A series of experiments was conducted to determine the efficacy of 15 synthetic retinoic acid amides (retinamides) as inhibitors of chemical carcinogenesis of the urinary bladder in C57BL/6 x DBA/2F1 mice. Eight of the retinamides tested had significant protective activity when administered at nontoxic levels in the diet. Minor structural alterations, such as the addition of a methyl or hydroxyl group to the terminal amide moiety had a major influence on the anticarcinogenic activity of the retinamides. Although 13-cis retinamides generally were less toxic on a molar basis than were their all-trans isomers, no consistent pattern of differential anticarcinogenic activity was noted among the six pairs of all-trans and 13-cis isomers tested. All-trans-4-hydroxyphenyl retinamide was among the most active and least toxic of the retinoids tested, and appears to be the compound of choice for further study.
Cimetidin Kristallisiert monoklin (Raumgruppe P21/c). Seine Struktur wurde röntgenographisch bestimmt und bis R = 0.035 verfeinert. Im Einzelmolekül entsteht durch eine intramolekulare N…HN‐Wasserstoffbrückenbindung zwischen Imidazolring und Guanidingruppe ein stabiler zehngliedriger Ring. Intermolekulare Wasserstoffbrückenbindungen, die von der Cyanguanidingruppe ausgehen, verbinden zwei Nachbarmoleküle paarweise in einer Kopf‐Schwanz‐Anordnung zu einem Zwölfring. Diese Molekülpaare verknüpfen sich über Wasserstoffbrücken zwischen Imidazolring und Cyangruppe zu gewellten Schichten.
The discovery of a novel series of therapeutic agents that has been designed and optimized for treating chronic obstructive pulmonary disease is reported. The pharmacological strategy was based on the identification of compounds that inhibit a defined subset of kinase enzymes modulating inflammatory processes that would be effective against steroid refractory disease and exhibit a sustained duration of action after inhaled delivery.
Die Umwandlung von Aldehyden und Ketonen 2 in die um ein C‐Atom reicheren Allylalkohole 3 gelingt durch Umsetzung zu den Vinylsulfoxiden 7, deren Isomerisierung zu den Allylsulfoxiden 9 und nachfolgende [2,3]sigmatrope Umlagerung.
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