Abstract: Compositions and methods are provided including a transporter peptide derived from the loop2 domain of the neuronally-derived lynx1 protein which can be conjugated to an effector agent to form a transporter-effector complex for transport of the therapeutic effector agent to a target that is found across the blood brain barrier.

Abstract: Aldehyde- and ketone-functionalized proteins are promising new substrates for the development of chemically modified biotherapeutics and protein-based materials. Their reactive carbonyl groups are typically conjugated with a-effect nucleophiles, such as substituted hydrazines and alkoxyamines, to generate hydrazones and oximes, respectively. However, the resulting C?N linkages are susceptible to hydrolysis under physiologically relevant conditions, which limits their utility in biological systems. Here we introduce a Pictet-Spengler ligation that is based on the classic Pictet-Spengler reaction of aldehydes and tryptamine nucleophiles. The ligation exploits the bioorthogonal reaction of aldehydes and alkoxyamines to form an intermediate oxyiminium ion; this intermediate undergoes intramolecular C—C bond formation with an indole nucleophile to form an oxacarboline product that is hydrolytically stable.

Abstract: A tetrakis(hydroxyphenyl)chlorin, bacteriochlorin or isobacteriochlorin, derivatised at one or more of the hydroxy groups by addition reaction with a diisocyanate, diisothiocyanate or isocyanate-isothiocyanate at one isocyanate or isothiocyanate group thereof, the other isocyanate or isothiocyanate group being itself derivatised by addition reaction with the hydroxy group of an w-alkylated or acylated poly(alkylene oxide) or to a hydroxy group of a link residue itself carrying a residue of such poly(alkylene oxide).

Abstract: A method for accelerating the process of removing ethanol from the blood through the use of certain additives that accelerate the metabolic oxidation of ethanol, and others which in addition act as catalysts or “pseudo” enzymes for the oxidation. These additives include multivalent transition metal ions, as well as complexes thereof, and NAD+ which enhance the oxidation reaction. The method described can act as a sobriety inducer and/or as an effective palliative for the unpleasant effects of overuse of ethanol.

Abstract: A composition for accelerating the disposal of ethanol from bodily fluid. Certain additives can accelerate the metabolic oxidation of ethanol, and others in addition act as catalysts or “pseudo” enzymes for the oxidation. Additives include the oxidant Nicotinamide Adenine Dinucleotide and a variety of other additives such as transition metal ions and complexes thereof which favor the oxidation reaction. The compositions described can act as a sobriety inducer and/or as an effective palliative for the unpleasant effects of overuse of ethanol.

Abstract: A fullerene-antibiotic conjugate including at least one antibiotic molecule per fullerene moiety. The fullerene may comprise C60 and the antibiotic may comprise vancomycin or may be selected from the group consisting of penicillins, cephalosporins, quinolones, fluoroquinolones, macrolides, lincosamines, carbepenems, conobactams, aminoglycosides, glycopeptides, tetracyclines, sulfonamides, rifampin, oxazolidonones, and streptogramins. The conjugate preferably includes at least two and more preferably at least three antibiotic molecules per C60 center. A method for making a fullerene(C60)-antibiotic conjugate, comprises: synthesizing a linker precursor (I); reacting the linker precursor (I) with C60 via a Bingel-reaction, to produce a fullerene-linker conjugate (II); hydrolyzing the fullerene-linker conjugate (II), resulting in a desired derivative of C60 (III); and reacting the derivative (III) with a desired antibiotic to produce a fullerene-antibiotic conjugate (IV).

Abstract: Disinfectant formulations are described which are preferably ecologically friendly and non-toxic to mammals and plants, and are highly effective against a broad spectrum of detrimental pathogenic microorganisms. The microbicidal formulation contains complexes having at least one metal ion which is microbicidal to at least one microorganism and potassium sodium tartrate in some form. When potassium sodium tartrate is used with these metal ions, it enhances the complex-forming properties of such metal complexes while concurrently increases their efficacy and potency at the same level of metal ion concentrations. These microbicidal formulations can be diluted in suitable proportions into aqueous systems to produce the desired dosages for each individual case, depending on the level and the severity of the contamination. The microbicidal formulations can be applied by conventional methods, e.g., spraying, soaking, fogging, impregnation, and the like.

