Carboxylic Acids

Odour detection thresholds, that we have previously obtained, have been analysed by a general equation for selective transport. It is shown that such selective transport can account for some 77% of the total effect. The remainder is due to a specific size effect, that might involve odour-binding proteins, and a specific effect for aldehydes and carboxylic acids. Our analysis raises

The activities of a number of side-chain analogues of delta-8-tetrahydrocannabinol (Δ8-THC) in rat cerebellar membrane preparations were tested.The affinities of each compound for the CB1 receptor were compared by their respective abilities to displace [3H]-SR141716A and their efficacies compared by stimulation of [35S]-GTPγS binding.It was found that the affinities varied from 0.19±0.03 nM for 3-norpentyl-3-[6′-cyano,1′,1′-dimethyl]hexyl-Δ8-THC to 395±66.3 nM for 5′-[N-(4-chlorophenyl)]-1′,1′-dimethyl-carboxamido-Δ8-THC.The efficacies of these compounds varied greatly, ranging from the very low efficacy exhibited to acetylenic compounds such as 1′-heptyn-Δ8-THC and 4′-octyn-Δ8-THC to higher efficacy compounds such as 5′-(4-cyanophenoxy)-1′,1′-dimethyl-Δ8-THC and 5′-[N-(4-aminosulphonylphenyl)]-1′,1′ dimethyl-carboxamido Δ8-THC. All agonist activities were antagonized by the CB1-selective antagonist SR141716A.It was found that a ligand's CB1 affinity and efficacy are differentially altered by modifications in the side-chain. Decreasing the flexibility of the side-chain reduced efficacy but largely did not alter affinity. Additionally, the positioning of electrostatic moieties, such as cyano groups, within the side-chain also has contrasting effects on these two properties.In summary, this report details the characterization of a number of novel Δ8-THC analogues in rat cerebellar membranes. It provides the first detailed pharmacological analysis of how the inclusion of electrostatic moieties in the side-chain and also how alteration of the side-chain's flexibility may differentially affect a CB1 cannabinoid receptor ligand's affinity and efficacy.The activities of a number of side-chain analogues of delta-8-tetrahydrocannabinol (Δ8-THC) in rat cerebellar membrane preparations were tested.The affinities of each compound for the CB1 receptor were compared by their respective abilities to displace [3H]-SR141716A and their efficacies compared by stimulation of [35S]-GTPγS binding.It was found that the affinities varied from 0.19±0.03 nM for 3-norpentyl-3-[6′-cyano,1′,1′-dimethyl]hexyl-Δ8-THC to 395±66.3 nM for 5′-[N-(4-chlorophenyl)]-1′,1′-dimethyl-carboxamido-Δ8-THC.The efficacies of these compounds varied greatly, ranging from the very low efficacy exhibited to acetylenic compounds such as 1′-heptyn-Δ8-THC and 4′-octyn-Δ8-THC to higher efficacy compounds such as 5′-(4-cyanophenoxy)-1′,1′-dimethyl-Δ8-THC and 5′-[N-(4-aminosulphonylphenyl)]-1′,1′ dimethyl-carboxamido Δ8-THC. All agonist activities were antagonized by the CB1-selective antagonist SR141716A.It was found that a ligand's CB1 affinity and efficacy are differentially altered by modifications in the side-chain. Decreasing the flexibility of the side-chain reduced efficacy but largely did not alter affinity. Additionally, the positioning of electrostatic moieties, such as cyano groups, within the side-chain also has contrasting effects on these two properties.In summary, this report details the characterization of a number of novel Δ8-THC analogues in rat cerebellar membranes. It provides the first detailed pharmacological analysis of how the inclusion of electrostatic moieties in the side-chain and also how alteration of the side-chain's flexibility may differentially affect a CB1 cannabinoid receptor ligand's affinity and efficacy.British Journal of Pharmacology (2001) 132, 525–535; doi:10.1038/sj.bjp.0703827

In the development of new antibacterial therapeutic approaches to fight multidrug-resistant bacteria, antimicrobial photodynamic therapy (aPDT) represents a well-known alternative to treat local infections caused by different microorganisms. Here we present a polypropylene (PP) fabric finished with citrate-hydroxypropyl-βCD polymer (PP-CD) entrapping the tetra-anionic 5,10,15,20-tetrakis(4-sulfonatophenyl)-21H,23H-porphine (TPPS) as photosensitizer eluting scaffold (PP-CD/TPPS) for aPDT. The concept is based on host-guest complexation of porphyrin in the cavities of CDs immobilized on the PP fibers, followed by its sustained and controlled delivery in release medium and simultaneous photo-inactivation of microorganisms. Morphology of fabric was characterized by optical (OM) and scanning electron microscopies (SEM). Optical properties were investigated by UV-vis absorption, steady- and time-resolved fluorescence emission spectroscopy. X-ray Photoelectron Spectroscopy (XPS) and FT-IR ...

