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Progress and prospects on DENV protease inhibitors

New treatments are desperately required to combat increasing rate of dengue fever cases reported in tropical and sub-tropical parts of the world. Among the ten proteins (structural and non-structural) encoded by dengue viral genome, NS2B-NS3 protease is an ideal target for drug discovery. It is responsible for the processing of poly protein that is required for genome replication of the virus. Moreover, inhibitors designed against proteases were found successful in Human Immuno-deficiency Virus (HIV) and Hepatitis C Virus (HCV). Complete molecular mechanism and a survey of inhibitors reported against dengue protease will be helpful in designing effective and potent inhibitors. This review provides an insight on molecular mechanism of dengue virus protease and covers up-to-date information on different inhibitors reported against dengue proteases with medicinal chemistry perspective.

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Design, synthesis and application of a new type of bifunctional Le-Phos in highly enantioselective gamma-addition reactions of N-centered nucleophiles to allenoates

A novel class of cyclic phosphine derived bifunctional catalysts (Le-Phos) is reported, which can be readily prepared from inexpensive and commercially available starting materials and exhibit good performances in enantioselective gamma-addition reactions of N-centered nucleophiles and allenoates under mild conditions. The salient features of this reaction include high product yields, good enantioselectivity, mild reaction conditions, and broad substrate scope and gram-scale scalability.

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Application of 2682-49-7, In homogeneous catalysis, the catalyst is in the same phase as the reactant. The number of collisions between reactants and catalyst is at a maximum.In a patent, Application of 2682-49-7, name is Thiazolidin-2-one, introducing its new discovery.

Synthesis and antibacterial studies of some 2-(p-substituted benzylidene)-3-(5-methyl-1,3,4-thiadiazol-2-yl)-thiazolidin-4-ones

A series of 2-(p-substituted benzylidene)-3-(5-methyl-1, 3, 4-thiadiazol-2-yl) thiazolidin-4-ones were synthesized by the reaction of Schiff’s bases of N-(p-substituted benzylidene)-5-methyl-1, 3, 4-thiadiazole-2-amines with thioglycolic acid in 1, 4-dioxane as solvent and studied for their in vitro antibacterial activity. Reaction of N-(psubstituted benzylidene)-5-methyl-1, 3, 4-thiadiazole-2-amines with different p-substituted benzaldehydes yielded the compounds Schiff’s bases of N-(p-substituted benzylidene)-5-methyl-1,3, 4-thiadiazole-2-amines which is further reaction with thioglycollic acid in presence of small amount of zinc chloride in 1,4 dioxane as solvent gave title compounds. These compounds were characterized by spectral analysis. All the synthesized compounds were evaluated for their in vitro for their antibacterial activity against two Gram positive bacterial strains (Bacillus subtilis and Staphylococcus aureus) and two Gram negative bacterial strains (Escherichia coli and Pseudomonas aeruginosa) and their minimum inhibitory concentration (MIC) were determined.

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In heterogeneous catalysis, the catalyst is in a different phase from the reactants. Quality Control of Thiazolidin-2-one, At least one of the reactants interacts with the solid surface in a physical process called adsorption in such a way. 2682-49-7, name is Thiazolidin-2-one. In an article,Which mentioned a new discovery about 2682-49-7

Synthesis and biological activity of some new thiazolidinone derivatives

The compound [G1] was prepared from the reaction of thiosemicarbazide with para-hydroxyphenylmethyl ketone in ethanol as a solvent. Then by sequence reactions prepared [G2] and [G3] compounds. The compound [G4] reaction with ethyl acetoacetoneto synthesized compound [G6] and acetyl acetone to synthesized compound [G5]. Reaction the [G3] with two different types of aldehydes in the present of pipredine to form new alkenes compounds [G7]and [G8].The compound [G3] reacted with hydrazine hydrate to formation[G4] with present the hydrazine hydrade 80% in (10) ml of absolute ethanol. Latter the compound [G4]reacted with different aldehydes with present the glacial acetic acid and the solvent was ethanol to formed the Schiff bases compounds[G9] and [G10]. All the prepared compounds were characterized by FT-IR, 1H-NMR spectra, also biologically activity evaluated, the synthesized derivatives have been screened for their two species of bacteria were used in this study as tested organisms. These are Escherichia Coli (Gram negative) and staphylococcus (Gram positive).

