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PubMed1978

tert-Butoxycarbanyl as a convenient protecting group in synthesis of potential centrally active dopamine derivatives.

Several pivaloyl and pivaloyloxy esters and amides of dopamine were synthesized for possible antiparkinson activity. The compounds were synthesized by select O- and N-acylation and N-methylation procedures. The tert-butoxycarbonyl function is an effective and easily removed nitrogen-protecting group for dopamine. Preliminary biological testing results showed that all compounds tested elicited a hypothermic response in mice, while only O,O-dipivaloyl-N,N-dimethyldopamine reversed reserpine-induced motor depression in mice. However, it is difficult to conclude from the preliminary data that the observed biological effects were due to central dopaminergic receptor stimulation.

Animals↗
PubMed1979

Isolation and identification of 3,3',5,5'-tetrabis(tert-butyl)stilbenequinone from polyethylene closures containing titanium dioxide and butylated hydroxytoluene.

A yellow compound was isolated from commercially available, discolored, polyethylene ophthalmic closures containing titanium dioxide and butylated hydroxytoluene (I). This compound was present at 7.46 ppm (w/w). It was identified by UV, IR, and mass spectra as 3,3',5,5'-tetrabis(tert-butyl)stilbenequinone (II), a dimer of I. Further structural confirmation was obtained by NMR. Formation of II is catalyzed by titanium dioxide.

Butylated Hydroxytoluene↗
PubMed1979

GLC determination of S-2-(3-tert-butylamino-2-hydroxypropoxy)-3-cyanopyridine in human plasma.

S-2-(3-tert-Butylamino-2-hydroxypropoxy)-3-cyanopyridine was recovered (approximately 90%) from human plasma and detected by conversion to a diheptafluorobutyryl derivative for electron-capture GLC. A homolog served as an internal standard. The method measures plasma drug concentrations at the 5-ng/ml level and is suitable for plasma analysis from humans who receive a therapeutic oral dose.

Antihypertensive Agents↗
PubMed1979

Synthesis of amino acyl adenylates using the tert-butoxycarbonyl protecting group.

Alayl, [ 14c]-alanyl, phenylalanyl, and methionyl adenylates have been synthesized in high yields and relatively good purities. Elemental analysis 1H nmr and ir spectra have been utilized for the characterization of these extremely labile compounds. The present synthesis, which uses readily available N-tert-butoxycarbonyl amino acids, is compared with previous methods.

Adenosine Monophosphate↗
PubMed1975

Some biochemical and physiochemical properties of the potent uncoupler SF 6847 (3,5-di-tert-butyl-4-hydroxybenzylidenemalononitrile).

Various physicochemical and biochemical properties of the most potent uncoupler of oxidative phosphorylation known to date 3,5-di-tert-butyl-4-hydroxybenzylidenemalononitrile (SF 6847), such as pH dependence of the uncoupling activity and binding to mitochondria, spectral properties in the presence of different types of liposomes, biopolymers and mitochondria, and effects on model membrane systems have been investigated. From the results, it is concluded that the uncoupler most likely is localized in the phospholipid part of the membrane.

Animals↗
PubMed1977

Occupational vitiligo induced by p-tert-butylphenol, a systemic disease?

Vitiligo, morphologically indistinguishable from true vitiligo, was detected in 54 of 198 men exposed to p-tert-butylphenol (P.T.B.P.) during its manufacture. There is evidence that P.T.B.P. caused vitiligo by a systemic mechanism and that the severity of the disease was related to the intensity of exposure. No association with autoimmune disease was found. Screening for other possible associated disorders revealed mildly abnormal liver-function tests in 6 workers: liver biopsy confirmed liver damage. