The structures of 5-(4-chlorophenyl)-1-{4-(methylsulfonyl)phenyl}-1H-tetrazole (3) and 4-{5-(4-methoxyphenyl)-1H-tetrazol-1-yl}benzenesulfonamide (5) have been determined by X-ray crystallography. Tetrazoles 3 and 5 crystallize in the monoclinic space groups Ia and P21/c, respectively. The cell ...
Heterocyclic compounds are the most attractive class for researchers due to their biological activities. In the undertaken research, a number of N-(5-chloro-2-methoxyphenyl)-4-(5-substituted-1,3,4-oxadiazol-2-ylthio)butanamide (6a–k) compounds were prepared by converting multifarious phenyl/ary...
Metallo-phthalocyanines substituted with four pentafluorobenzyloxy units through benzyloxy-bridges were synthesized from a new phthalonitrile derivative and characterized by spectroscopic methods. The aggregation behaviour of these compounds were investigated in different concentrations of tetra...
The useful synthons sugar enones (2-benzyloxypyran-3-ones) derived from pentoses have been prepared starting from 2-acetoxyglycals or benzyl pentopyranosides. The glycals were glycosylated with benzyl alcohol in the presence of a Lewis acid (SnCl4 or InCl3) to give enantioenriched enones (ee = 8...
In the present study we investigated the ability of the arachidonic acid metabolites, prostaglandin H2 and thromboxane A2, to release Ca2+ from isolated platelet vesicles. The vesicles were prepared through modification of previously described procedures. 45Ca uptake and release were determined ...
Because of its highly unstable nature, TXA2, produced by platelet metabolism of arachidonic acid, does not lend itself to use as a receptor probe for its own receptor. As such, the stable TXA2/PGH2 antagonist, trans-13-azaprostanoic acid (trans-13-APA, 12b), was prepared as the [17,18 3H] deriva...
Two novel oxime derivatives of naltrexone, 6-[2-phenylethyl]-oximino naltrexone (NPC 831) and 6-[3-phenylpropyl]-oximino naltrexone (NPC 836) were potent agonists at opioid receptors. Both compounds inhibited binding to all three opioid receptor subtypes with nanomolar affinities. In vivo, NPC 8...
A series of [5-substituted-4-phenyl-1,3-thiazol-2-yl] benzamide and furamide analogues were investigated in radioligand binding studies at adenosine receptor subtypes with an aim to obtain potent and selective adenosine receptor ligands. Benzamide and furamide linked to thiazole was found to be ...
Alcohols can be easily transformed to their corresponding methylthiomethyl ethers under mild conditions by treatment with methyl sulfide and benzoyl peroxide in acetonitrile.
A mild and efficient method for the synthesis of diverse isoindolinones from o-phthaldehydic acid methylthiomethyl ester and aliphatic/aromatic amines has been developed. A number of nucleophiles including a hydride ion were successfully added to the intermediate Schiff's base providing iso...
A series of mixed N-heterocycles/N-heterocyclic carbene palladium(II) allyl complexes with general formula [(NHC)Pd(η3-allyl)]2(μ2-N-heterocycles)(BF4)2 were prepared in one pot based on anion metathesis of (NHC)Pd(η3-allyl)Cl complexes and then ligand replacement with N-heterocycles [N-heter...
Two series of N-containing heterocycles were synthesized by one-step intramolecular or intermolecular annulations of N-substituted pyrrole-2-carbaldehydes and pyrrole-2-carbonitriles. These facile and atom-economic synthetic routes involved the inherent three potential electrophilic and nucleoph...
We have developed an efficient one-pot method for the microwave-assisted synthesis of ureas and carbamates via a proposed Lossen rearrangement. Herein we report the first examples of the direct conversion of benzoyl chlorides into N,N′-disubstituted ureas and N-aryl carbamates using hydroxylami...
(4-Methoxyphenyl)(3,4,5-trimethoxyphenyl)methanone (PHT) is a known cytotoxic compound belonging to the phenstatin family. However, the exact mechanism of action of PHT-induced cell death remains to be determined. The aim of this study was to investigate the mechanisms underlying PHT-induced cyt...
Leishmaniasis is a group of diseases caused by protozoan parasites from the genus Leishmania. There are estimated 1.3 million new cases annually with a mortality of 20,000–30,000 per year, when patients are left untreated. Current chemotherapeutic drugs available present high toxicity and low e...
We present a theoretical study of the structure and electronic and optical properties of several L2–M compounds where L is bis(N-(5-(4-methoxyphenyl)-1,3,4-oxadiazol-2-yl)ethanimidamidato, or C11H11N4O2, and M = Co, Ni, Cu, Zn, Pd, Cd. Our calculations are carried out in the framework of the de...
Tetra-peripherally and non-peripherally 7-oxy-3-(m-methoxyphenyl)coumarin-substituted zinc(II) (4a and 5a), indium(III)acetate (4b and 5b) and magnesium(II) (4c and 5c) phthalocyanines were synthesized for the first time. These phthalocyanines were characterized by elemental analysis, FT-IR, 1H ...
Deficient osseointegration and implant-related infections are pivotal issues for the long-term clinical success of titanium (Ti) implants. Zinc (Zn) and strontium (Sr) serve dual functions by promoting osteogenesis and inhibiting bone destruction, and Zn has good antibacterial activity. As such,...
Current methods for the decontamination of radioactively contaminated surfaces in nuclear facilities typically rely on the use of liquid agents to remove radionuclides. This generates large volumes of highly hazardous liquid waste which must then be treated in costly processes which often requir...
To meet the requirements of minimally invasive surgical treatments for osteoporotic vertebral compression fracture, various strategies have been proposed to enhance the properties of calcium phosphate cement (CPC). Here, a new strategy was developed by incorporating poly (γ-glutamic acid) (γ-P...
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