scholarly journals Design, Synthesis and Characterization of Novel Isoxazole Tagged Indole Hybrid Compounds

2020 ◽  
Vol 18 (1) ◽  
pp. 138-148 ◽  
Author(s):  
Raed A. Al-Qawasmeh ◽  
Louy A. Al-Nazer ◽  
Sarah A. Dawlat-Kari ◽  
Luay Abu-Qatouseh ◽  
Salim S. Sabri ◽  
...  
Keyword(s):  
Chemical Structure ◽  
Bacterial Strains ◽  
Anticancer Activities ◽  
Design Synthesis ◽  
X Ray ◽  
Hybrid Compounds ◽  
Indole Compounds ◽  
New Compounds ◽  
Single Crystal Analysis

AbstractSixteen new isoxazole tagged indole compounds have been synthesized via copper (I) catalyzed click chemistry of the aryl hydroxamoyl chloride and an indole containing alkyne moiety. The chemical structure of the synthesized compounds has been established using various physicochemical techniques. X-ray single crystal analysis of Ethyl 1-((3-phenylisoxazol-5-yl) methyl)-1H-indole-2-carboxylate (8a) has been analyzed. All compounds were tested for their antibacterial and anticancer activities. The activities for the new compounds were weak against both bacterial strains and the cancer cell lines.

scholarly journals Design, Synthesis, Experimental and Theoretical Characterization of a New Multitarget 2-Thienyl-N-Acylhydrazone Derivative

2018 ◽  
Vol 11 (4) ◽  
pp. 119 ◽  
Author(s):  
Isadora Bastos ◽  
Pedro Pinheiro ◽  
Fanny Costa ◽  
Miguel Rocha ◽  
Carlos Sant’Anna ◽  
...  
Keyword(s):  
Intramolecular Interaction ◽  
Pde4 Inhibitor ◽  
Drug Candidate ◽  
Design Synthesis ◽  
Adequate Treatment ◽  
X Ray ◽  
A2a Receptor ◽  
Pulmonary Arterial ◽  
Adenosine A2a

Pulmonary arterial hypertension (PAH) is a chronic cardiovascular disease that displays inflammatory components, which contributes to the difficulty of adequate treatment with the available therapeutic arsenal. In this context, the N-acylhydrazone derivative LASSBio-1359 was previously described as a multitarget drug candidate able to revert the events associated with the progression of PAH in animal models. However, in spite of having a dual profile as PDE4 inhibitor and adenosine A2A receptor agonist, LASSBio-1359 does not present balanced potencies in the modulation of these two targets, which difficult its therapeutic use. In this paper, we describe the design concept of LASSBio-1835, a novel structural analogue of LASSBio-1359, planned by exploiting ring bioisosterism. Using X-ray powder diffraction, calorimetric techniques, and molecular modeling, we clearly indicate the presence of a preferred synperiplanar conformation at the amide function, which is fixed by an intramolecular 1,5-N∙∙∙S σ-hole intramolecular interaction. Moreover, the evaluation of LASSBio-1835 (4) as a PDE4 inhibitor and as an A2A agonist confirms it presents a more balanced dual profile, being considered a promising prototype for the treatment of PAH.

Crystallographic characterization of three cathinone hydrochlorides new on the NPS market: 1-(4-methylphenyl)-2-(pyrrolidin-1-yl)hexan-1-one (4-MPHP), 4-methyl-1-phenyl-2-(pyrrolidin-1-yl)pentan-1-one (α-PiHP) and 2-(methylamino)-1-(4-methylphenyl)pentan-1-one (4-MPD)

2022 ◽  
Vol 78 (1) ◽  
Author(s):  
Marcin Rojkiewicz ◽  
Piotr Kuś ◽  
Maria Książek ◽  
Joachim Kusz
Keyword(s):  
Chemical Structure ◽  
Crystallographic Data ◽  
New Psychoactive Substances ◽  
Monoclinic Space Group ◽  
Psychoactive Substances ◽  
Space Group ◽  
X Ray ◽  
X Ray Crystallography ◽  
Analytical Laboratories

