inflammation is one of the main causes of preterm birth, frequently associated to intrauterine infection or chorioamnionitis. Oxidative stress is involved in preterm birth. On the one hand, reactive oxygen species are released by inflammatory cells against infection; on the other hand it is responsible of placental tissue damage after chorioamnionitis. Because of improvement in obstetric and perinatal care, survival rate in preterm births has increased, leading to changes in pathology of several processes, such as bronchopulmonary dysplasia. Bronchopulmonary dysplasia is a multifactorial entity which is consequence of multiple mechanisms, including perinatal inflammation and oxygen free radicals. Preterm newborn is very susceptible to chronic lung damage because of both, low antioxidant capacity, and exposure to high oxygen fractions during postnatal life. Modest lung oxidative stress damage after exposure to fetal endotoxin in premature newborns has been shown. Postnatal injury is needed to amplify the intrauterine inflammatory damage. Cell death induction by reactive oxygen species has been suggested as mechanism of lung damage. Several antioxidant therapies have been used in experimental studies in order to reduce or prevent bronchopulmonary dysplasia. So far, care is needed to standardize its use, because of its undesirable effects on inflammatory defense and development.

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Formylation of N-substituted phenyl succinimides was carried out by using Vilsmeier-Haack reagent which formed 2,5-dichloro-3,4-diformyl (N-substituted Phenyl) pyrroles (III) compounds. Compounds (III) was treated with ethylene glycol in presence of PTSA to get dioxolane derivatives (IV) which on further treatment with hydrazine hydrate formed compound (V) described in (Scheme-I). The synthesis of Schiffbases (VI) by treating 2 moles of substituted aromatic primary amines with 1 mole of compound (III). This compound (VI) on treatment with 2 moles of thioglycolic acid formed corresponding 4-thiazolidinone derivatives (VII) of 2,5-dichloro-3,4-diformyl (Nsubstituted phenyl) pyrroles. (Scheme-II).

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Leishmaniasis is a neglected tropical disease caused by around 20 species of obligate intramacrophage protozoa of the genus Leishmania. This disease is an important cause of morbidity and mortality that primarily impacts the poorest populations living in tropical and sub-tropical regions of the world, but has become of concern in some developed countries. The resistance of leishmanial parasites to the drugs available and their undesirable side effects have prompted the discovery of new synthetic compounds with potent antileishmanial activity and fewer side effects that can serve as new therapeutic agents. In this article, we make a comprehensive review of the most recent advances of synthetic compounds with antileishmanial activity (from 2015 to the early 2017). Furthermore, we covered the structure- activity relationship studies that allow for optimization and selection of the most promising drugs, and the biochemical mechanisms that explain the antileishmanial activities observed.

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Following the first report on the nucleoside phosphoramidate (ProTide) prodrug approach in 1990 by Chris McGuigan, the extensive investigation of ProTide technology has begun in many laboratories. Designed with aim to overcome limitations and the key resistance mechanisms associated with nucleoside analogues used in the clinic (poor cellular uptake, poor conversion to the 5?-monophosphate form), the ProTide approach has been successfully applied to a vast number of nucleoside analogues with antiviral and anticancer activity. ProTides consist of a 5?-nucleoside monophosphate in which the two hydroxyl groups are masked with an amino acid ester and an aryloxy component which once in the cell is enzymatically metabolized to deliver free 5?-monophosphate, which is further transformed to the active 5?-triphosphate form of the nucleoside analogue. In this review, the seminal contribution of Chris McGuigan?s research to this field is presented. His technology proved to be extremely successful in drug discovery and has led to two Food and Drug Administration-approved antiviral agents.

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Background: A series of 2-(1H-benzo[d]imidazol-2-ylthio)-N-(substituted 4-oxothiazolidin-3-yl) acetamides was synthesized and characterized by physicochemical and spectral means. The synthesized compounds were evaluated for their in vitro antimicrobial activity against Staphylococcus aureus, Bacillus subtilis, Escherichia coli, Candida albicans and Aspergillus niger by tube dilution method. The in vitro cytotoxicity study of the compounds was carried out against human colorectal (HCT116) cell line. The most promising anticancer derivatives (5l, 5k, 5i and 5p) were further docked to study their binding efficacy to the active site of the cyclin-dependent kinase-8. Results: All the compounds possessed significant antimicrobial activity with MIC in the range of 0.007 and 0.061 muM/ml. The cytotoxicity study revealed that almost all the derivatives were potent in inhibiting the growth of HCT116 cell line in comparison to the standard drug 5-fluorouracil. Compounds 5l and 5k (IC50 = 0.00005 and 0.00012 muM/ml, respectively) were highly cytotoxic towards HCT116 cell line in comparison to 5-fluorouracil (IC50 = 0.00615 muM/ml) taken as standard drug. Conclusion: The molecular docking studies of potent anticancer compounds 5l, 5k, 5i and 5p showed their putative binding mode and significant interactions with cyclin-dependent kinase-8 as prospective agents for treating colon cancer.

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