piperidines and diphenyl

Ion-induced change in fluorescence is a straight-forward method for detection of toxic metal ions showing immediate response. Cadmium ions are toxic to the environment. We report in this paper a piperidine-4-one-based fluorescent chemosensor of Cd

Topics: Biphenyl Compounds; Cadmium; Fluorescent Dyes; Molecular Structure; Particle Size; Piperidines; Surface Properties

A conventional and microwave assisted efficient synthesis of diphenyl substituted pyrazole using PEG 600 as green solvent has been described. A relatively shorter reaction time with excellent yield of the piperidine mediated protocol has been attracted economically attractive and eco-friendly. All newly synthesized compounds were characterized by standard spectroscopic techniques viz., UV-visible, FT-IR, (1)H-NMR and Mass spectra. The anti-microbial activities of compounds have also been tested using Minimum Inhibitory Concentration (MIC) method with two different microorganisms Staphylococcus aureus (MTCC3381) and Escherichia coli (MTCC739). The results of the antimicrobial activity revealed that the diphenyl substituted pyrazole derivatives have nice inhibiting nature against both types of bacteria of present investigation than corresponding chalcones. Since, the work has been focused on green chemical approach towards the synthesis, this protocol may be recommended for eco-friendly applications.

Topics: Anti-Bacterial Agents; Biphenyl Compounds; Chalcones; Escherichia coli; Magnetic Resonance Spectroscopy; Microbial Sensitivity Tests; Microwaves; Piperidines; Polyethylene Glycols; Pyrazoles; Solvents; Spectroscopy, Fourier Transform Infrared; Staphylococcus aureus

Antagonists of the CB1 receptor can be useful in the treatment of several important disorders. However, to date, the only clinically approved CB1 receptor antagonist, rimonabant, was withdrawn because of adverse central nervous system (CNS)-related side effects. Since rimonabant's withdrawal, several groups are pursuing peripherally selective CB1 antagonists. These compounds are expected to be devoid of undesirable CNS-related effects but maintain efficacy through antagonism of peripherally expressed CB1 receptors. Reported here are our latest results toward the development of a peripherally selective analog of the diphenyl purine CB1 antagonist otenabant 1. Compound 9 (N-{1-[8-(2-chlorophenyl)-9-(4-chlorophenyl)-9H-purin-6-yl]piperidin-4-yl}pentanamide) is a potent, orally absorbed antagonist of the CB1 receptor that is >50-fold selective for CB1 over CB2, highly selective for the periphery in a rodent model, and without efficacy in a series of in vivo assays designed to evaluate its ability to mitigate the central effects of Δ(9)-tetrahydrocannabinol through the CB1 receptor.

Topics: Animals; Area Under Curve; Binding, Competitive; Biphenyl Compounds; Body Temperature; Male; Mice; Mice, Inbred ICR; Molecular Structure; Motor Activity; Piperidines; Purines; Rats; Rats, Sprague-Dawley; Receptor, Cannabinoid, CB1; Receptor, Cannabinoid, CB2

Vestipitant (1) is a novel NK1 antagonist currently under investigation for the treatment of CNS disorders and emesis. The first synthetic step comprised a Grignard synthesis. An impurity was identified and initially expected to be a symmetric biphenyl. This paper reports the work to synthesise the supposed structure and the spectroscopic analyses (LC-NMR and HR-NMR) to correctly identify the real structure and understand the chemical pathway of the impurity.

Topics: Biphenyl Compounds; Chromatography, High Pressure Liquid; Drug Contamination; Fluorobenzenes; Magnetic Resonance Spectroscopy; Neurokinin-1 Receptor Antagonists; Piperidines

Topics: Antineoplastic Agents; Biphenyl Compounds; Chemistry, Pharmaceutical; Pharmacy; Piperidines; Research

Topics: Acetylcholine; Anesthesia, Local; Anesthetics, Local; Biphenyl Compounds; Blood Pressure; Epinephrine; Intestine, Small; Intestines; Ketones; Lidocaine; Mice; Muscle, Smooth; Pharmacology; Piperidines; Rabbits; Rats; Research; Respiration; Toxicology; Vasomotor System

Topics: Amphetamine; Amphetamines; Biphenyl Compounds; Chemical Phenomena; Chemistry; Dioxolanes; Heterocyclic Compounds; Hexobarbital; Hot Temperature; Hyperesthesia; Mice; Morphine; Pharmacology; Piperidines; Quinones; Reaction Time; Research; Reserpine; Sleep

Topics: Antipyretics; Biphenyl Compounds; Body Temperature; Lysergic Acid Diethylamide; Methanol; Piperidines; Salts

Topics: Analgesics; Analgesics, Non-Narcotic; Antipyretics; Biphenyl Compounds; Piperidines

Topics: Anti-Allergic Agents; Autonomic Agents; Biphenyl Compounds; Histamine H1 Antagonists; Humans; Phenothiazines; Piperidines; Psychotic Disorders; Syndrome

Topics: Analgesics; Biphenyl Compounds; Humans; Meperidine; Methadone; Parasympatholytics; Piperidines