Activity reduction

Some of these compounds show antibacterial activity. Reduction gives 2-[(2-aminoethyl)amino]ethanols which react with organic acids to form amides that, on further heating, cyclize to imidazolines (6). For example, the diamine obtained by reducing (1) reacts with an organic acid (R"COOH) to give... 

Incorporation of extensive branching in the side chain similarly does not decrease pharmacologic activity. Reductive alkylation of aminoalcohol, 42, with isobutyraldehyde affords the amine, 43. Acylation of the amine with benzoyl chloride probably goes initially to the amide (44). The acid catalysis used in the reaction leads to an N to 0 acyl migration to afford iso-bucaine (45). ... 

It is known that the presence of the 143-hydroxyl group and a sugar at the 3 position are absolute requirements for activity. A modified drug actodigin (100) demonstrates that reversal of the lactone 17 is consistent with activity. Reduction of digitoxigenin 91, the aglycone of digitoxin... 

Zivin JA, Lyden PD, DeGirolami U, Kochhar A, Mazzarella V, Hemenway CC, Johnston P. Tissue plasminogen activator. Reduction of neurologic damage after experimental embolic stroke. Arch Neurol. 1988 45 387-391. 

A comprehensive account of the oxidation of benzylamine by both neutral and alkaline permanganate has been published recently . The neutral amine is the active reductant at all pH values and at pH 9.9 good second-order kinetics were obtained. Under these conditions the stoichiometry is... 

Further data on this reaction are summarised in Table 20. The role of complexing anions is clear from the kinetics and also from relative rates. It appears that strongly bound ligands are associated with second-order reduction but that weakly bound ligands such as H2O result in a third-order reaction. One view of the third-order term for dilute sulphuric acid (as for aqueous HCIO4) is that the active reductant is a bridged species of the type (Fe S04 Fe ) . 

Sodium borohydride is sometimes used in conjunction with CeCl3 (Luche s reagent).70 The active reductants under these conditions are thought to be alkoxyborohydrides. Sodium cyanoborohydride is a useful derivative of sodium borohydride.71 The electron-attracting cyano substituent reduces reactivity and only iminium groups are rapidly reduced by this reagent. 

A catalytic amount (5-20 mol %) of the reagent, along with BH3 as the reductant, can reduce ketones such as acetophenone and pinacolone in more than 95% e.e. An adduct of borane and 18 is the active reductant. This adduct can be prepared, stored,... 

In a similar vein, the keto bridge in 5 can be replaced by oxygen with retention of activity. Reduction of acetophenone derivative 19 by means of sodium borohydride leads to the corresponding alcohol (20). Reaction with phosphorus tribromide with cyanide gives... 

The release of N2 occurs within function 3. It involves the dissociation of NO (via a dinitrosyl-adsorbed intermediate), followed by subsequent formation of N2 and scavenging of the adsorbed oxygen species left from NO dissociation. The removal of adsorbed oxygen is due to the total oxidation of an activated reductant (CxHyOz). This reaction corresponds to a supported homogeneous catalytic process involving a surface transition metal complex. The corresponding catalytic sequence of elementary steps occurs in the coordinative sphere of the metal cation. 

A dinitrosyl (NO)2 species forms, whose dissociation leads to N2 the remaining adsorbed oxygen species have to be scavenged by the activated reductant, C, HvOz to recover the free active site, permitting the catalytic cycle to turn over (Figure 5.1, function 3) [10]. 

DeNO should occur as soon as active reductants are delivered to alumina at the temperature when NO dissociates, to scavenge Oads left by NO (function 3). 

Scheme 10 Activity reduction in ethylene-methyl acrylate copolymerizations due to the formation of stable chelate 1.30...

Unusual Carbon Monoxide Activation, Reduction, and Homologation Reactions of 5/-Element Organometallics... 

No adverse effect on liver microsomal activity Reduction in liver aniline hydroxylase activity liver histopathology... 

Acute oral LD50 for rats fed a normal protein diet (USEPA 1980) Reduced sexual activity, reduction in number of viable litters, increased rate of death of progeny prior to weaning (WHO 1984)... 

Life-style modifications Weight reduction Moderation of alcohol intake Regular physical activity Reduction of sodium intake Smoking cessation... 

Nitration opens up another pathway to metabolic activation. Nitro-PAHs are wide-spread environmental pollutants that are mutagenic and carcinogenic. Metabolism of nitro-PAHs could occur via nitro-activation (reduction to hydroxylamine, eventually leading to nitrenes that can bind to nucleotides) and/or by ring oxidation and formation of DEs. ... 

Spontaneous activity reduction. Petroleum ether extract of the dried entire plant, administered intraperitoneally to guinea pigs at a dose of 100 mg/kg, was active . 

T0056 Arctech, Inc., Light-Activated Reduction of Chemicals (LARC)... 

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