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Quinuclidine – Wikipedia,
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In homogeneous catalysis, the catalyst is in the same phase as the reactant. The number of collisions between reactants and catalyst is at a maximum.In a patent, 2682-49-7, name is Thiazolidin-2-one, introducing its new discovery. Formula: C3H5NOS

Synthesis, ADME evaluation, and in vitro antimycobacterial studies of a novel series of 2-thiazolylimino-5-arylidene-4-thiazolidinone derivatives

Background: The emergence of multi-drug resistant and extensively drug-resistant cases of tuberculosis has lead to the search for new structural classes of anti-tuberculosis drugs. There are many reports on antimycobacterial screening of compounds containing the 4-thiazolidinone moiety. The 5-arylidene moiety in the 2-heteroarylimino-5-benzylidene-4-thiazolidinone scaffold plays an important role in antimicrobial activity against Gram-positive and Gram-negative bacteria, yeasts and moulds. Objective: To synthesize 2-thiazolylimino-5-arylidene-4-thiazolidinone derivatives, with different substituents on the aryl ring, and evaluate their in vitro antimycobacterial activity against M. tb H37Rv. Methods: The derivatives were synthesized by previously reported methods, and structures confirmed by spectral data. Qikprop, the ADME prediction program was used in predicting pharmacokinetic properties of the derivatives, which helped in designing and synthesis of novel and more potent analogs. In vitro antimycobacterial activity against drug-sensitive M. tb H37Rv was performed in BACTEC-460 TB radiometric system. Results: The synthesis and antimycobacterial activities of 2-thiazolylimino-5-arylidene-4-thiazolidinone derivatives have been reported. The chemical modifications not only altered the physicochemical properties but also pharmacological activities. The compounds exhibited moderate to excellent in vitro activity (88-99.7% inhibition) against M. tb H37Rv, and few demonstrated >99% inhibition at 6.25 mug/mL. The activity was considerably affected by various substituents and compounds with di- and trisubstitutions on the aromatic ring of the 4-thiazolidinone were more active. Conclusion: These preliminary but encouraging results indicate that 2-thiazolylimino-5-arylidene-4- thiazolidinones are promising scaffolds for design and development of new molecules for antimycobacterial activity. Several compounds were identified as novel and potential lead for design and synthesis of new antimycobacterial agents.

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Quinuclidine – Wikipedia,
Quinuclidine | C7H381N | ChemSpider

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Synthetic Route of 2682-49-7, Chemistry is the science of change. But why do chemical reactions take place? Why do chemicals react with each other? The answer is in thermodynamics and kinetics.In a document type is Article, and a compound is mentioned, 2682-49-7, Thiazolidin-2-one, introducing its new discovery.

Benzothiazole incorporated thiazolidin-4-ones and azetidin-2-ones derivatives: Synthesis and in vitro antimicrobial evaluation

In this study, a series of novel thiazolidin-4-ones (5a?g) and azetidin-2-ones (6a?g) were synthesized from N-(6-chlorobenzo[d]thiazol-2-yl)hydrazine carboxamide derivatives of the benzothiazole class. Antimicrobial properties of the title compound derivatives were investigated against one Gram (+) bacteria (Staphylococcus aureus), three Gram (?) bacteria (Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumoniae) and five fungi (Candida albicans, Aspergillus niger, Aspergillus flavus, Monascus purpureus and Penicillium citrinum) using serial plate dilution method. The investigation of antibacterial and antifungal screening data revealed that all the tested compounds showed moderate to good inhibition at 12.5?200 mug/mL in DMSO. It has been observed that azetidin-2-ones derivatives are found to be more active than thiazolidin-4-ones derivatives against all pathogenic bacterial and fungal strains.

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Related Products of 2682-49-7, One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, such as the rate of change in the concentration of reactants or products with time.In a article, authors is Mangasuli, Sumitra N., mentioned the application of Related Products of 2682-49-7, Name is Thiazolidin-2-one, molecular formula is C3H5NOS

Synthesis, molecular docking studies and biological evaluation of potent coumarin-thiazolidinone hybrids: An approach to microwave synthesis

We report a series of C?N bridged coumarin-thiazolidine-2,4-dione derivatives 3(a?q). These compounds have been synthesized under both conventional as well as microwave irradiation techniques. The synthesized compounds were characterized by spectral and elemental analyses. The computational study performed for targeted compounds and results obtained were mimicking the potent bio-molecules. All the newly synthesized compounds were screened for their in vitro anti-microbial and anti-inflammatory activities and have shown promising results. In vitro Anti-microbial activity of compounds (3a) and (3i) was found to be most active with bacterial and fungal strains. The compound (3i) shows best anti-inflammatory activity with IC50 of 43.26 mug/mL against protein denaturation.

