Showing papers by "Eli Lilly and Company published in 1977"

Hyperalgesia induced by naloxone follows diurnal rhythm in responsivity to painful stimuli.

Abstract: A diurnal rhythm was observed in the responsiveness of mice to nociceptive stimuli and in the hyperalgesic activity of endogenous opioid peptides and may partly account for previous controversy over the direct action of naloxone in opiate-naive animals.

Macrolide Resistance in Staphylococcus aureus: Inducers of Macrolide Resistance

Abstract: Several macrolide-, lincosamide-, and streptogramin B-type (MLS) antibiotics were tested as inducers of erythromycin A (EM)-resistant [(14)C]leucine incorporation. Only 14-membered-ring macrolides having a glycosidically linked 6-deoxy sugar at the C-3 position of the lactone ring and the structurally dissimilar lincosamide, celesticetin, showed inducer activity. Modifications of EM at the C-4'' position of cladinose can apparently destroy the inducer property but do not affect the inhibitory properties of the antibiotic. The findings clearly show that inducer and inhibitor activities can be dissociated and are consistent with the concept that distinct binding/receptor sites are utilized for inhibition of ribosome function and induction of resistance.

Aqueous emulsion polymer nail coating formulations

Abstract: Novel nail coating formulations containing aqueous emulsion polymers which have a T g range from about -10° C. to 50° C., a solids content from about 30 to 55 percent, and a moisture vapor transmission of the film from about 0.1 to 1.6 mg./cm. 2 /hr. have improved properties, such as, reduced occlusion, faster drying time, non-yellowing of the nail, and non-flammable solvent.

Terminal Stages in the Biosynthesis of Tylosin

Abstract: Tylosin, a macrolide antibiotic, was co-produced with four structurally similar antibiotics in fermentation cultures of Streptomyces fradiae. Macrocin, desmycosin, lactenocin, and relomycin were found to be components of a common pathway that functions in tylosin biosynthesis. Data obtained by the addition of the purified (14)C-labeled antibiotics to cultures of S. fradiae revealed that macrocin and desmycosin were direct precursors of tylosin, whereas lactenocin was an immediate precursor of both macrocin and desmycosin. Incubation of these cultures with [(14)C]tylosin resulted in an equivalent distribution of radioactive label between relomycin and an unidentified component. The kinetics of incorporation of label into the two species were similar, suggesting that both were derived directly from tylosin. A system that supported that methylation of macrocin to tylosin by cell-free extracts of S. fradiae was developed. A proposed scheme defining the terminal stages of tylosin biosynthesis is presented.

Use of solvent cavity area and number of packed solvent molecules around a solute in regard to hydrocarbon solubilities and hydrophobic interactions

Abstract: Two currently used methods of calculating the area of contact between a solute molecule and the solvent are examined and some important differences are pointed out. Some pitfalls and uncertainties in the application of the concept of molecular surface area to the quantitative estimation of unitary free energies of solution are discussed.

Genetics of obesity in zucker rats and koletsky rats

Abstract: The breeding data on Zucker rats and on Koletsky rats confirm that the obesity in these two strains of rats is inherited recessively and results from single gene mutations. Mating a Zucker heterozygote to a Koletsky heterozygote produced obese F1 progeny. Inter-stock breeding results indicate that the obesity in the Zucker-Koletsky hybrid stock is also inherited in a recessive manner. The gene that controls obesity in the Zucker rats, fatty (fa), and the gene that controls obesity in the Koletsky rats, f, are thus alleles at the same locus. We propose that f be renamed fak until it can be proven that fa and fak are identical.

The isolation and structure elucidation of macrocyclic lactone antibiotic, A26771B.

Abstract: The isolation, biological properties and structure elucidation of a sixteen-membered macrocyclic lactone antibiotic, designated A26771B (1), obtained from Penicillium turbatum are discussed.

Carton and bag container

Abstract: A collapsible carton and plastic bag container is provided from a single sheet of plastic material and a single layer of paper board which is affixed to the plastic sheet material.

Somatostatin analogs and intermediates thereto

Abstract: The tetradecapeptides ##STR1## in which Y is L-Asn or L-Ala are described along with corresponding non-toxic pharmaceutically-acceptable acid addition salts as well as intermediates useful in the synthesis of the tetradecapeptides. These tetradecapeptides as well as their pharmaceutically-acceptable acid addition salts exhibit various activities including inhibition of the release of gastric acid.

Penicillin conversion by halogen electrophiles and anti-bacterials derived thereby

Abstract: Novel beta-lactam compounds of the formula ##STR1## and process for their preparation in which a penicillin ester is reacted with a source of positive halogen to selectively open the thiazolidine nucleus of the penicillin. These compounds are useful as intermediates in the preparation of novel anti-bacterial compounds of the formula: ##STR2##

Rapid Analysis of Cefazolin in Serum by High-Pressure Liquid Chromatography

Abstract: A high-pressure liquid chromatography (HPLC) method has been developed for the analysis of cefazolin in serum. Serum was deproteinized by the addition of 6% trichloroacetic acid and injected onto a reverse-phase column with a mobile phase of 10 to 15% methanol in 1% aqueous acetic acid. Cefazolin chromatographed without interference from ultraviolet-absorbing components of serum, with a retention time of 3.1 min. Standard curves comparing peak area with concentration prepared from dog or human sera were linear over a range of 1.6 to 200 μg/ml. Results from the HPLC assay were compared with microbiological assays (cylinder plate method) on both standard serum samples and sera from dogs and human subjects receiving intramuscular cefazolin. The HPLC method was somewhat more accurate in comparison with the microbiological assay performed on serum samples of known concentration. The comparison of results from an analysis of serum levels of dogs or human subjects receiving cefazolin indicated that the two methods would lead to identical conclusions concerning pharmacokinetics or the achievement of therapeutic serum levels. The HPLC assay method presents an alternative to conventional microbiological assays, with marked improvement in speed (30 min) and considerable potential for future development.