Alkaline wet oxidation pre-treatment (water, sodium carbonate, oxygen, high temperature and pressure) of wheat straw was performed as a 24−1 fractional factorial design with the process parameters: temperature, reaction time, sodium carbonate and oxygen. Alkaline wet oxidation was an efficient pre-treatment of wheat straw that resulted in solid fractions with high cellulose recovery (96%) and high enzymatic convertibility to glucose

We quantify global emissions of C4-C14 perfluoroalkyl carboxylic acid (PFCA) homologues during the life-cycle of products based on perfluorooctanoic acid (PFOA), perfluorononanoic acid (PFNA), perfluorooctane sulfonyl fluoride (POSF), and fluorotelomer compounds. We estimate emissions of 2610-21400 tonnes of C4-C14 PFCAs in the period from 1951 to 2015, and project 20-6420 tonnes to be emitted from 2016 to 2030. The global annual emissions steadily increased in the period 1951-2002, followed by a decrease and then another increase in the period 2002-2012. Releases from fluoropolymer production contributed most to historical PFCA emissions (e.g. 55-83% in 1951-2002). Since 2002, there has been a geographical shift of industrial sources (particularly fluoropolymer production sites) from North America, Europe and Japan to emerging Asian economies, especially China. Sources differ between PFCA homologues, sometimes considerably, and the relative contributions of each source change over ...

This work describes recent results from our research program aiming at the synthesis and evaluation of new compounds acting as potential anti-inflammatory drugs. A series of novel acyl-hydrazones bearing 2-aryl-thiazole moiety were synthesized by the condensation between derivatives of 4-[2-(4-methyl-2-phenyl-thiazole-5-yl)-2-oxo-ethoxy]-benzaldehyde and 2, 3 or 4-(2-aryl-thiazol-4-ylmethoxy)-benzaldehyde, respectively and different carboxylic acid hydrazides. The structures of newly synthesized compounds were established by the combined use of IR, (1)H NMR, mass spectral data and elemental analysis. These compounds were tested in vivo for their anti-inflammatory activity, in an acute experimental inflammation. The acute phase bone marrow response, phagocytes' activity and NO synthesis were evaluated. Compounds 10, 15, 17, 18 and 22 reduced the absolute leukocytes count due to the lower neutrophils percentage. Phagocitary index was decreased by all the compounds. Seven of them r...

The present study report the synthesis of the Zn(II) complex with Isonicotinic acid hydrazide and 2-acetylnaphthalene and their characterization using FTIR and Magnetic susceptibility studies. Our studies reveal the presence of different mode of linkages of the ligand with Zn(II). The IR spectra of the ligand imply that the ligand is bidentate with the amide group and azomethine –nitrogen as the two coordination sites was compared. The Zn(II) complex exhibit an identical pattern suggesting them to be isostructural with six coordinated spin free octahedral complex. The complex have been screened for their biological activity against the multidrug resistant bacterial and fungal pathogens. The results of this study show that the Zn (II) complex was effective against fungus than the bacteria.

Penetrating microscale microelectrodes made from flexible polymers tend to bend or deflect and may fail to reach their target location. The development of flexible neural probes requires methods for reliable and controlled insertion into the brain. Previous approaches for implanting flexible probes into the cortex required modifications that negate the flexibility, limit the functionality, or restrict the design of the probe. This study investigated the use of an electronegative self-assembled monolayer (SAM) as a coating on a stiff insertion shuttle to carry a polymer probe into the cerebral cortex, and then the detachment of the shuttle from the probe by altering the shuttle's hydrophobicity.

Polydimethylsiloxane (PDMS) and polyimide probes were inserted into an agarose in vitro brain model using silicon insertion shuttles. The silicon shuttles were coated with a carboxyl terminal SAM. The precision of insertion using the shuttle was measured by the percentage displacement of the probe upon shuttle removal after the probe was fully inserted. The average relative displacement of polyimide probes inserted with SAM-coated shuttles was (1.0 ± 0.66)% of the total insertion depth compared to (26.5 ± 3.7)% for uncoated silicon shuttles. The average relative displacement of PDMS probes was (2.1 ± 1.1)% of the insertion depth compared to 100% (complete removal) for uncoated silicon shuttles. SAM-coated shuttles were further validated through their use to reliably insert PDMS probes in the cerebral cortex of rodents. This study found that SAM-coated silicon shuttles are a viable method for accurately and precisely inserting flexible neural probes in the brain.