SIB-1553A ((±)-4-[2-(1-methyl-2-pyrrolidinyl)ethyl]thio]phenol HCl) is a neuronal nicotinic acetylcholine receptor (nAChR) ligand which displaced the binding of [3H]nicotine (NIC) to the rat brain nAChRs with an IC50 value of 110 nM with no appreciable affinity to the α7 nAhRs. SIB-1553A showe...
A synthesis of (±)-(E)-3-(4-hydroxyphenyl)-N-[4-(3-methyl-2,5-dioxo-1-pyrrolidinyl)butyl]-2-propenamide (7) is described. This phenolic amide was prepared in six steps with an overall yield of 46%.
A novel series of 4-pyridylpiperazine derivatives with varying alkyl linker length and eastern part substituents proved to be potent histamine H3 receptor (hH3R) ligands in the nanomolar concentration range. While paying attention to their alkyl linker length, derivatives with a six methylene li...
A novel two-dimensional network bimetallic Fe Au spin crossover coordination polymer based on 3-phenylpyridine-coordinated iron centers and linear gold cyanide bridges {Fe(3-phenylpyridine)2[Au(CN)2]2}n (1), has been synthesized. The compound is characterized by elemental analysis, IR, single-cr...
In this study the experimental and theoretical vibrational frequencies of a newly synthesized anti-tumor, antiviral, hypoglycemic, antifungal and anti-HIV agent namely, 5-Methyl-3-phenylisoxazole-4-carboxylic acid has been investigated. The experimental FT-IR (4000–400 cm−1) and Laser-Raman spe...
The oxadiazole pharmacophore is considered a viable lead structure for the synthesis of more efficacious and broad spectrum antimicrobial agents. The significance of this study was to prepare various oxadiazole derivatives by introducing the 1,3,4 oxadiazole core into several molecules to explor...
The structural, electronic, and spectroscopic properties of 4-methyl-5-((5-phenyl-1,3,4 oxadiazol-2-yl)thio)benzene-1,2-diol (MPOTB) have been carried out at ab initio and DFT levels. A detailed study of geometrical parameters, Infrared spectrum, chemical shifts (13C NMR, 1H NMR), and electronic...
Using 2,4,5-trifluorophenylpyridine as a monoanionic cyclometalated ligand, 2-(5-phenyl-1,3,4-oxadiazol-2-yl)phenol, 2-(5-(4-fluorophenyl)-1,3,4-oxadiazol-2-yl)phenol and 2-(5-(4-trifluoro-methylphenyl)-1,3,4-oxadiazol-2-yl)phenol as ancillary ligands, three new heteroleptic iridium(III) complex...
The red seaweed, Gelidium amansii, contains proteins such as R-phycoerythrin and R-phycocyanin, as well as polysaccharides. Initial protein extraction from G. amansii yielded 53 μg/g R-phycoerythrin and 56 μg/g R-phycocyanin. After protein extraction, monosaccharides were produced using hyper ...
The objective of this study was to develop straightforward processes that could be applied to the large-scale production of β-cryptoxanthin in an attempt to facilitate investigation of its biological activity. An oleoresin obtained from crude extracts of marigold flowers (Tagetes erecta) with a...
(R)-2-(4-hydroxyphenoxy)propionic acid ((R)-HPOPA) is an important intermediate for the synthesis of optically pure aryloxyphenoxypropionic acid herbicides. Regioselective hydroxylation of (R)-2-phenoxypropionic acid ((R)-POPA) by microbes is one of the most useful methods for the industrial pro...
Trifluoromethyl ether and difluoro(methylthio)methyl ether of phenols and aliphatic alcohols were selectively synthesized from the corresponding dithiocarbonates. When IF5-pyridine-HF was used alone in the reaction of the dithiocarbonate, the difluoro(methylthio)methyl ether was selectively form...
Experimental and theoretical studies on the thermodynamics and properties of 2-substituted 6(4)-methyl-1,4(1,6)-dihydropyrimidine-5-carboxylates were undertaken by 1H NMR measurements and DFT (density functional theory) calculations. The ratios of tautomers a/b of dihydropyrimidines (DPs) 1, 2, ...
Three new coordination polymers (CPs), [Ag(MTP)2(PF6)]n 1, [Ag(MTP)(NO3)]n 2 and [Ag(MTP)(OTf)]n 3 (where MTP = 2-(Methylthio)Pyrazine and OTf = CF3SO3−) have been synthesized and characterized by different spectroscopic techniques. The single crystal X-ray study reveals that CPs 1 and 2 are two...
Until recently, (methylthio)phenols as natural products had only been reported from bacteria. Now, four representatives of this class of sulfurous aromatic compounds have been discovered as semiochemicals in the orchid Caladenia crebra, which secures pollination by sexual deception. In this case...
A new 2-[(bis(2-pyridylmethyl)amino)methyl]-4-methyl-6-(methylthio)phenol copperII perchlorate, complex, [Cu2(μ-SL)2](ClO4)2 (1), was synthesized and magnetically and structurally characterized. The complex consists of two similar but not equivalent [Cu2(μ-SL)2]2+ bimetallic cations designed a...
SummaryGenetic defects on 6-pyruvoyl-tetrahydropterin synthase (PTPS) are the most prevalent cause of hyperphenylalaninaemia not due to phenylalanine hydrolyase deficiency (phenylketonuria). PTPS catalyses the second step of tetrahydrobiopterin (BH4) cofactor biosynthesis, and its deficiency rep...
1,2-Disubstituted cyclopropene, 1-methyl-2-phenylcyclopropene (18), was generated by bromo-lithium exchange of 1-bromo-2-phenylcyclopropene followed by treatment with methyl iodide. Compound 18 was oxidized by oxygen to give the α,β-unsaturated carbonyl product 25 and diketone 27 and the tauto...
TMSOTf-mediated reactions of 2-aryl-1-(1-phenylcyclopropyl)ethanones 1 with diethyl 2-oxomalonate 2 afford a novel method for the synthesis of spiro-γ-lactone derivatives 3 in good to excellent yields via a sequential reaction involving a nucleophilic ring-opening reaction of the cyclopropane b...
Three ZnII complexes containing bispicam ligands (bispicam = bis(2-pyridylmethyl)amine), [Zn(bispicam)2](NO3)2·2CH3OH 4A, [Zn(bispicam)(NO3)2] 4B, and [Zn(bispicam)2](OTf)2 6, were obtained, and their structures were determined by X-ray crystallography. Complexes of the general formulation [Zn(...
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