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Recent Advances in the Synthesis of Hydantoins: The State of the Art of a Valuable Scaffold

The review highlights the hydantoin syntheses presented from the point of view of the preparation methods. Novel synthetic routes to various hydantoin structures, the advances brought to the classical methods in the aim of producing more sustainable and environmentally friendly procedures for the preparation of these biomolecules, and a critical comparison of the different synthetic approaches developed in the last twelve years are also described. The review is composed of 95 schemes, 8 figures and 528 references for the last 12 years and includes the description of the hydantoin-based marketed drugs and clinical candidates.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H347N | ChemSpider

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Chromans and chromenes, compositions and hypertensive method

Compounds of formula (I): STR1 a pharmaceutically acceptable salt or solvate thereof having anti-hypertensive activity, a process for their preparation and their use as pharmaceuticals.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H181N | ChemSpider

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Quinine conjugates and quinine analogues as potential antimalarial agents

Malaria is a tropical disease, prevalent in Southeast Asia and Africa, resulting in over half a million deaths annually; efforts to develop new antimalarial agents are therefore particularly important. Quinine continues to play a role in the fight against malaria, but quinoline derivatives are more widely used. Drugs based on the quinoline scaffold include chloroquine and primaquine, which are able to act against the blood and liver stages of the parasite’s life cycle. The purpose of this review is to discuss reported biologically active compounds based on either the quinine or quinoline scaffold that may have enhanced antimalarial activity. The review emphasises hybrid molecules, and covers advances made in the last five years. The review is divided into three sections: modifications to the quinine scaffold, modifications to aminoquinolines and finally metal-containing antimalarial compounds.

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Quinuclidine | C7H329N | ChemSpider

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Acid-Catalyzed Synthesis of Thiazolidin-4-ones

A two-steps synthesis of thiazolidin-4-ones, from alpha-tetralone 6 or thiochroman-4-one 7, catalyzed by acids is described. The reactions of alpha-tetralone 6 or thiochroman-4-one 7, with substituted thiosemicarbazides, under AcOH or heteropolyacid (HPAs) catalysis afford thiosemicarbazones 8 and 9 in excellent yields. Condensations of the previous compounds 8 and 9 with alpha-bromoester, under sulfuric acid or heteropolyacid catalysis, yield the corresponding thiazolidin-4-ones 10 and 11.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H433N | ChemSpider

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Synthesis and Biological Evaluation of Novel 5-Oxo-1-Phenylpyrrolidine-3-Carboxylic Acid Analogs

A number of 5-oxo-1-phenyl-4-(substituted methyl) pyrrolidine-3-carboxylic acid derivatives bearing pyrrolidine ring and methylamino residues in their structure were synthesized as potential antibacterial drugs. The chemical structures of all the compounds were established by their UV-Vis absorption spectroscopy, IR, 1 H, 13 C NMR and mass spectroscopy. The in vitro antibacterial screening of all novel compounds was done against gram-positive Staphylococcus aureus, Bacillus subtilis and gram-negative Pseudomonas aeruginosa. The results revealed that compounds 5d, e, f and g showed moderate to good activity against the tested microbes.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H264N | ChemSpider

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Design, synthesis, and anticancer potential of the enzyme (PARP-1) inhibitor with computational studies of new triazole, thiazolidinone, – thieno [2, 3-d] pyrimidinones

Background: Thienopyrimidine, triazole and thiazolidinone derivatives have recently gained attention due to their effective pharmacological activities. They show antioxidant, antitumor, antimicrobial, antiviral, anti-inflammatory and analgesic properties. Objective: Synthesis of new ethyl 2-amino-4-isopropyl-5-methylthiophene-3-carboxylate (2) was used as a starting material to produce 2-mercapto-methylthienopyrimidinone (3), (4) and 2- hydrazinyl-methylthienopyrimidinone (5), through high yields and evaluating anticancer activities. Methods: A series of novel Schiff?s bases (6-9) were produced after treatment of (5) with aldehydes. Triazolopyrimidinones (6a, 7a, 8a, 9a) were produced from cyclization of benzylidene (6-9) using Br2 / AcOH or dry pyridine /Ac2O. Thiazolidinones (6b, 7b, 8b, 9b) were synthesized from benzylidene (6-9) with mercaptoacetic acid. Results: All the compounds were synthesized in good yields (55-85%) in a regularly actual system under mild condition. The new compounds have been established by means of diverse spectroscopic ways as IR, NMR and MS. The newly synthesized compounds were evaluated for their antiproliferative activity against the breast MCF-7 carcinoma cell line. Compound (7) showed promising anticancer activity with IC50 of 6.9 muM, and 40.8% of antioxidant effect as DPPH inhibition. Molecular docking of (7) showed deltaG values of-20.54 kcal/ mol and -25.60 kcal/ mol. Molecular dynamics simulation of (7) in complex with PARP-1 revealed RMSD of 3.00 a. Conclusion: The QSAR study confirmed the presence of a relationship between anticancer activity and subdivided surface area descriptors with coefficient r2 = 0.98 with high predictive power.