Cathinones belong to a group of compounds of great interest in the new psychoactive substances (NPS) market. Constant changes to the chemical structure made by the producers of these compounds require a quick reaction from analytical laboratories in ascertaining their characteristics. In this article, three cathinone derivatives were characterized by X-ray crystallography. The investigated compounds were confirmed as: 1-[1-(4-methylphenyl)-1-oxohexan-2-yl]pyrrolidin-1-ium chloride (1, C17H26NO+·Cl−, the hydrochloride of 4-MPHP), 1-(4-methyl-1-oxo-1-phenylpentan-2-yl)pyrrolidin-1-ium chloride (2; C16H24NO+·Cl−, the hydrochloride of α-PiHP) and methyl[1-(4-methylphenyl)-1-oxopentan-2-yl]azanium chloride (3; C13H20NO+·Cl−, the hydrochloride of 4-MPD). All the salts crystallize in a monoclinic space group: 1 and 2 in P21/c, and 3 in P21/n. To the best of our knowledge, this study provides the first detailed and comprehensive crystallographic data on salts 1–3.

scholarly journals Insecticidal Activity of Bacteria from Larvae Breeding Site with Natural Larvae Mortality: Screening of Separated Supernatant and Pellet Fractions

Pathogens ◽  
2020 ◽  
Vol 9 (6) ◽  
pp. 486 ◽  
Author(s):  
Handi Dahmana ◽  
Didier Raoult ◽  
Florence Fenollar ◽  
Oleg Mediannikov
Keyword(s):  
Biological Control ◽  
Insecticidal Activity ◽  
Breeding Site ◽  
Bacterial Strains ◽  
Activity Prediction ◽  
Pcr Screening ◽  
Breeding Sites ◽  
Insecticide Activity ◽  
New Compounds

Mosquitoes can transmit to humans devastating and deadly pathogens. As many chemical insecticides are banned due to environmental side effects or are of reduced efficacy due to resistance, biological control, including the use of bacterial strains with insecticidal activity, is of increasing interest and importance. The urgent actual need relies on the discovery of new compounds, preferably of a biological nature. Here, we explored the phenomenon of natural larvae mortality in larval breeding sites to identify potential novel compounds that may be used in biological control. From there, we isolated 14 bacterial strains of the phylum Firmicutes, most of the order Bacillales. Cultures were carried out under controlled conditions and were separated on supernatant and pellet fractions. The two fractions and a 1:1 mixture of the two fractions were tested on L3 and early L4 Aedes albopictus. Two concentrations were tested (2 and 6 mg/L). Larvae mortality was recorded at 24, 48 and 72 h and compared to that induced by the commercialized B. thuringiensis subsp. israelensis. Of the 14 strains isolated, 11 were active against the A. albopictus larvae: 10 of the supernatant fractions and one pellet fraction, and mortality increased with the concentration. For the insecticide activity prediction in three strains of the Bacillus cereus complex, PCR screening of the crystal (Cry) and cytolytic (Cyt) protein families characteristic to B. thuringiensis subsp. israelensis was performed. Most of the genes coding for these proteins’ synthesis were not detected. We identified bacterial strains that exhibit higher insecticidal activity compared with a commercial product. Further studies are needed for the characterization of active compounds.

Darstellung und Charakterisierung des Zwitterions S2C—C(NMe2)2; eine übergangsmetallinduzierte C—C-Kopplung. Komplexchemie der Zwitterionen S2C—C(NR2)2 / Synthesis and Characterization of the Zwitter Ion S2C —C(NMe2)2; a Transition Metal Induced C —C Coupling. Complex Chemistry of the Zwitter Ions S2C —C(NR2)2

1987 ◽  
Vol 42 (11) ◽  
pp. 1411-1418 ◽  
Author(s):  
Manfred L. Ziegler ◽  
Hannelore Weber ◽  
Bernhard Nuber ◽  
Orhan Serhadle
Keyword(s):  
Transition Metal ◽  
Synthesis And Characterization ◽  
X Ray ◽  
Zwitter Ion ◽  
Complex Chemistry ◽  
New Compounds

