Activity Of Trans Research Articles

Antitumor activity of (trans)dermally delivered aromatic tetra-amidines

The present work describes the design and preparation of lecithin microemulsion gels containing the aromatic tetra-benzamidine (TAPP-Br) and the antitumor evaluation of this topical formulation on nude mice xenografted with the highly tumorigenic cell line FH06T 1 -1, in comparison to the antitumor activity of TAPP-Br administered by intraperitoneal injections (0.5 mg/injection).After (trans) dermal treatment with 0.1 ml lecithin gels incorporating TAPP-Br (0.2 mg/ml), a reduction of in vivo tumor cell growth was observed. These results could be of great interest with a view to developing a releasing system useful for experimental chemotherapy of tumor lesions occurring at cutaneous or subcutaneous level.

High Catalytic Activity of trans-[FeCl2(cyclam)]+ for Peroxidation of Linolenic Acid

Abstract The reaction mixture of trans-[FeCl2(cyclam)]+ and linolenic acid exhibited high ability for degradation of tetraphenylcyclopentadienone, one of the famous singlet oxygen(1Δg) quenchers, and the peroxidation of linolenic acid was found to proceed in this solution.

Synthesis and biological activity of trans(+-)-N-methyl-2-(3-pyridyl)-2-tetrahydrothiopyrancarbothioamide 1-oxide (RP 49356) and analogues: a new class of potassium channel opener.

The synthesis and biological activity of trans-(+-)-N-methyl-2-(3-pyridyl)-2-tetrahydrothiopyrancarbothioamid+ ++ e 1-oxide (8a, RP 49356) and analogues is reported. These compounds constitute a new structural class of K(+)-channel opener. The effects of changes in pyridyl group, thioamide, and thiane ring on in vitro K(+)-channel opening reactivity are discussed. A 3-pyridyl or 3-quinolyl group, a small N-alkyl thioamide function, and a thiane oxide ring, in which the sulfoxide is in a trans relationship to the thioamide, are preferred for activity. Selected compounds were tested intravenously in the normotensive anaesthetized rat for hypotensive effects, and the activities reflect their in vitro K(+)-channel opening activity. This led to further evaluation of compound 8a and the selection of the (-)-enantiomer 8b (RP 52891) for development as an antihypertensive and antianginal agent.

Synthesis and antimicrobial activity of optically active trans-cycloheximide isomers.

Optically active tiraras-cycloheximide isomers such as cycloheximide [(2S,4S,6R,αR)-form (1)], naramycin B[(25,4S,6RαR)-form(4)], and new stereoisomers (2S,4S,6S,αS)-form (8) and (2S,4S,6R,αS)-from (9) were synthesized by an aldol condensation of trans-2,4-dimethyl-l-cyclohexanone (5b), with 4-(2-oxoethyl)-2,6-piperidinedione(6). The antimicrobial activity of trans- cycloheximide isomers (1, 4, 8, and 9) was examined against S. cerevisiae and P. oryzae. The stereoisomers 1 and 4 exhibited marked antimicrobial activity against both microorganisms as compared with their C- α-epimers 8 and 9.

The activity of cis and trans -2- (aminomethyl) cyclopropane carboxylic acids on gaba — related mechanisms in the central nervous system of limulus and periplanata and of mammals

Some pharmacological actions of (±) — cis — and (±) — trans -2-(aminomethyl) cyclopropane carboxylic acids, conformationally restricted analogues of GABA, are described. The trans isomer (TAMP) was 17 and 4.5 times less active than GABA in hyperpolarising central neurones of Limulus and Periplanata and 10.8 times less active in displacing [ 3H]-muscimol from rat brain membranes. The cis isomer (CAMP) was ineffective on Limulusneurones at 35 μmoles, 650 times less active on Periplanata neurones and only weakly displaced [ 3H]-muscimol at 100 μm. Neither isomer inhibited synaptosomal uptake of [ 3H]-GABA at 100 μM. These data suggest that the invertebrate receptors studied respond to GABA in an extended conformation.

The surface active properties and anti-bacterial activity of the compounds, trans-[Rh(L) 4Cl 2]Cl· nH 2O

The antibacterial activity and surfactant activity of the compounds trans-[Rh(L) 4Cl 2]Cl· nH 2O increase in the order L = pyridine<4-methylpyridine<4-ethylpyridine<4- n-propylpyridine. As surfactants, the compounds are far more effective at reducing the interfacial tension, n-hexadecane H 2O , than the surface tension, H 2O air . The most effective and efficient surfactant in this series, trans-[Rh(4- n-propylpyridine) 4Cl 2]Cl·H 2O, can cause the leakage of intracellular manganese ions from the gram-positive bacteria, Bacillus brevis ATCC 9999, at a concentration of 130 ppm but there is no observable effect on the retention of intracellular manganese ions at the minimum concentration required to prevent growth of this organism (∼0.6 ppm at 23°C in nutrient broth). At 130 ppm, trans-[Rh(4- n-propylpyridine) 4Cl 2]Cl·H 2O does not cause the loss of intracellular manganese ions from the gram-negative bacteria, Escherichia coli JS-1. In this case, a concentration of at least 63 ppm of this rhodium compound is required to prevent the growth of this organism in M9TUH medium at 35°C. On the basis of these results, it is suggested that gross membrane disruption effects caused by the surfactants trans-[Rh(L) 4Cl 2]Cl· nH 2O are not directly responsible for their observed antibacterial action.