Dissociation of obesity, hypercholesterolemia and diabetes from atherosclerosis in ob/ob mice

Abstract: Genetically obese, diabetic and hypercholesterolemic C57BL/6J-ob/ob mice were placed on Purina Laboratory Chow containing 2% cholesterol for up to 4 months. They developed higher plasma cholesterol levels and accumulated an increased quantity of cholesterol in the liver but failed to develop atherosclerotic lesions in the aorta as would be expected in an obese, diabetic and hypercholesterolemic human adult.

Substituted azetidin-2-one antibiotics

Abstract: Monocyclic β-lactam antibiotics of the formula ##STR1## WHEREIN R is amino or acylamino, e.g., phenylacetylamino, phenylglycylamino and 2-[4-(3-amino-3-carboxypropoxy)phenyl]-2-hydroximinoacetylamino; R1 is H or ester forming group; R2 is H, --OCH3, --SCH3, or --CH3 ; and R3 is H or acetoxy; are useful antibacterials for controlling β-lactamase producing gram-negative bacteria and other pathogens. Intermediates useful in the preparation of the antibiotics and a novel process for preparing 4α-acetoxy substituted azetidin-2-ones are provided.

Pleuromutilin glycoside derivatives

Abstract: Pleuromutilin glycoside derivatives which are useful agents against gram-positive and gram-negative bacteria, anaerobic bacteria, and mycoplasma.

A2315, new antibiotics produced by Actinoplanes philippinensis. 2. Structure of A2315A.

Abstract: Antibiotic A2315A is a new member of the virginiamycin family of antibiotics. Physical and chemical data indicate that it is related to ostreogrycin A. Structure II is proposed for A2315A.

Weed competition in irrigated cotton (Gossypium barbadense L.) and groundnut (Arachis hypogaea L.) in the Sudan Gezira

Abstract: Summary: Losses of crop yield due to weed competition in unweeded plots averaged nearly 60% of weed-free yields in cotton and 70% in groundnuts. Weed competition was not directly related to weed groundcover but was dependent on the seasonal growing conditions. The critical period of weed competition in both crops was the 6 weeks between 4 and 10 weeks after crop emergence. During this period cotton could tolerate up to 25% weed groundcover without appreciable loss in crop yield. Groundnuts could tolerate not more than 10% weed cover before yield loss occurred. A main factor in achieving standards of weed control within these limits was preventing the early growth of monocotyledonous weed species: pre-sowing application of trifluralin and benfiuralin provided this over a wide range of growing conditions. Resume: Concurrence des mauvaises herbes dans les cultures de coton irrigue (Gossypium barbadense L.) et d'arachide (Arachis hypogaea L.) au Soudan Gezira Les pertes de rendement provoquees par la concurrence des mauvaises herbes dans les parcelles non desherbees ont atteint en moyenne pres de 60 pour cent par rapport aux parcelles desherbees, pour le coton et 70 pour cent pour l'arachide. La concurrence des mauvaises herbes ňa pas ete en fonction directe de la couverture du sol par les mauvaises herbes mais elle a ete en relation avec les conditions saisonnieres de croissance. La periode critique de la concurrence des mauvaises herbes, pour les deux cultures, sest situee pendant les six semaines qui separent la quatrieme et la dizieme semaine apres la levee de la plante cultivee. Pendant cette periode, le coton a supporte jusqu'a 25 pour cent de couverture du sol, sans perte de rendement appreciable. Les arachides n'ont pas supporte plus de 10 pour cent de couverture sans qu'une perte de rendement se produise. l'un des facteurs principaux dans les regles a observer pour le desherbage durant cette periode a ete de prevenir une croissance precoce des especes monocotyledones de mauvaises herbes: des applications de trifluraline et de benfluraline en presemic ont assure l'observance de cette regle dans une large serie de conditions de croissance. Zusammenfassung Unkrautkonkurrenz in bewaserter Baumwolle (Gossypium barbadense L.) und Erdnuss (Arachis hypogaea L.) in der Gezira Sudan Die Ertragsverluste durch Unkrautkonkurrenz in den verunkrauteten Parzellen betrugen durchschnittlich 60% bei Baumwolle und 70% bei Erdnuss, bezogen auf die Ertrage in den unkrautfreien Parzellen. Die Unkrautkonkurrenz stand nicht in direktor Beziehung mit dem Unkrautdeckungsgrad, war aber von den saisonalen Wachstumsbedingungen abhangig. Bei beiden Kulturpflanzen war die kritische Periode der Unkrautkonkurrenz die Zeit zwischen der vierten und zehnten Woche nach ihrem Auflaufen. Wahrend dieser Periode konnte die Baumwolle bis zu 25% Unkrautbedeckung ohne nennenswerten Ertragsverlusttolerieren. Bei der Erdnuss waren es nicht mehr als 10%. Um innerhalb dieser Grenzen eine gute Unkrautbekampfung zu erreichen, war es wichtig die fruhe Entwicklung monokotyler Arten auszuschliessen. Durch die Vorsaatbehandlung mit Trifluralin und Benfluralin war diese Bedingung uber einen weiten Bereich von Wachstumsbedingungen zu erreichen.