A transition metal induced C-C coupling by the reaction of W2(N(CH3)2)6, (4) and CS2 yielded the zwitter ion S2C-C(N(CH3)2)2 (1d) besides W2(N(CH3)2)2(CS2)2S4 (5). The com- plex chemistry of the zwitter ions 1d and S2CC(N(CH2)4X)2 (X = CH2, O) has been investigated by their reaction with (η5-C5H5)2Mo2(CO)4 (2) and (η5-C5H5)Mo(CO)3Cl (3). Reaction of the former led to complexes (η5-C5H5)Mo(CO)2(S2CR) (R = N(CH3)2, N(CH2)4X) and the new compounds [(η5-C5H5)Mo(CO)2(S2C-CR2)]+. X-ray structure analyses of 1d and ((η5-C5H5)Mo(CO)2(S2C-C(N(CH2)5)2)]⊕PF6⊖ (10b) are described.

Synthesis and structural characterization of zinc complexes of the imido–amido phosphate anions OP[(NHR)3–x(NR)]x– (R = Me, t-Bu; x = 1–3) and EP[(NH-t-Bu)2(N-t-Bu)]– (E = S, NSiMe3)

2005 ◽  
Vol 83 (10) ◽  
pp. 1768-1778 ◽  
Author(s):  
Andrea F Armstrong ◽  
Tristram Chivers ◽  
Mark Krahn ◽  
Masood Parvez
Keyword(s):  
Nmr Spectroscopy ◽  
Structural Characterization ◽  
Zinc Phosphate ◽  
Membered Ring ◽  
Molar Ratio ◽  
Centrosymmetric Dimer ◽  
X Ray ◽  
Phosphate Anions ◽  
New Compounds

The reaction of OP(NH-t-Bu)3 with 1 equiv. of ZnMe2 generates the dimeric eight-membered ring {MeZn[(µ-NH-t-Bu)(µ-N-t-Bu)P(NH-t-Bu)(µ-O)]}2 (5) and the cubane {[MeZn]3[OP(N-t-Bu)3][OP(NH-t-Bu)3]} (6), which contains the first known trisimidophosphate trianion. A related complex {Zn[ZnMe]2[OP(N-t-Bu)(NH-t-Bu)2][OP(N-t-Bu)3]} (7) is obtained by the reaction of OP(NH-t-Bu)3 with ZnMe2 in a 2:3 molar ratio. The treatment of OP(NHMe)3 with 1 equiv. of ZnMe2 produces the oxide-templated cluster {Zn4(µ4-O)[OP(NMe)(NHMe)2]4[OP(NMe)2(NHMe)]}2 (8). Each half of this centrosymmetric dimer contains a tetrahedral arrangement of four 4-coordinate Zn2+ ions surrounding the central µ4-O2- anion. The reaction of SP(NH-t-Bu)3 with ZnMe2 in a 1:1 molar ratio generates the dimer {MeZn(µ-S)(µ-N-t-Bu)P(NH-t-Bu)2}2 (10), which has a ladder-type structure. When a 2:1 molar ratio of the same reagents is employed, the bis(N,S)-chelated complex {Zn[(µ-S)(µ-N-t-Bu)P(NH-t-Bu)2]2} (11) is obtained. The monomeric N,N′-chelated complex {MeZn[(µ-N-t-Bu)(µ-NSiMe3)P(NH-t-Bu)2]} (12) results from the reaction of Me3SiNP(NH-t-Bu)3 with 1 equiv. of dimethylzinc. All new compounds have been characterized by multinuclear (1H, 13C, and 31P) NMR spectroscopy and, in the case of 5, 6, 7, 8, and 10, by X-ray structural determinations.Key words: zinc, phosphate, imido ligands, sulfur.

scholarly journals Isolation and Characterization of Bacterium isolated from Bantala Tannery Solid Wastes

2019 ◽  
Vol 1 (1) ◽  
Author(s):  
Anannya Banerjee ◽  
Sudipta Tripathi
Keyword(s):  
Inhibitory Concentration ◽  
West Bengal ◽  
Accession Number ◽  
Bacterial Strains ◽  
X Ray ◽  
Isolation And Characterization ◽  
Chrome Tanning ◽  
Tanning Process ◽  
Mic Minimum Inhibitory Concentration

