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The basic objective of this investigation is to explore potential metallo-organic antimicrobial agents based on silver?heterocyclic-2-thiones. In this respect, a series of silver(I) halide complexes with imidazolidine-2-thiones (L-NR, R = H, Me, Et, Prn, Bun, Ph), namely, mononuclear [AgX(L-NR)(PPh3)2] (X, R: Cl, Bu, 1; Br, Ph, 7); [AgX(L-NR)3] (Br, Bu, 5; Br, Prn, 8) and halogen bridged dinuclear [Ag2(mu-X)2(L-NR)2(PPh3)2] (Cl, Bun, 2; Cl, Ph, 3; Cl, Prn, 4; Br, Ph, 6) have been synthesized and characterized using modern techniques. The thio-ligands are terminally S-bonded in all the complexes. The in vitro antimicrobial potential and biosafety evaluation of the above complexes as well as that of previously reported analogous silver complexes has been studied against Gram positive bacteria, namely, Staphylococcus aureus (MTCC 740) and Methicillin resistant Staphylococcus aureus (MRSA), Gram negative bacteria Klebsiella pneumoniae (MTCC 109), Salmonella typhimurium (MTCC 98) and a yeast Candida albicans (MTCC 227). Most of the complexes tested have shown significant antimicrobial activity with low values of minimum inhibitory concentration (MIC). Significantly, the activity against MRSA is an important outcome of this investigation. Among complexes tested for their cytotoxicity using MTT [3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyl tetrazolium bromide] assay, some complexes showed low cellular toxicity with high percent cell viability. A dinuclear complex [Ag2(mu-Cl)2(L-NPh)2(PPh3)2] 3 with 93.3% cell viability emerges the most important candidate for further investigations.

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Reference:
Thiazole | C3H6292NS – PubChem,
Thiazole | chemical compound | Britannica

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In the present work, 12 new 2-(5-substituted-benzothiazol-2-ylsulfanyl)-N-(substitutedbenzyl)-N-(4-substitutedphenyl) acetamide derivatives (4a?l) was designed and synthesized. The structures of the synthesized compounds were clarified using Fourier transform infrared spectroscopy (FTIR), proton nuclear magnetic resonance (1H-NMR), carbon-13 nuclear magnetic resonance (13C-NMR) and high-resolution mass spectrometry (HRMS) spectral data. Purity of synthesized compounds was checked by high-performance liquid chromatography (HPLC) analyses and purity ratio was found between 96.5?99.9%. The inhibitory activity of the compounds against MAO-A and MAO-B enzymes was evaluated by using in vitro flurometric method in which kynuramine was used as a substrate. Most of the compounds exhibited more selective inhibitory activity towards monoamine oxidase B (MAO-B) than monoamine oxidase A (MAO-A). Compound 4h was determined as the most potent compound against both enzyme types. The MAO-B enzyme kinetic of the compound 4h was studied and nature of MAO-B inhibition, caused by this compound, was investigated. The graphical analysis of steady-state inhibition data indicated that compound 4h is a mixed type inhibitor. Theoretical calculation of absorption, distribution, metabolism, excretion (ADME) properties for the synthesized compounds was also carried out and observed data supported the potential of compound 4h.

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Reference:
Thiazole | C3H6325NS – PubChem,
Thiazole | chemical compound | Britannica

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Synthesis of N-(Chloromethyl)-2,6-diethylcarbaniloyl Chloride (1) and Derivatives <1>

The reaction of N-methylene-2,6-diethylbenzenamine with phosgene furnished the titled compound 1.The reaction of 1 with the potassium salts of thiazolethiols in an acetone medium afforded the expected N-substituted 2,6-diethylthiolcarbanilates 2-6.Substituting the above thiazolethiols with the potassium salt of 2-mercaptobenzimidazole furnished a novel heterocyclic compound 7 in 98percent yield.The reaction of 1 with the triethylamine salt of disubstituted-dithiocarbamic acids afforded an alternative method for the synthesis of bis(N-substituted-thiocarbonyl)sulfides 8 and 9.

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Reference:
Thiazole | C3H6277NS – PubChem,
Thiazole | chemical compound | Britannica

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Ag+ complexes as potential therapeutic agents in medicine and pharmacy

Silver is a non-essential element with promising antimicrobial and anticancer properties. This work is a detailed summary of the newest findings on the bioinorganic chemistry of silver, with a special focus on the applications of Ag+ complexes and nanoparticles. The coordination chemistry of silver is given a reasonable amount of attention, summarizing the most common silver binding sites and giving examples of such binding motifs in biologically important proteins. Possible applications of this metal and its complexes in medicine, particularly as antibacterial and antifungal agents and in cancer therapy, are discussed in detail. The most recent data on silver nanoparticles are also summarized.

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Reference:
Thiazole | C3H6299NS – PubChem,
Thiazole | chemical compound | Britannica

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Synthesis, Characterization, and Molecular Docking Study of Some Novel Imidazole Derivatives as Potential Antifungal Agents

The azole pharmacophore is still regarded as a viable lead structure for the synthesis of more effective antifungal agents. In this study, two novel series of imidazole derivatives containing dithiocarbamate (5a?5g) and (benz)azolethiol (6a?6n) side chains that are structurally related to the famous antifungal azole pharmacophore were synthesized, and the structures of them were characterized by spectral (IR, 1H NMR, 13C NMR, and MS spectra) analyses. The synthesized compounds were screened in vitro antifungal activity against pathogenic strains fungi. Theoretical ADME (absorption, distribution, metabolism, and excretion) predictions were calculated for final compounds. A molecular docking study of the most active compound with target ?lanosterol 14alpha-demethylase? (CYP51) was performed to unravel the mode of antifungal action. Compound 5e, which features imidazole and 4-methoxybenzyl piperazine scaffolds, showed the most promising antifungal activity with an MIC50 value of 0.78 mug/mL against C. krusei. Effect of the compound 5e against ergosterol biosynthesis was observed by LC?MS?MS method, which is based on quantification of ergosterol level in C. krusei.

