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A series of innovative 5-(benzofuran-2-yl)-N?-(2-substituted-4-oxothiazolidin-3-yl)-1-phenyl-1H-pyrazole-3- carboxamide (4a-i) derivatives were synthesized by cyclocondensation reaction of various carbohydrazones (3a-i) with thioglycolic acid in DMF. The intermediate N?-(benzylidene)-5-(benzofuran-2-yl)-1- phenyl-1H-pyrazole-3-carbohydrazides (3a-i) was obtained by condensation of 5-(benzofuran-2-yl)-1-phenyl-1Hpyrazole- 3-carbohydrazide (1) with various substituted aromatic aldehydes (2a-i) in ethanol. The structures of newly synthesized compounds (4a-i) were corroborated through elemental analysis and spectral studies like IR, 1H NMR, 13C NMR and Mass spectra. The compounds were screened for their in-vitro antibacterial activity against a panel of pathogenic microorganism including gram-negative strains E. coli, P. vulgaris and S. typhi and grampositive bacterial strain, S. aureus at diverse concentrations and the result of bioassay was compared with Chloramphenicol.

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Background: Infectious diseases symbolize a global consequential strain on public health security and impact on the socio-economic stability all over the world. The increasing resistance to the current antimicrobial treatment has resulted in crucial need for the discovery and development of novel entity for the infectious treatment with different modes of action that could target both sensitive and resistant strains. Methods: Compounds were synthesized using classical methods of organic synthesis. Results: All 20 synthesized compounds showed antibacterial activity against eight Gram-positive and Gram-negative bacterial species. It should be mentioned that all compounds exhibited better antibacterial potency than ampicillin against all bacteria tested. Furthermore, 18 compounds appeared to be more potent than streptomycin against Staphylococcus aureus, Enterobacter cloacae, Pseudomonas aeruginosa, Listeria monocytogenes, and Escherichia coli. Three the most active compounds 4h, 5b, and 5g appeared to be more potent against MRSA than ampicillin, while streptomycin did not show any bactericidal activity. All three compounds displayed better activity also against resistant strains P. aeruginosa and E. coli than ampicillin. Furthermore, all compounds were able to inhibit biofilm formation 2- to 4-times more than both reference drugs. Compounds were evaluated also for their antifungal activity against eight species. The evaluation revealed that all compounds exhibited antifungal activity better than the reference drugs bifonazole and ketoconazole. Molecular docking studies on antibacterial and antifungal targets were performed in order to elucidate the mechanism of antibacterial activity of synthesized compounds. Conclusion: All tested compounds showed good antibacterial and antifungal activity better than that of reference drugs and three the most active compounds could consider as lead compounds for the development of new more potent agents.

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A novel series of Schiff bases 5a-j and 4-thiazolidinones 6a-j have been prepared from the building blocks 2-chloro pyridine-3-carboxylic acid [1] and 2-amino-6-methoxy-benzothiazole [2]. All of the synthesized compounds have been confirmed by elemental analyses, IR, 1H NMR and 13C NMR spectral data. These newly synthesized compounds were screened for their antimicrobial activity. Variable and modest activity was observed against the investigated strains of bacteria and fungi, however, compound 6h revealed significant antibacterial activity against Escherichia coli. Compounds 1, 2, 3, 5c, 5g and 5h, on the other hand, revealed potent antifungal activity against Candida albicans compared to the reference drug greseofulvin.

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The present invention provides methods of screening an agent for activity using teleosts. Methods of screening an agent for angiogenesis activity, toxic activity and an effect cell death activity in teleosts are provided. Methods of screening an agent for an activity in the brain or central nervous system in zebrafish are provided. The invention further provides high throughput methods of screening agents in multi-well plates.

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A library of novel naphthyl bearing 2-iminothiazolidin-4-ones (2-ITZDs) (2 a?2 q) was designed and synthesized through a facile route involving regioselective heterocyclization of unsymmetrical thioureas (1 a?1 q). The synthesis was achieved at ambient temperature in good to excellent yields under catalyst free conditions. The molecular structures of 2-ITZDs were elucidated by spectroscopic techniques such as FT-IR, 1H-NMR and 13C-NMR. X-ray structural data was used to establish the structure (2 o) unequivocally and to define the geometry of exo double bond. The in vitro anticancer activity of 2-ITZDs (2 a?2 q) was investigated in several human cancer cell lines (A549, LNCap, PC-3, MDA-MB-231, BxPC3, MIA PaCa2). All compounds showed cytotoxicity with IC50 values ranging from 6?23 muM in the tested cancer cell lines except MDA-MB-231. Compound 2 k (IC50=7 muM) and the homologous analog 2 q (IC50=6 muM) were found to be equipotent to 2 k and showed moderate cytotoxicity against human breast cell line (DA-MB-231). Furthermore, compound 2 k exhibited a medium permeability, enough metabolic stability and no significant inhibition of hERG channel. Compound 2 k inhibited cytochrome P450 activity below 50 % in 1 A2, 3 A4 and 2 C19, but not in 2 C9 and 2D6 at 10 muM. Structure-activity relationships (SAR) provided useful insights towards this class of compounds and tiled a way to design novel analogues with increased potency.