Leather industries that uses the conventional chrome tanning process are subjected to high risk of contamination due to the emission of toxic Cr(VI) that poses a serious threat to the environment and human’s wellbeing. The present study were made to isolate and characterize chromium tolerant bacteria in the samples collected from four different plots of Bantala Tannery, Kolkata, West Bengal, India. Pure chromium tolerant bacterial strains were isolated from the tannery sludge samples and their relative MIC (Minimum Inhibitory Concentration) were recorded at different concentrations of Cr (VI) salts to select the highest chromium tolerant bacterium. The selected bacterium was further taken for their growth studies followed by different cultural, morphological and molecular analysis (16S rDNA). The bacterial strain was further studied through SEM (Scanning Electron microscopy) and EDX (Energy Dispersive X-ray) spectroscopy which revealed that TW4 was a gram positive, rod shaped, endospore forming, pleomorphic bacterium with phylogenetic similarities with Isoptericola sp. and genebank accession number SUB1732465 TW4 KX640927.

scholarly journals Biosynthesis and Characterization of Extracellular Silver Nanoparticles from Streptomyces aizuneusis: Antimicrobial, Anti Larval, and Anticancer Activities

Molecules ◽  
2021 ◽  
Vol 27 (1) ◽  
pp. 212
Author(s):  
Hemmat M. Abd-Elhady ◽  
Mona A. Ashor ◽  
Abdelkader Hazem ◽  
Fayez M. Saleh ◽  
Samy Selim ◽  
...  
Keyword(s):  
Silver Nanoparticles ◽  
Human Lung ◽  
Spherical Shape ◽  
Antimicrobial Activities ◽  
Anticancer Activities ◽  
X Ray ◽  
Transmission Electron ◽  
Vis Spectroscopy ◽  
Human Lung Carcinoma

The ability of microorganisms to reduce inorganic metals has launched an exciting eco-friendly approach towards developing green nanotechnology. Thus, the synthesis of metal nanoparticles through a biological approach is an important aspect of current nanotechnology. In this study, Streptomyces aizuneusis ATCC 14921 gave the small particle of silver nanoparticles (AgNPs) a size of 38.45 nm, with 1.342 optical density. AgNPs produced by Streptomyces aizuneusis were characterized by means of UV-VIS spectroscopy and transmission electron microscopy (TEM). The UV-Vis spectrum of the aqueous solution containing silver ion showed a peak between 410 to 430. Moreover, the majority of nanoparticles were found to be a spherical shape with variables between 11 to 42 nm, as seen under TEM. The purity of extracted AgNPs was investigated by energy dispersive X-ray analysis (EDXA), and the identification of the possible biomolecules responsible for the reduction of Ag+ ions by the cell filtrate was carried out by Fourier Transform Infrared spectrum (FTIR). High antimicrobial activities were observed by AgNPs at a low concentration of 0.01 ppm, however, no deleterious effect of AgNPs was observed on the development and occurrence of Drosophila melanogaster phenotype. The highest reduction in the viability of the human lung carcinoma and normal cells was attained at 0.2 AgNPs ppm.

scholarly journals Design, Synthesis and Characterization of Some Novel benzamide derivatives and it's Pharmacological Screening

2020 ◽  
pp. 68-74 ◽  
Author(s):  
Akshay R. Yadav ◽  
Shrinivas K. Mohite
Keyword(s):  
Chemical Structure ◽  
Design Synthesis ◽  
Different Types ◽  
Anti Inflammatory ◽  
Benzoyl Isothiocyanate ◽  
Pharmacological Screening ◽  
Benzamide Derivatives

The new series of substituted N-(phenylcarbamothioyl)benzamide derivatives (2a-2f) was designed, development and synthesized by using conventional and microwave method. In present work 6 different N-(phenylcarbamothioyl)benzamide were synthesized. Substituted benzoyl chloride is converted into benzoyl isothiocyanate by esterification. Benzoyl isothiocyanate is converted into Substituted (phenylcarbamothioyl)benzamide by treating with different types of substituted aniline. Confirmation of the chemical structure of the synthesized was substantiated by TLC, IR, 1H NMR, MS spectroscopy.Novel synthesized compounds screened for their in vivo and in-vitro anti-inflammatory studies and compound 2f shows promising anti-inflammatory activity.

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