Protein - ligand interactions play pivotal role in almost all the biological processes occurring in living organisms, and therefore such studies hold immense importance from the standpoint of rational drug design and development. In this study the binding of the topoisomerase I inhibitor drug, t...

Topotecan is a relatively large, planar, asymmetric and polar molecule with a lactone moiety. In neutral or basic aqueous solutions, this ring opens forming the carboxylate form of Topotecan that is biologically inactive and uncapable of passively cross membranes. Nevertheless, despite this inab...

Trifluoromethoxy radical formation (by O-atom addition to trifluoromethyl) and dissociation (by F-atom elimination) are studied by ab initio molecular-orbital theory. The activation enthalpy (298 K) for F-atom elimination is 35.3 kcal mol−1 at the UMP4SDQ/6-31 G∗//UHF/6-31 G∗+ΔZPE+Δ(H-E0 level...

5-Trifluoromethoxy-1H-indole-2,3-dione 3-(N-ethyl/benzylthiosemicarbazone) (2a/2b) and 5-trifluoromethoxy-1-morpholinomethyl-1H-indole-2,3-dione 3-(N-ethylthiosemicarbazone) (3a) were synthesized. The structures of the compounds were confirmed by elemental analysis, spectral data and X-ray singl...

New series of 5-methyl/trifluoromethoxy-1H-indole-2,3-dione 3-thiosemicarbazones 3a-t, 1-methyl-5-methyl/trifluoromethoxy-1H-indole-2,3-dione 3-thiosemicarbazones 4a-y and 5-trifluoromethoxy-1-morpholinomethyl-1H-indole-2,3-dione 3-thiosemicarbazones 5a-m were synthesized. The structures of the ...

Carbonyl cyanide p-(trifluoromethoxy) phenylhydrazone (FCCP) is an uncoupler of mitochondrial oxidative phosphorylation in eukaryotic cells. Here, we evaluated the in vitro effects of FCCP on the growth of Calu-6 lung cancer cells. FCCP inhibited the growth of Calu-6 cells with an IC50 of approx...

We describe here a study devoted to the comparison of the relative influence of chlorine, fluorine, and trifluoromethoxy substituents on the regiochemical outcome of the Diels–Alder reaction. For this purpose, we examined the behavior of mixed ‘halogenated’ quinones bearing these groups in th...

A series of binary metal complexes [M(L1)2] and [M(L2)2], (where M = Cu(II), Co(II), Ni(II)) of Schiff bases, HL1 = 2-((E)-(4-(trifluoromethoxy)phenylimino)methyl)-4-methylphenol, HL2 = 2-((E)-(4-(trifluoromethoxy)phenylimino)methyl)-5-methoxyphenol, were synthesized and characterized by differe...

An expeditious and concise synthesis of 3-(difluoromethoxy)-5,6,7,8-tetrahydro-1,6-naphthyridine and 3-(trifluoromethoxy)-5,6,7,8-tetrahydro-1,6-naphthyridines is described. Starting from N-benzyl piperidone, the key intermediates leading to these two biologically desirable synthones were rapidl...

Four novel Schiff base ligands, L1 (1-((E)-(6-(trifluoromethoxy)benzo[d]thiazol-2-ylimino)methyl)naphthalen-2-ol, C19H11F3N2O2S), L2 (3-((E)-(6-(trifluoromethoxy)benzo[d]thiazol-2-ylimino)methyl)benzene-1,2-diol, C15H9F3N2O3S), L3 (2-((E)-(6-(trifluoromethoxy)benzo[d]thiazol-2-ylimino)methyl)-5-...

Fluorinated substances play a significant role for many industrial and consumer products, but many of these chemicals are attributed with an adverse ecological profile and persistence in the environment. Herein, three potentially more environmentally benign substitutes were assessed for aerobic ...

The synthesis of new nucleoside derivatives from 6- and 7-trifluoromethoxy-4-quinolones is described. The present synthesis is a combination of the Gould–Jacobs reaction for the preparation of 4-quinolones and a modified Vorbrüggen reaction for the construction of nucleoside derivatives. The t...

Background and objectivesPediatric patients frequently require deep sedation or general anesthesia for colonoscopy. This study was designed to compare the sedative efficacy of remifentanil–ketamine combination with propofol–ketamine combination in children undergoing colonoscopy.

Background and objectiveSome surgical procedures such as laryngoplasty require patients to remain conscious during the intraoperative phase in order to enable speech monitoring. Dexmedetomidine and remifentanil were used in this study, since they promote appropriate patient collaboration with fa...

Remifentanil based anesthesia is nowadays spread worldwide. This drug is characterized by a rapid onset of the analgesic effects, but also by a rapid onset of the side effects. For this reason, the knowledge of the remifentanil concentration in the human body is a key topic in anesthesiology. Th...

AimLipopolysaccharide (LPS)-induced myocardial injury is a leading cause of death in patients with sepsis, which is associated with excessive activation of PKCβ (especially PKCβ2) and autophagy. Remifentanil, a μ-opioid receptor agonist, is well demonstrated to have beneficial effects during ...

BackgroundAdding the μ-opioid receptor agonist remifentanil to agents used to induce general anaesthesia in electroconvulsive therapy (ECT) can reduce the required doses of induction agents and their unfavourable effects on seizure threshold and quality. However, whether remifentanil has favour...

Chemokines related neuroinflammation and N-methyl-d-aspartate receptor (NMDAR) mediated nociceptive transmission are pivotal determinants in the pathogenesis of opioid-induced hyperalgesia (OIH), but little is known about specific mechanism and treatment. Chemokine CXCL12 with its receptor CXCR4...

A closed-loop control system for the control of the depth of hypnosis in anesthesia by using propofol-remifentanil coadministration and the Bispectral Index as feedback signal is proposed. A PID controller is employed together with a fixed ratio between propofol and remifentanil infusions. The r...

BackgroundIntravenous remifentanil patient-controlled analgesia (PCA) has been routinely available for labouring women in our unit since 2004, the regimen using a 40 µg bolus available two minutely on demand, continuous pulse oximetry and mandatory one-to-one care. We examined remifentanil use ...