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At least 19 recordsLinked to original sources
PubMed1978

3-Tertiary amino-1-aryloxy- or aryl-propanes and -propan-2-ols and some related compounds.

The synthesis and pharmacological activity of some 3-tertiary amino-1-aryloxy- or 1-aryl-, 1-thiophenoxy and 1-anilino-propan-2-ols and -propanes, particularly those derived from N-phenylpiperazines are described. Effect of substituents (nature/position) on the phenyl ring, the phenoxy ring as well as alteration in the hydroxylic function vis-à-vis the structure-activity relationships (SAR) are discussed. In general, the 1-aryloxy compounds have hypotensive activity--this being more pronounced in those carrying an o-substituent on the phenyl ring, while m and p-substituted derivatives have their effect primarily on the CNS. Variations in the phenoxy moiety do not significantly alter the intrinsic activity. The 1-aryl compounds, on the other hand, have significant CNS activity, which is markedly affected by the substituents on the 1-aryl residue.

1-Propanol↗
PubMed1978

beta-Adrenergic blocking agents. 18. 1-(Aryloxy)-3-(arylthioalkylamino)propan-2-ols and 1-substituted alkylthioamino-3-(aryloxy)propan-2-ols.

The synthesis is described of a seris of derivaties of 1-(aryloxy)-3-(arylthioalkylamiho)propan-2-ols and 1-(alkylthioamino)- and 1-(aralkylamino)-3-(aryloxy)propan-2-ols. These compounds were investigated for their beta-adrenoreceptor blocking properties and their selectivity of action for the cardiac beta1 receptor. The structure-activity relationships are discussed with particular reference to the effects of the sulfur, sulfoxide, and sulfone groups on beta-adrenoreceptor blocking potency and selectivity.

Adrenergic beta-Antagonists↗
PubMed1975

A study of the oxidation of butan-1-ol and propan-2-ol by nicotinamide-adenine dinucleotide catalysed by yeast alcohol dehydrogenase.

1. The kinetics of oxidation of butan-1-ol and propan-2-ol by NAD+, catalysed by yeast alcohol dehydrogenase, were studied at 25 degrees C from pH 5.5 to 10, and at pH 7.05 from 14 degrees to 44 degrees C, 2. Under all conditions studied the results are consistent with a mechanism whereby some dissociation of coenzyme from the active enzyme-NAD+-alcohol ternary complexes occurs, and the mechanism is therefore not strictly compulsory order. 3. A primary 2H isotopic effect on the maximum rates of oxidation of [1-2H2]butan-1-ol and [2H7]propan-2-ol was found at 25 degrees C over the pH range 5.5-10. Further, in stopped-flow experiments at pH 7.05 and 25 degrees C, there was no transient formation of NADH in the oxidation of butan-1-ol and propan-2-ol. The principal rate-limiting step in the oxidation of dependence on pH of the maximum rates of oxidation of butan-1-ol and propan-2-ol is consisten with the possibility that histidine and cysteine residues may affect or control catalysis.

1-Propanol↗
PubMed1979

Cardioselectivity of beta-adrenoceptor blocking agents 1. 1-[(4-Hydroxyphenethyl)amino]-3-(aryloxy)propan-2-ols.

A series of 1-[(4-hydroxyphenethyl)amino]-3-(aryloxy)propan-2-ols was synthesized together with several 1-[(3,4-dimethoxyphenethyl)amino]-3-(aryloxy)propan-2-ols. Their affinity to beta 1- and beta-2-adrenoceptors was determined and compared with the affinity of known beta-blockers. We were able to confirm the substantial cardioselectivity of 1-(3,4-dimethoxyphenethyl)-3-[(4-substituted aryl)oxy]propan-2-ols when compared to those with a 1-(4-hydroxyphenethyl) group. An increase in the size of the 4 substitutent of the 3-(aryloxy) moiety to caproamido leads to a substantially higher affinity for the beta 1--adrenoceptor of rat ventricular muscle in the presence of the 3,4-dimethoxyphenethyl than in the presence of the 4-hydroxyphenethyl or isopropyl group; this combination also gave the highest cardioselectivity.