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Gonadotropins and Their Analogs: Current and Potential Clinical Applications

The gonadotropin receptors LH receptor and FSH receptor play a central role in governing reproductive competency/fertility. Gonadotropin hormone analogs have been used clinically for decades in assisted reproductive therapies and in the treatment of various infertility disorders. Though these treatments are effective, the clinical protocols demand multiple injections, and the hormone preparations can lack uniformity and stability. The past two decades have seen a drive to develop chimeric and modified peptide analogs with more desirable pharmacokinetic profiles, with some displaying clinical efficacy, such as corifollitropin alfa, which is now in clinical use. More recently, low-molecular-weight, orally active molecules with activity at gonadotropin receptors have been developed. Some have excellent characteristics in animals and in human studies but have not reached the market-largely as a result of acquisitions by large pharma. Nonetheless, such molecules have the potential to mitigate risks currently associated with gonadotropin-based fertility treatments, such as ovarian hyperstimulation syndrome and the demands of injection-based therapies. There is also scope for novel use beyond the current remit of gonadotropin analogs in fertility treatments, including application as novel contraceptives; in the treatment of polycystic ovary syndrome; in the restoration of function to inactivating mutations of gonadotropin receptors; in the treatment of ovarian and prostate cancers; and in the prevention of bone loss and weight gain in postmenopausal women. Here we review the properties and clinical application of current gonadotropin preparations and their analogs, as well as the development of novel orally active, small-molecule nonpeptide analogs.

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Colorimetric probes based on bioactive organic dyes for selective sensing of cyanide and fluoride ions

Eight novel bioactive azo dyes containing thiazolidinone (TZD) derivatives (1O-4S) were designed and synthesized for antibacterial assays and colorimetric sensing of anions. Synthesized compounds were evaluated for their antibacterial activities using the disc diffusion technique. Majority of the compounds showed potent antibacterial activities against the tested bacterial strains in the zone assay. Moderate antibacterial activities were also exhibited in the minimum inhibitory concentration (MIC) assay. In addition, the synthesized compounds were evaluated for their colorimetric sensing of anions. In contrast to dyes with electron donating groups (EDGs), 4O having electron withdrawing groups (EWGs) showed highly selective colorimetric sensing of CN- ions. Binding interaction of 4O with CN- ions provides a remarkable colorimetric response from yellow to blue (Deltalambda = 186 nm), enabling naked-eye sensing without any spectroscopic instrumentation. Furthermore, the limit of detection (LOD) for 4O towards CN- was found to be 0.74 muM.

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Quinuclidine – Wikipedia,
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Related Products of 2682-49-7, Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 2682-49-7, molcular formula is C3H5NOS, introducing its new discovery.

Syntheses, characterization and evaluation of some 3-(Benzothiazol-2-yl)-2-(4-substituted phenyl) thiazolidin-4-ones as antimicrobial agents

Background: The increasing predominance of microbial resistance towards available antimicrobial drugs urges the need to develop novel antimicrobial agents that will be effective against resistant bacteria and fungi. Objective: A series of 3-(benzothiazol-2-yl)-2-(4-substituted phenyl) thiazolidin-4-one derivatives were synthesized as pharmacophore hybrid of benzothiazole and thiazolidin-4-one moieties as exclusive antimicrobial agents. Methods: Proposed compounds were synthesized by four step reactions. First three steps involved synthesis of phenylthiourea, benzothiazol-2-ylamine and Schiff?s base srespectively. Finally, Schiff`s baseswere cyclized in the presence of thioglycolic acid to yield 4-thiazolidinone derivatives (2a-g), characterized by spectroscopic and elemental analysis. Resulted compounds were evaluated for their in vitro antimicrobial activities against four bacterial (Staphylococcus aureus, Bacillus subtilis, Escherichia coli and Pseudomonas aeruginosa) and two fungal (A. niger and P. crysogenum) strains using agar diffusion method. The minimum inhibitory concentrations (MIC) of the synthesized compounds were also determined by tube dilution method. Results: All the compounds displayed good to moderate antimicrobial activity. Compound 2d was found most potent against Bacillus subtilis (MIC25mug/ml), whereas compound 2e was most active (MIC 25mug/ml) against Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa. Conclusion: The compounds having electron-withdrawing groups in the phenyl ring exhibited promising activity. A correlation between the antimicrobial activity and Log P was also established. Most active compounds can be considered as the potential antibacterial agents and deserve further investigation for their pharmacological and toxicological profiling.

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Quinuclidine – Wikipedia,
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