Physiochemical properties

Solvent solubihty 4.31 g/L in n-hexane at 25 °C Miscible with acetone, ethanol, chloroform, toluene and xylene at 25 °C 

Stabihty Stable for light and air at room temperature, decompose under the acidic or basic conditions 

Long-term storage Keep in dark and dry place at low temperature ( 15 °C) 

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Table 4. In Vitro Conduction Blocking and Physiochemical Properties of Local Anesthetic Agents ...

The rate of removal of the local anesthetic from the site of injection also affects its profile. AH local anesthetic agents possess some vasodilatory activity at clinically useful concentrations. Agents which are more potent in this regard tend to be absorbed more rapidly by the vasculature. They are less potent anesthetics and have shorter durations than those having lower vasodilatory activity. A comparison of potency, onset, and duration as a function of physiochemical properties is presented in Table 4. 

In subsequent studies attempting to find a correlation of physicochemical properties and antimicrobial activity, other parameters have been employed, such as Hammett O values, electronic distribution calculated by molecular orbital methods, spectral characteristics, and hydrophobicity constants. No new insight on the role of physiochemical properties of the sulfonamides has resulted. Acid dissociation appears to play a predominant role, since it affects aqueous solubiUty, partition coefficient and transport across membranes, protein binding, tubular secretion, and reabsorption in the kidneys. An exhaustive discussion of these studies has been provided (10). 

The isoxazolecarboxylic acids are the most intensively investigated of the isoxazole derivatives, and a detailed compilation of their physiochemical properties has been made 62HC(17)l,p. 177). Similar studies have also been carried out with the 5-isoxazolones (62HC(17)l,p. 124), and pK values of 1,2-benzisoxazole derivatives are listed in Table 4. 

Table 1. Physiochemical properties of proteins of the contact activation cascade... 

Wenlock MC, Austin RP, Barton P, Davis AM, Leeson PD. A comparison of physiochemical property profiles of development and marketed oral drngs. I Med Chem 2003 4 1250-6. 

Distribution is an important aspect of a drug s pharmacokinetic profile. The structural and physiochemical properties of a drug determine the extent of... 

Barron, E.S.G., Ambrose, J. and Johnson, P. (1955). Studies on the mechanisms of action of ionising radiations XIII. The effect of X-irradiation on some physiochemical properties of proteins. Radiat. Res. 2, 145-152. 

Electrochemical study of biologically active compounds at the O/W interface provides information on physiochemical properties of the compounds at the O/W interface and in the O and W phases or, in short, hydrophobicity or lipophilicity of biologically active compounds, which seems essential to understand their biological effects, including mode of action, structure-activity relationship, delivery, and others. 

At the broadest end of the spectrum, filters based on the calculation of physiochemical properties, the most obvious being the Lipinski s rule of... 

Carotenoids are a class of lipophilic compounds with a polyisoprenoid structure. Most carotenoids contain a series of conjugated double bonds, which are sensitive to oxidative modification and cis-trans isomerization. There are six major carotenoids (ji-carotenc, a-carotene, lycopene, P-cryptoxanthin, lutein, and zeaxanthin) that can be routinely found in human plasma and tissues. Among them, p-carotene has been the most extensively studied. More recently, lycopene has attracted considerable attention due to its association with a decreased risk of certain chronic diseases, including cancers. Considerable efforts have been expended in order to identify its biological and physiochemical properties. Relative to P-carotene, lycopene has the same molecular mass and chemical formula, yet lycopene is an open-polyene chain lacking the P-ionone ring structure. While the metabolism of P-carotene has been extensively studied, the metabolism of lycopene remains poorly understood. 

Recently, metal cluster catalysts composed of two different metallic elements are of interest from both scientific and technological points of view because of their interesting physiochemical properties [46, 47]. Bimetallic clusters are known to exhibit specific reactivity. Their catalytic efficiency is also controlled by their size. 

Correlations between volume of distribution and experimental physiochemical properties... 

K. Kinoshita, Carbon, Electrochemical and Physiochemical Properties , Wiley Interscience, New York, 1988. 

Porphyrazines (pz), or tetraazaporphyrins, are compounds that can be viewed as porphyrin variants in which the meso carbon atoms are replaced with nitrogen atoms, as Fig. 1 shows (1). This difference intrinsically gives porphyrazines discrete physiochemical properties from the porphyrins. In addition, despite their similar molecular architecture, porphyrazines are prepared by an entirely different synthetic route than porphyrins—by template cyclization of maleonitrile derivatives, as in Fig. 2, where the open circle with the A in it represents the peripheral substituent of the pz—rather than by the condensation of pyrrole and aldehyde derivatives (1). The pz synthetic route allows for the preparation of macrocycles with chemical and physical properties not readily accessible to porphyrins. In particular, procedures have been developed for the synthesis of porphyrazines with S, N, or O heteroatom peripheral functionalization of the macrocycle core (2-11). It is difficult to impossible to attach the equivalent heteroatoms to the periphery of porphyrins (12). In addition, the preparation and purification of porphyrazines that bear two different kinds of substituents is readily achievable through the directed cocyclization of two different dinitriles, Fig. 3 (4, 5, 13). 

Electrochemistry-EPR. The redox potentials of the porphyrazines, 69a, 69b, 70a, and 70b were measured using cyclic voltammetry (Table XX). The redox potentials of the molybdocene appended porphyrazines 70a and 70b showed marked changes from that observed for the parent ligands 69a or 69b suggesting that the peripheral metalation by molybdocene profoundly alters the physiochemical properties of the macrocycle by more than just the sum of the two parts (6). 

The manner of nickel excretion depends on the route of exposure and the physiochemical properties of the nickel-containing material. In rodents, the major excretion pathway for absorbed nickel is renal about 90% of an administered dose is excreted according to this mechanism [281, 315]. 

This article will focus primarily on recent medicinal chemical studies aimed at addressing or studying particular issues which include inherent activity (versus the enzymatic target as well as in whole cells), in vivo efficacy, pharmacokinetics, physiochemical properties and efforts to elucidate salient features... 

Table 6.17. PHYSIOCHEMICAL PROPERTIES AND PHARMACOKINETICS OF (4S>7-(4-AMINO-2-SUBSTITUTED)QUINOLONES IN MICE [85]...

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