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Schiff bases [1]a,b were prepared from the reaction of 2-amino-5-mercapto-1,3,4-thiadiazole with aromatic aldehydes. In the present study a series of some four, five-and seven-membered heterocyclic compounds have been synthesized by the reaction of schiff bases [1]a,b with thioglycolic acid, chloroacetyl chloride, sodium azide or various anhydrides to give thiazolidinone [2]a, azetidinone [6]b, tetrazole [7]b and 1,3-oxazepine derivatives [14-16]b respectively, then compounds[2]a, [6,7]b and[14-16]b were reacted with Na2CO3 of distilled water as a solvent, then of ClCH2COOH was added to produce [3]a, [8,9]band[17-19]b. The compounds [3]a, [8,9]b and [17-19]b reacted with SOCl2 in the presence of Benzene to producing the compounds [4]a, [10,11]b and [20-22]b. Chemical modification of Poly(vinyl alcohol) were obtained by reaction of PVA with compounds [4]a, [10,11]b and [20-22]b using the Dimethyl formamide to produce compounds [5]a,[12,13]b and [23-25]b. The structure of the synthesized compounds were set by their analytical and spectral data such as, FTIR spectra,1H-NMR., UV-Vis Spectroscopy and Elemental analysis (CHNS). Finally study antibacterial activity screened via two types of bacteria. Anticancer activity also examined for all modifier polyvinyl alcohol.

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A highly efficient three-component reaction has been developed for the synthesis of thiazolidinones involving the reaction of 2-amino-1-phenylethanone hydrochloride with an aromatic aldehyde and mercaptoacetic acid in the presence of diisopropylethylamine in a single pot. Critically, this reaction exhibited excellent chemoselectivity, with the nitrogen atom of the 2-amino-1-phenylethanone component reacting selectively with the aromatic aldehyde to give the corresponding Schiff base. Nucleophilic attack at the carbon of the Schiff base by the sulfur atom of mercaptoacetic, followed by a cyclocondensation reaction between the nitrogen and the carboxylic acid moiety afforded the desired thiazolidinones, which were fully characterized by spectroscopic techniques.

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The ongoing spread of multidrug-resistant bacteria demands an intensive search for new antibacterial agents. In the present study, a series of new 1,3-thiazolidin-4-ones has been synthesized and investigated for its in vitro antibacterial activity. The most potent antibacterial compound 4c was found to be active, at low micromolar range, against Staphylococcus aureus, Staphylococcus epidermidis, Enterococcus faecalis and the pneumonic plague causative agent Yersinia pestis with minimum inhibitory concentrations of 5 muM, 2.5 muM, 2.5 muM and 5 muM, respectively. Compound 4c showed the ability to kill E. faecalis JH212 strain with a minimum bactericidal concentration of 5 muM. Furthermore, compounds 9b and 10a inhibited the biofilm formation in S. epidermidis, where they showed 70% to 80% inhibition at a concentration of 40 muM.

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A new 2-iminothiazolidin-4-ones compound and its derivatives were synthesized and characterized by FT-IR, CHN, and1HNMR techniques. The target compounds were assessed for their anti-inflammatory and analgesic activities, and the study was performed using Swiss albino mice (25-30 g) for investigation. A hind edema model caused by carrageenan, while the analgesic activity was assessed using an acetic acid-induced writhing and a hot plate test evaluated the anti-inflammatory activity.

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A series of innovative 5-(benzofuran-2-yl)-N?-(2-substituted-4-oxothiazolidin-3-yl)-1-phenyl-1H-pyrazole-3- carboxamide (4a-i) derivatives were synthesized by cyclocondensation reaction of various carbohydrazones (3a-i) with thioglycolic acid in DMF. The intermediate N?-(benzylidene)-5-(benzofuran-2-yl)-1- phenyl-1H-pyrazole-3-carbohydrazides (3a-i) was obtained by condensation of 5-(benzofuran-2-yl)-1-phenyl-1Hpyrazole- 3-carbohydrazide (1) with various substituted aromatic aldehydes (2a-i) in ethanol. The structures of newly synthesized compounds (4a-i) were corroborated through elemental analysis and spectral studies like IR, 1H NMR, 13C NMR and Mass spectra. The compounds were screened for their in-vitro antibacterial activity against a panel of pathogenic microorganism including gram-negative strains E. coli, P. vulgaris and S. typhi and grampositive bacterial strain, S. aureus at diverse concentrations and the result of bioassay was compared with Chloramphenicol.

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