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2.
RSC Adv ; 12(2): 698-707, 2021 Dec 22.
Article in English | MEDLINE | ID: mdl-35425141

ABSTRACT

Cobalt doped magnetite nanoparticles (Co x Fe3-x O4 NPs) are investigated extensively because of their potential hyperthermia application. However, the complex interrelation among chemical compositions and particle size means their correlation with the magnetic and heating properties is not trivial to predict. Here, we prepared Co x Fe3-x O4 NPs (0 ≤ x ≤ 1) to investigate the effects of cobalt content and particle size on their magnetic and heating properties. A detailed analysis of the structural features indicated the similarity between the crystallite and particle sizes as well as their non-monotonic change with the increase of Co content. Magnetic measurements for the Co x Fe3-x O4 NPs (0 ≤ x ≤ 1) showed that the blocking temperature, the saturation magnetization, the coercivity, and the anisotropy constant followed a similar trend with a maximum at x = 0.7. Moreover, 57Fe Mössbauer spectroscopy adequately explained the magnetic behaviour, the anisotropy constant, and saturation magnetization of low Co content samples. Finally, our study shows that the relaxation loss is a primary contributor to the SAR in Co x Fe3-x O4 NPs with low Co contents as well as their potential application in magnetic hyperthermia.

3.
J Med Chem ; 35(19): 3474-82, 1992 Sep 18.
Article in English | MEDLINE | ID: mdl-1404229

ABSTRACT

(-)-trans-(2S,5S)-2-[3-[(2-Oxopropyl)sulfonyl]-4-n-propoxy-5-(3- hydroxypropoxy)phenyl]-5-(3,4,5-trimethoxyphenyl)tetrahydrofuran (10) is one of the most potent platelet-activating factor (PAF) antagonists in vitro and in vivo developed to date. This diaryltetrahydrofuran derivative evolved from modifications of MK 0287 which has been evaluated in clinical studies for asthma. Two structural modifications of MK 0287 were made: (1) elaboration of the 3'-[(hydroxyethyl)sulfonyl] group to a beta-keto propylsulfonyl, and (2) replacement of the 5'-methyl ether by a 3-hydroxypropyl ether. Compound 10 potently and specifically inhibits the binding of [3H]-C18-PAF to human platelet membranes (Ki 1.85 nM) and PMN membranes (Ki 2.89 nM). In vivo, 10 inhibits PAF-induced plasma extravasation and elevated N-acetyl-beta-D-glucosaminidase (NAGA) levels in male rats with ED50 values of 60 micrograms/kg, po and 4 micrograms/kg, iv respectively, and inhibits PAF-induced bronchoconstriction in guinea pigs with an ED50 value of 15 micrograms/kg after intraduodenal administration. Compound 15, a water-soluble phosphate ester prodrug derivative of 10 is at least equipotent to 10 in the in vivo models. Compound 19S, the primary and major metabolite of 10 and 15, is equipotent in in vitro and in vivo models.


Subject(s)
Furans/chemical synthesis , Platelet Activating Factor/antagonists & inhibitors , Prodrugs/chemical synthesis , Sulfones/chemical synthesis , Administration, Oral , Animals , Furans/chemistry , Furans/pharmacology , Guinea Pigs , Humans , Male , Platelet Aggregation Inhibitors/pharmacology , Prodrugs/chemistry , Prodrugs/pharmacology , Rats , Solubility , Stereoisomerism , Structure-Activity Relationship , Sulfones/chemistry , Sulfones/pharmacology
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