Abstract: A biocidal composition composed of a ternary complex of a negatively-charged biocide, a transition metal ion and chelator has synergistic biocidal effects as compared with a composition of each of the components alone. The chelator is preferably a neutral or positively-charged chelator. The ternary complex may be used for killing or inhibiting the growth of living cells.

Abstract: A composition and method for ameliorating a cellular dysfunction of a tissue such as the cosmetic treatment of hair loss and stimulation of hair growth are disclosed. The method comprises administering a spin label such as 2-(acetoxymercuri)-4,4,5,5-tetramethyl-2-imidazolin-1-yloxy-3-oxide, 3-carbamoyl-2,5-dihydro-2,2,5,5,-tetramethyl-1H-pyrrol-1-yloxy, or 3-(?ethoxycarbonyl!-oxycarbonyl)-2,5-dihydro-2,2,5,5-tetramethyl-1H-pyrrol -1-yloxy to the affected tissue.

Abstract: The invention relates to 1-aryl-2-fluoro-2-azolyl alkanones, alkanols, esters and ethers of formula I ##STR1## wherein Az is 1H-1,2,4-triazole, 4H-1,2,4-triazole or 1H-imidazole;T is --C(O)--, --CH(OH)-- or one of the groups ##STR2## wherein R.sub.7 is C.sub.1 -C.sub.6 alkyl which is unsubstituted or substituted by C.sub.1 -C.sub.3 -alkoxy, halogen or cyano, or is C.sub.3 -C.sub.6 alkenyl, C.sub.3 -C.sub.6 alkynyl, C.sub.3 -C.sub.6 cycloalkyl, 2-furyl, 2-tetrahydrofuryl, or is phenyl or benzyl, each unsubstituted or substituted by halogen, nitro, C.sub.1 -C.sub.3 -alkyl, C.sub.1 -C.sub.3 alkoxy, C.sub.1 -C.sub.3 haloalkyl and/or C.sub.1 -C.sub.3 haloalkoxy;R.sub.8, R.sub.9 and R.sub.10 are each independently hydrogen, nitro, halogen, cyano, C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy, C.sub.1 -C.sub.3 haloalkoxy, --COO(C.sub.1 -C.sub.3 alkyl), NH.sub.2 or NHCOCH.sub.3 ;R is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.1 and R.sub.2 are each independently hydrogen, halogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.

Abstract: 1-Azolyl-3-pyrazolyl-2-propanol derivatives of the general formula ##STR1## in which Az represents 1,2,4-triazol-1-yl, imidazol-1-yl or pyrazol-1-yl andR represents alkyl, alkenyl, alkinyl, optionally substituted phenyl, optionally substituted phenylalkyl, optionally substituted phenylalkenyl, optionally substituted phenylalkinyl, naphthyl or optionally substituted cycloalkyl,and acid addition salts and metal salt complexes thereof, which possess fungicidal activity. Oxirane intermediates lacking Az are also new.

Abstract: The invention relates to microbicidal mandelic acid derivatives of the formula I ##STR1## wherein X is the bridge member --CH.dbd. or --N.dbd.,Ar is a phenyl, diphenyl or naphthyl group,R.sub.1, R.sub.2 and R.sub.3 independently of one another are hydrogen, nitro, halogen, C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy or C.sub.1 -C.sub.3 haloalkyl,R is one of the groups ##STR2## R.sub.5 is C.sub.2 -C.sub.10 alkenyl which is unsubstituted or substituted by halogen; C.sub.2 -C.sub.10 alkynyl which is unsubstituted or substituted by halogen; or is a C.sub.3 -C.sub.8 cycloalkyl group or a phenyl group which is unsubstituted or substituted; or is a C.sub.1 -C.sub.12 alkyl chain which from C.sub.2 alkyl may be interrupted by oxygen or sulfur and is unsubstituted or substituted by a member selected from the group consisting of halogen, phenyl, --COO--C.sub.1 --C.sub.4 alkyl, --CO--C.sub.1 --C.sub.