Adrenergic beta-Antagonists↗
PubMed1975

Effect of a single oral dose of methanol, ethanol and propan-2-ol on the hepatic microsomal metabolism of foreign compounds in the rat.

Methanol and ethanol administered to rats as a single oral dose increased aniline hydroxylation by the hepatic microsomal fraction by a maximum of 169 and 66% respectively, whereas aminopyrine demethylation was inhibited by 51 and 61%. The concentration of microsomal cytochrome P-450, and the activities of NADPH-cytochrome c reductase and NADPH-cytochrome P-450 reductase were unchanged. Propan-2-ol, administered as a single oral dose, increased microsomal aniline hydroxylation by 165% and increased aminopyrine demethylation by 83%. The concentration of cytochrome P-450 was unchanged whereas NADPH-cytochrome c reductase and NADPH-cytochrome P-450 reductase were both increased by 38%. Methanol, ethanol and propan-2-ol administration resulted in a decreased type I spectral change but had no effect on the reverse type I spectral change. Methanol administration decreased the type II spectral change whereas ethanol and propan-2-ol had no effect. Cycloheximide blocked the increases in aniline hydroxylation and aminopyrine demethylation but could not completely prevent the decreases in aminopyrine demethylation. The increases in aniline hydroxylation were due to an increase in V, but Km was unchanged. The ability of acetone to enhance and compound SKF 525A to inhibit microsomal aniline hydroxylation was decreased by the administration of all three alcohols. The decrease in the metabolism of aminopyrine may result from a decrease in the binding to the type I site with a consequent failure of aminopyrine to stimulate the reduction of cytochrome P-450. Methanol administration may lead to an increase in aniline hydroxylation because of a failure of aniline to inhibit cytochrome P-450 reduction.

1-Propanol↗
PubMed1979

Liquid propane cold injury: a clinicopathologic and experimental study.

A case of liquid propane cold injury is described. This injury was produced by evaporative heat loss, without ignition, from skin and underlying tissues. The cutaneous appearance was that of a flame burn but underlying deep tissue damage was present. Acute vascular compromise and progressive wound sepsis were complications which required surgical intervention. A liquid propane animal model was created which defined the pathophysiology of the clinical injury. The potential for this injury exists wherever volatile liquified gases are used.

Adolescent↗
PubMed1977

[Derivatives of 1,3-bis-(methlendioxyphenoxy)propane with antispastic activity].

A number of amines derived from 1,3-bis(3,4-methylen-dioxyphenoxy)propane have been prepared from 1,3-bis-(3,4-methylendioxy-phenoxy)propan-2-one. The acute toxicity and the activity of these compounds on isolated guinea pig ileum have been studied. The majority of the compounds showed clear antagonist activity towards BaCl2, histamine and acetylcholine contracting responses, generally grater than that of papaverine; on the contrary, their antagonist activity towards 5-HT responses was slightly lower.

Acetylcholine↗
PubMed1979

Bacterial metabolism of propane-1,2-diol.

The pathway of propane-1,2-diol metabolism by a species of Flavobacterium able to grow on the diol as the sole source of carbon was influenced by the degree of aeration of the growth medium. Under strongly aerobic conditions the diol was exclusively catabolised to lactaldehyde by an initial diol oxidase, subsequently metabolised to pyruvate and then oxidised to CO2 by the tricarboxylic acid cycle. Under microaerophilic conditions some propane-1,2-diol was catabolised by the oxidase-initiated pathway, but some diol was alternatively catabolised by an inducible diol dehydrase to propionaldehyde and subsequently reduced to n-propanol as an end product of metabolism.

Cell Division↗
PubMed1978

Cardioselectivity as a function of molecular structure in beta-adrenoceptor blocking agents of the 1-(para-substituted aryloxy)-3-(isopropylamino)propan-2-ol type.

