The acute oral toxicity of 3,7-bis-(4-trifluoromethylphenyl)-1,5,3,7-dioxadiazocane (4-TFMPD) was compared with its 3-substituted isomer, 3,7-bis-(3-trifluoromethylphenyl)-1,5,3,7-dioxadiazocane (3-TFMPD) and with N,N′-oxydimethylenebis (2-trifluoromethylaniline) (N,N'-oxy-DM-bis (2-TFMA))...

A novel fluorinated epoxy resin, 1,1-bis(4-glycidylesterphenyl)-1-(3′-trifluoromethylphenyl)-2,2,2-trifluoroethane (BGTF), was synthesized through a four-step procedure, which was then cured with hexahydro-4-methylphthalic anhydride (HMPA) and 4,4′-diaminodiphenyl-methane (DDM). As comparison,...

A novel pyridine-containing aromatic diamine monomer, 4-(4-trifluoromethylphenyl)-2,6-bis[4-(4-aminophenoxy)phenyl]pyridine (FAPP), was synthesized via the modified Chichibabin pyridine synthesis of 4-(4-nitrophenoxy)-acetophenone with 4-trifluoromethyl-benzaldehyde, followed by a catalytic redu...

The therapeutic targeting of nicotinic receptors requires the identification of drugs that selectively activate or inhibit a limited range of nicotine acetylcholine receptors (nAChRs). In this study, we identified N-(4-trifluoromethylphenyl)amide group of the synthetic histamine receptor ligands...

Pyrazine and its derivatives form an important class of compounds present in several natural flavors and complex organic molecules. Quantum chemical calculations of the equilibrium geometry, harmonic vibrational frequencies, infrared intensities and Raman activities of 5-tert-Butyl-N-(4-trifluor...

2-Pyrazolins 14a–l and pyrazoles 15a–l were designed as celecoxib analogs for the evaluation of their in vitro COX-1/COX-2 inhibitory activity and the in vivo anti-inflammatory activity. Compounds 14i, 15a, 15d and 15f were the most COX-2 selective derivatives (S.I. = 5.93, 6.08, 5.03 and 5.27...

A set of pyridine-2,6-dicarboxylic acids (dipicolinic acids, DPAD, Lx) were prepared to study the photo-physical properties of their ternary complexes with Eu(III) and ethylenediaminetetraacetic acid (EDTA or Y). The stability constant of the formation of EuY-L1 (L1= dipicolinic acid, measured l...

The aim was to study the pharmacokinetic equivalence of the local anaesthetic ropivacaine and its stable isotope analogue [2H3]-ropivacaine. Ropivacaine (40.0–53.0 mg) and [2H3]-ropivacaine (41.9–52.4 mg) were given simultaneously to eight healthy subjects as a single i.v. infusion. Blood and ...

The main objective of this study was to evaluate the potential of ropivacaine-loaded nanostructured lipid carriers (RPV-NLCs) as a transdermal delivery system. RPV-NLCs were prepared by the method of emulsion evaporation–solidification at low temperature. The average entrapment efficiency and d...

Following epidural administration, cerebrospinal fluid bioavailability of local anesthetics is low, one major limiting factor being diffusion across the arachnoid mater barrier. The aim of this study was to evaluate the influence of absorption enhancers on the meningeal permeability of epidurall...

The objective of this research was to develop novel ropivacaine-loaded lipid nanocapsules (RPV-LNCs) and evaluate the potential of RPV-LNCs as external preparation for transdermal delivery. RPV-LNCs were prepared by phase inversion technique and optimized by response surface design. The permeati...

The aim of the study was to develop a polyester visceral implant modified with a cyclodextrin polymer for the local and prolonged delivery of ropivacaine to reduce post operatory pain. Therefore, we applied a coating of an inguinal mesh with a crosslinked polymer of hydroxypropyl-β-cyclodextrin...

Background and objectives Bupivacaine is a first choice for regional anesthesia considering its effectiveness, long duration and less motor blockade. Bupivacaine (S75-R25) is a mixture of optical isomers containing 75% levobupivacaine (S-) and 25% dextrobupivacaine (R+) created by a Brazilian ph...

IntroductionMultidrug resistance of cancer cells constitutes a serious problem in chemotherapy and a challenging issue in the discovery of new cytotoxic drugs. Many saponins are known to display anti-cancer effects. In this study, the cytotoxicity and the modes of action of a naturally occuring ...

ObjectiveTo investigate the reproductive toxicity and cytotoxicity of T-2 toxin, which is a mycotoxin, and to explore its potential apoptotic induction mechanism.

This study examined the effect of climate change (CC) abiotic factors of temperature (20, 25, 30 °C), water activity (aw; 0.995, 0.98) and CO2 exposure (400, 1000 ppm) may have on (a) growth, (b) gene expression of biosynthetic toxin genes (Tri5, Tri6, Tri16), and (c) T-2/HT-2 toxins and associ...

T-2 toxin is the type-A trichothecene and a common contaminant of food and cereals, produced by Fusarium species. T-2 toxin easily penetrates skin due to its lipophilic nature and causes skin irritation and blisters in humans. Physical protection of the skin and airway is the only proven effecti...

ObjectiveTo investigate the reproductive toxicity and cytotoxicity of T-2 toxin, which is a mycotoxin, and to explore its potential apoptotic induction mechanism.

ObjectiveTo investigate the effect of T-2 toxin on murine embryonic stem cells (ESCs) cardiac differentiation and mitochondrial biogenesis in vitro.

T-2 toxin is one of the most toxic among several trichothecenes involved in both human and animal poisoning cases. We investigated the biochemical and histological alterations behind inflammation and cutaneous injury caused by T-2 toxin. Swiss albino mice were exposed to T-2 toxin topically at d...