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Quinuclidine | C7H209N | ChemSpider

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Recent advances in the discovery of HIF-1alpha-p300/CBP inhibitors as anti-cancer agents

Hypoxia-inducible factor-1 (HIF-1), a heterodimeric (containing alpha and beta subunits) transcription factor, is involved in hypoxia response pathway that regulates the expression of many tumor-related genes. The stabilized HIF-1 heterodimer couples to the general co-activators p300/CBP (CREB binding protein), forming an active transcription factor to initiate hypoxic responses. Inhibiting the transcription factor-coactivator HIF-1alpha-p300/CBP interaction represents an attractive approach for blocking hypoxia pathway in tumors. Recently, diverse HIF-1alpha-p300/CBP inhibitors have been designed and their anti-tumor activities have been evaluated. The developments of inhibitors of HIF-1alpha-p300/CBP are discussed in this review. An outline of structures and biological activities of these inhibitors can be traced, along with the approaches for inhibitors discovery. The challenges in identifying novel and selective potent inhibitors of HIF-1alpha-p300/CBP are also put forward.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H480N | ChemSpider

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Computational screening of drugbank database for novel cell cycle inhibitors

The cell cycle is governed by a family of proteins i.e. cyclin dependent kinases (CDKs) and their inhibitors (CDKIs) through activating and inactivating events. Cdks are heteromeric serine/threonine kinases that control progression through the cell cycle in concert with their regulatory subunits, the cyclins. CDK activity was found to increase in different types of human tumors as well as progression and/or invasiveness of some cancers such as breast, leukemia, and melanoma. Computer aided drug design was implemented to find novel compounds as possible CDK inhibitors. Screening of 1400 drugs from DrugBank database was carried out using Molegro software against various CDKs derived from Protein Data Bank. From the result, the best three drugs which exhibited high binding affinity against all targets are reported. The analysis against eight proteins resulted in 14 drugs and the top three drugs obtained are Olmesartan, Verteporfin and Atorvastatin.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H349N | ChemSpider

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Glucosinolate hydrolysis products in the crucifer Barbarea vulgaris include a thiazolidine-2-one from a specific phenolic isomer as well as oxazolidine-2-thiones

Two isomeric phenolic glucosinolates, m- and p-hydroxyl derivatives of epiglucobarbarin [(R)-2-hydroxy-2-phenylethylglucosinolate], co-occur in an eastern chemotype (P-type) of the crucifer Barbarea vulgaris along with epiglucobarbarin itself. Levels of the phenolic derivatives in B. vulgaris were low in summer but higher during fall and winter, allowing isolation of all three glucosinolates. Hydrolysis in vitro, catalyzed by Sinapis alba myrosinase at near neutral pH, resulted in expectable oxazolidine-2-thione type hydrolysis products of epiglucobarbarin and its m-hydroxyl derivative. In contrast, a thiazolidine-2-one type product was formed in vitro from p-hydroxy epiglucobarbarin and characterized by UV, IR, MS/MS and 2D NMR. Maceration of leaf material resulted in disappearance of the glucosinolates and formation of the same oxazolidine-2-thione and thiazolidine-2-one products as found in vitro. The detected amounts were comparable to initial amounts of precursor glucosinolates. The corresponding oxazolidine-2-thione type product was also detected quantitatively from glucobarbarin in foliage of a western genotype (G-type). We suggest that p-hydroxy epiglucobarbarin is initially converted into the conventional oxazolidine-2-thione, which would further rearrange to a thiazolidine-2-one due to the activating effect of the p-hydroxyl group. We conclude that a subtle difference between isomeric phenolic glucosinolates results in significantly different natural hydrolysis products.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H212N | ChemSpider

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Chemistry can be defined as the study of matter and the changes it undergoes. Recommanded Product: Thiazolidin-2-one. You¡¯ll sometimes hear it called the central science because it is the connection between physics and all the other sciences, starting with biology.Recommanded Product: Thiazolidin-2-one, Name is Thiazolidin-2-one, molecular formula is C3H5NOS, introducing its new discovery.

Synthesis and anticancer activity of isatin, oxadiazole and 4-thiazolidinone based conjugates

Following the N-alkylation reaction of starting 2-chloro-N-(5-aryl-1,3,4-oxadiazol-2-yl)-acetamides 1a-c with 2,4-thiazolidinedione or 5-sudstituted isatins the corresponding non-condensed oxadiazole derivatives with thiazolidine 2a-c or isatin 4a-h fragments were synthesized. The obtained compounds have been used in Knoevenagel condensation with 5R-isatin (for 2a-c) or 4-thiazolidinone derivatives (for 4a-h) for synthesis of the appropriate 5-ylidenederivatives 3a-g, 5a-k and 6a-d. Anticancer activity of eight synthesized compounds was evaluated toward 60 human tumor cell lines panel in National Cancer Institute.

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Reference£º
Quinuclidine – Wikipedia,
Quinuclidine | C7H362N | ChemSpider