The relationship between molecular structure and cardioselectivity is described in the 1-(para-substituted aryl-oxy)-3-(isoprophylamino)propan-2-ol type of beta-adrenoceptor blocking agents. Cardioselectivity in the aforementioned series requires that the aromatic substitution in the position para to the amino alcohol side chain will have a minimal linear length of 5.0 A. Highest cardioselectivity is obtained when this para substituent is a rigid group coplanar with the aromatic ring. This may result from steric hindrance for binding at the beta2-adrenoceptor subtype which does not occur in the beta1 subtype. Evidence in favor of this suggestion was obtained by the finding that the trans isomer of 1-[4-(1-propenyl)-2-methoxyphenoxy]-3-(isopropylamino)propan-2-ol is cardioselective (beta1/beta2 = 25), whereas the cis isomer is beta2 selective (beta1/beta2 = 0.1).

Adrenergic beta-Antagonists↗
PubMed1978

Metabolites of 1,2-epoxy-3-phenoxy- and 1,2-epoxy-3-(p-nitrophenoxy)propane.

1. Rabbits and rats dosed with 1,2-epoxy-3-phenoxypropane excrete 2-hydroxy-3-phenoxypropionic acid and N-acetyl-S-(2-hydroxy-3-phenoxypropyl)-L-cysteine. 2. Rabbits and rats dosed with 1,2-epoxy-3-(p-nitrophenoxy)propane excrete 2-hydroxy-3-(p-nitrophenoxy)propionic acid, N-acetyl-S-[2-hydroxy-3-(p-nitrophenoxy/propyl)propyl]-L-cysteine and p-nitrophenol. 3. The administration of either epoxide to the rat produces a marked fall in hepatic GSH level. 4. The biliary excretion of metabolites of 1,2-epoxy-3-(p-nitrophenoxy)-propane is described.

Animals↗
PubMed1979

[Experimental poisoning with gaseous hydrocarbons: changes in concentrations of propane and butane in the lung and adipose tissue in relation to the time of death].

Postmortal changes of propane, butane and iso-butane concentration in the lung and fat of mice exposed to lethal intoxication with commercial liquid gas are studied. The hydrocarbon tissue concentrations after exposure were determined by gas liquid chromatography. The hydrocarbons progressively decreased in the lung and disappeared, depending on the degree of putrefaction; even in case of remarkable putrefaction, it was still possible to detect them in the fat tissue.

Adipose Tissue↗
PubMed1977

Structural and functional determinants of Mucor miehei protease VI. Inactivation of the enzyme by diazoacetyl norleucine methyl esters, pepstatin and 1,2-epoxy-30(p-nitro-phenyoxy)propane.

Mucor miehei protease (EC 3.4.21 -- ), an acid protease of fungal origin, was rapidly inhibited at pH 5.0 and 10 degrees C by a 78-fold molar excess of diazoacetyl norleucine methyl ester (N2Ac-Nle-OMe) when simultaneously added with a 78-fold molar excess of Cu(II). Preincubation with Cu(II) before the addition of N2Ac-Nle-OMe reduced the initial rate of activity loss presumably due to a copper-induced structural change as deduced from an examination of CD spectra. Cof norleucine and 1.02 +/- 0.041 mol of copper. The conformation of the N2Ac-Nle-OMe-inhibited enzyme appeared to be somewhat altered since the rate of H-3H exchange determined for the slowest exchanging class of hydrogens was reduced by more than 10-fold although the estimated number of hydrogens in this class remained constant. Mucor miehei protease was also inhibited by pepstatin; complete inactivation required a 6-fold molar excess of inhibitor and was associated with a major conformational change as determined from CD spectra. Loss of activity also occurred in the presence of 1,2-epoxy-3-(p-nitrophenyoxy)propane (EPNP).

Aminocaproates↗
PubMed1976

On the reaction kinetics in water of 1,3-propane sultone and 1,4-butane sultone: a comparison of reaction rates and mutagenic activities of some alkylating agents.