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Reference:
Thiazole | C3H6293NS – PubChem,
Thiazole | chemical compound | Britannica

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Transition-metal-free formal sonogashira coupling and alpha-carbonyl arylation reactions

Transition-metal-free formal Sonogashira coupling and alpha-carbonyl arylation reactions have been developed. These transformations are based on the nucleophilic aromatic substitution (SNAr) of beta-carbonyl sulfones to electron-deficient aryl fluorides, producing a key intermediate that, depending on the reaction conditions, gives the aromatic alkynes or alpha-aryl carbonyl compounds. The development of these reactions is presented and, based on investigations under basic and acidic conditions, mechanisms have been proposed. To develop the formal disclosed that expands the reaction concept. The scope of these reactions is demonstrated for the synthesis of Sonogashira and alpha-carbonyl arylated products from a range of electron-deficient aryl fluorides with a variety of functional groups and aryl-, heteroaryl-, alkyl-, and alkoxy-substituted sulfone nucleophiles. These transition-metal-free reactions complement the metal-catalyzed versions in terms of substitution patterns, simplicity, and reaction conditions.

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Reference:
Thiazole | C3H6266NS – PubChem,
Thiazole | chemical compound | Britannica

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Enhancing ganglioside species detection for MALDI-TOF imaging mass spectrometry in negative reflectron mode

Enhanced ganglioside species detection was achieved for matrix assisted laser desorption ionization time-of-flight imaging mass spectrometry (MALDI-TOF IMS) in negative reflectron mode using a novel sample preparation protocol that involves washing the tissue in ammonium salt solutions followed by spray depositing ammonium salts and waiting 24. h after sublimation of 1,5-diaminonaphthalene (DAN) before data acquisition. Application of this novel method to normal adult mouse brains led to more than 10-fold increase in total ion intensity in the ganglioside mass range and an increase in the number of detected sialylated species from 3 to 15, with no apparent delocalization observed at 20. mum spatial resolution, making it a powerful technique with the potential to provide greater information about gangliosides in numerous biological contexts.

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Reference:
Thiazole | C3H6331NS – PubChem,
Thiazole | chemical compound | Britannica

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Synthesis, in vitro alpha-glucosidase inhibitory activity and molecular docking studies of novel benzothiazole-triazole derivatives

Benzothiazole-triazole derivatives 6a?6s have been synthesized and characterized by1H-NMR and13C-NMR. All synthetic compounds were screened for their in vitro alpha-glucosidase inhibitory activity by using Baker?s yeast alpha-glucosidase enzyme. The majority of compounds exhibited a varying degree of alpha-glucosidase inhibitory activity with IC50 values between 20.7 and 61.1 muM when compared with standard acarbose (IC50 = 817.38 muM). Among the series, compound 6s (IC50 = 20.7 muM) bearing a chlorine group at the 5-position of the benzothiazole ring and a tert-butyl group at the para position of the phenyl ring, was found to be the most active compound. Preliminary structure-activity relationships were established. Molecular docking studies were performed to predict the binding interaction of the compounds in the binding pocket of the enzyme.

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Reference:
Thiazole | C3H6348NS – PubChem,
Thiazole | chemical compound | Britannica

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Chiral beta – amino derivatives of the preparation method (by machine translation)

The invention belongs to the technical field of chemical synthesis, in particular to a chiral beta – amino derivatives of the preparation method. The chiral beta – amino derivatives of the preparation method, comprises the following steps: providing a formula I indicated by the azetidine quaternary ammonium salt, shown as formula II of the nucleophiles; will of the said heterocyclic butane quaternary ammonium salt and the nucleophiles soluble in the organic solvent in the 1st, in alkali and formula III shown under the condition of the catalyst of the asymmetric ring-opening reaction, shown as formula IV obtained chiral beta – amino derivatives. This invention adopts the chiral phosphate chiral catalyst, can be effective to form a chiral phosphorus acid salt, promote the reaction system the occurrence of ion exchange, and then high-efficiency, high selectively to get chiral beta – amino derivative product. Therefore, the preparation method is not merely the reaction condition is simple and easy to control, but also selectively high, to obtain high purity of product. (by machine translation)

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Thiazole | C3H6283NS – PubChem,
Thiazole | chemical compound | Britannica

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Design, synthesis and biological evaluation of some tetrazole acetamide derivatives as novel non-carboxylic PTP1B inhibitors

A series of ten N-(3-(1H-tetrazole-5-yl)phenyl)acetamide derivatives (NM-07 to NM-16) designed from a lead molecule identified previously in our laboratory were synthesized and evaluated for protein tyrosine phosphatase 1B (PTP1B) inhibitory activity. Among the synthesized molecules, NM-14, a 5-Cl substituted benzothiazole analogue elicited significant PTP1B inhibition with an IC50 of 1.88 muM against reference standard suramin (IC50 ? 10 muM). Furthermore, this molecule also showed good in vivo antidiabetic activity which was comparable to that of standard antidiabetic drugs metformin and glimepiride. Overall, the results of the study clearly reveal that the reported tetrazole derivatives especially NM-14 are valuable prototypes for the development of novel non-carboxylic inhibitors of PTP1B with antidiabetic potential.

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Reference:
Thiazole | C3H6361NS – PubChem,
Thiazole | chemical compound | Britannica