Synthesis and structure elucidation of allyl Pd(II) complexes of NHC ligands derived from substituted imidazo1,5-aquinolin-1(2H)-ylidene
Publication date: 15 November 2017 Source:Journal of Organometallic Chemistry, Volume 851 Author(s): Rumen Lyapchev, Petar Petrov, Miroslav Dangalov, Nikolay G. Vassilev Nine Pd(II) complexes involving N-heterocyclic carbenes (NHCs) derived from 2-substituted and 2- and 7-substituted imidazo[1,5-a]quinolin-1(2H)-ylidene with auxiliary allylic ligands were synthesized and characterized. The structure and configuration of the complexes were elucidated on the basis of combination of dynamic NMR and DFT studies. Conformational studies in respect of hindered rotation around Pd-C bond and η3-η1-η3 pseudo allyl rotation were performed. The results from dynamic NMR and DFT studies confirmed the mechanism of selective η3-η1-η3 isomerization, whose energy barriers are affected by steric hindrance of substituents at nitrogen atom. Energy barriers of isomerization (16.7–18.8 kcal/mol) are slightly influenced by the electronic nature of substituents at seventh position in imidazo[1,5-a]quinolin-1(2H)-ylidene moiety. The results from DFT calculations were in good agreement with the experimental energy barriers. Graphical abstract
Conclusions: Results reveals that developed nitrendipine nanoemulsion gel overcomes the limitation of low penetration and accentuate permeation through albino Wistar rat skin. It was concluded that nanoemulsion gel could be utilized as a potential carrier for transdermal delivery of nitrendipine. PMID: 31976777 [PubMed - as supplied by publisher]
Authors: Rezaie Shirmard L, Ghofrani M, Bahari Javan N, Bayrami S, Tavassoli A, Rezaie A, Amini M, Kebriaee-Zadeh A, Rouini MR, Dinarvand R, Rafiee-Tehrani M, Dorkoosh FA Abstract Uncontrolled distribution of nanoparticles (NPs) within the body can significantly decrease the efficiency of drug therapy and is considered among the main restrictions of NPs application. The aim of this study was to develop a depot combination delivery system (CDS) containing fingolimod loaded poly (3-hydroxybutyrate-co-3-hydroxyvalerate) (PHBV) NPs dispersed into a matrix of oleic acid-grafted-aminated alginate (OA-g-AAlg) to minimize ...
Authors: Yoshida T, Sako K, Kondo H Abstract High consumption of oil formulations has been reported to reduce the blood exposure of drugs like tacrolimus. Consumption of oil formulations has also been shown to inhibit T-cell production of interleukin-2 (IL-2) compared to solid dispersion formulations (SDFs). However, a large amount of oil causes gastrointestinal side effects such as diarrhea and low compliance. Here, we investigated the feasibility of reducing the amount of oil and substitution of chemically synthetized oils for natural oils in these formulations. Reducing the amount of sunflower oil increased bloo...
CONCLUSIONS: In conclusion, the potential for supersaturation in LBDDS, and the risk of precipitation, was found to be highly drug dependent. The apparent degree of supersaturation was considered a major factor impacting the ability to maintain drug supersaturation upon storage. PMID: 31975613 [PubMed - as supplied by publisher]
Authors: Mailhot Vega RB, Hoppe BS PMID: 31976780 [PubMed - as supplied by publisher]
With a second case of a deadly Chinese virus confirmed in the United States, and four cases under investigation in New York, Buffalo-area hospitals are on alert and preparing as best as they can. The novel coronavirus was first identified in Wuhan, China, in December. More than 850 cases have since been reported worldwide, with more than 40 deaths in China. Transportation has been shutdown with travel restricted for millions in that country as international officials work to contain the di sease. In…