To determine correlations between the biological action pattern and chemical reactivity of alkylating agents, the rate constants for reactions of 1,3-propane sultone and 1,4-butane sultone with a series of nucleophiles at 37 degrees C have been determined. Previously published data on the mutagenicity of the two sultones and of some alkyl methanesulfonates and dialkyl sulfates towards Schizosaccharomyces pombe have been used in the evaluation of the dependence of mutagenic effectiveness on chemical reactivity. It is of interest to note that the mutagenic effectiveness of the two sultones, if expressed per alkylating event at a certain low nucleophilicity is the same as that of e.g. methyl methanesulfonate and ethyl methanesulfonate.

Alkanesulfonates↗
PubMed1978

Animal experiments on the compensation of the immunosuppressive action of cyclophosphamide by 2-[-2-cyanaziridinyl-(1)-]-2-[-2-carbamoylaziridinyl-(1)]-propane BM 12 531.

BM U2 531, the 2-[2-Cyanaziridinyl-(1)-]-2-[-2-carbamoylaziridinyl-(1)-]-propane, the further development of BM 06 002 is able to compensate the immunosuppressive action of Cyclophosphamide and to increase the carcinostatic action of Cyclophosphamide. These properties are demonstrated 1. by a leucocytosis induced after application of BM 12 531 in rats 2. by a quick restauration of leucocyte depression induced by Cyclophosphamide in rats and dogs 3. by an increase of resistance against an infection (candida albicans) in mice 4. by an increase of antitumour effect of Cyclophosphamide against a DS-carcinosarcoma in rats.

Animals↗
PubMed1976

The structure and function of acid proteases. V. Comparative studies on the specific inhibition of acid proteases by diazoacetyl-DL-norleucine methyl ester, 1,2-epoxy-3-(p-nitrophenoxy) propane and pepstatin.

Comparative studies have been made on the effects of diazoacetyl-DL-norleucine methyl ester (DAN), 1,2-epoxy-3-(p-nitrophenoxy)propane (EPNP) and pepstatin on acid proteases, including those from Acrocylindrium sp., Aspergillus niger, Aspergillus saitoi, Mucor pusillus, Paecilomyces varioti, Rhizopus chinensis, and Trametes sanguinea, and also porcine pepsin [EC 3.4.23.1] and calf rennin [EC 3.4.23.4] for comparative purposes. These enzymes were rapidly inactivated at similar rates and in 1:1 stiochiometry by reaction with DAN in the presence of cupric ions. The pH profiles of inactivation of these enzymes were similar and had optima at pH 5.5 to 6. They were also inactivated at similar rates by reaction with EPNP, with concomitant incorporation of nearly 2 EPNP molecules per molecule of enzyme. The pH profiles of inactivation were again similar and maximal inactivation was observed at around pH 3 to 4. Some of the EPNP-inactivated enzymes were treated with DAN and shown still to retain reactivity toward DAN. All these enzymes were inhibited strongly by pepstatin, and the reactions of DAN and EPNP with them were also markedly inhibited by prior treatment with pepstatin. These results indicate that the active sites of these enzymes are quite similar and that they presumably have at least two essential carboxyl groups at the active site in common, one reactive with DAN in the presence of cupric ions and the other reactive with EPNP, as has already been demonstrated for porcine pepsin and calf rennin. Pepstatin appears to bind at least part of the active site of each enzyme in a simmilar manner.

Aminocaproates↗
PubMed1977

Amino acid sequences around 1, 2-epoxy-3-(p-nitrophenoxy)propane-reactive residues in rhizopus chinensis acid protease: homology with pepsin and rennin.

Two different peptides containing an aspartyl residue reactive with 1, 2-epoxy-3-(p-nitrophenoxy)propane (EPNP) in the acid protease from Rhizopus chinensis were isolated from a peptic digest of the EPNP-modified enzyme. One of the peptides was sequenced as Asp-Thr-Gly-Ser-Asp. The amino acid sequence had very high homology with those around the EPNP-reactive aspartyl residues in rennin (chymosin) [EC 3.4.23.4] and pepsin [EC 3.4.23.1]. The other peptide contained no methionine residue and gave the sequence: Asp-Thr-Gly-Thr-Thr-Leu. The N-terminal aspartyl residue of each peptide was deduced to be the EPNP-reactive site.

Amino Acid Sequence↗