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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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Among all heterocycles, the triazine scaffold occupies a prominent position, possessing a broad range of biological activities. Triazine is found in many potent biologically active molecules with promising biological potential like anti-inflammatory, anti-mycobacterial, anti-viral, anti-cancer etc. which makes it an attractive scaffold for the design and development of new drugs. The wide spectrum of biological activity of this moiety has attracted attention in the field of medicinal chemistry. Due to these biological activities, their structure-activity relationship has generated interest among medicinal chemists and this has culminated in the discovery of several lead molecules. The outstanding development of triazine derivatives in diverse diseases within very short span of time proves its magnitude for medicinal chemistry research. Therefore, these compounds have been synthesized as target structure by many researchers, and were further evaluated for their biological activities. In this review, we have compiled and discussed the biological potential of s-triazine derivatives, which could provide a low-height flying bird’s eye view of the triazine derived compounds to a medicinal chemist, for a comprehensive and target oriented information for the development of clinically viable drugs.

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The present invention relates to novel 2-thiazolidinone derivatives of the general formula (I), STR1 wherein A stands for hydrogen, halogen or a C1-4 alkyl, C1-4 alkoxy or nitro group; and n is 0 or 1. The compounds according to the invention show a cytoprotective and gastric acid secretion-inhibiting effect and thus, may be used in the therapy of gastric and duodenal ulcers.

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The synthesis and evaluation of the anticancer activity of new acylated oximes derivatives of oleanolic acid with 4-thiazolidinone-3(5)-carboxylic acid moieties were described. Newly synthesized compounds were elucidated on the basis of elemental analyses and spectral data (IR, 1H, and 13C NMR). Anticancer activity of the tested compounds has been evaluated in vitro at National Cancer Institute (NCI) in which some structure activity relationships (SARs) were discussed. Among the tested compounds, 3-[(2,4-thiazolidinedione-5-ylidene)-carboxyimino] olean-12-en-28-oic acid methyl ester (IVm) was superior to other related compounds with mean values of pGI50 = 5.51/5.57, pTGI = 5.09/5.13, and pLC50 = 4.62/4.64, low toxicity and moderate activity level in vivo hollow fiber assay. Springer Science+Business Media, LLC 2011.

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We have developed a new class of pyridine catalyst for asymmetric acylation of sec-alcohols having a conformation switch system in which interconversion between self-complexation and uncomplexation is induced by acylation and deacylation steps, respectively. Kinetic resolution of various sec-alcohols is performed by the asymmetric acylation with isobutyric anhydride using 0.05 to 0.5 mol % catalyst 1a with s values of up to 30. In addition, dl-diols are also resolved in a similar manner in good selectivity. Moreover, asymmetric desymmetrization of meso-1,X-diols (X = 2-6) are achieved in the presence of 0.5-5 mol % catalyst 1a. A working model for the reaction mechanism is proposed on the basis of the 1H NMR measurements, X-ray structural analyses, and AM1 and DFT calculations, where the conformation switch system governed by an intramolecular cation-pi interaction between a pyridinium ring and a thiocarbonyl group would play a key role to attain both good selectivity and high catalytic activity.

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COA of Formula: C6H11NS2, Chemistry is a science major with cience and engineering. The main research directions are chemical synthesis,preparation and modification of special coatings. In some cases, the catalyzed mechanism may include additional steps.In a article, 76186-04-4, molcular formula is C6H11NS2, introducing its new discovery.

The first diastereoselective synthesis of aryloxyphosphoramidate prodrugs of 3?-deoxy-2?,3?-didehydrothymidinemonophosphate (d4TMP) was recently reported. The synthetic approach utilized the chiral auxiliary (S)-4-isopropylthiazolidine-2-thione (2). For this strategy, a stereochemically pure phosphorodiamidate intermediate was needed. The diastereoselective formation of this key compound was investigated by using different phenols and L-alanine methyl or benzyl ester. Generally, the reaction with 3- or 4-substituted phenols led to significantly better diastereoselectivities compared to their 2-substituted counterparts. Moreover, variation of the ester group in the amino acid residue resulted in no significant differences with regard to the obtained diastereoselectivity. From the reported results, a model for the transition state was elaborated. Finally, eight new (S P)-arylphosphoramidates were synthesized with very high diastereoselectivities (up to ? 95 % de) and tested for their anti-HIV potency, showing a tendency for higher antiviral activity from the (S P) diastereomers.

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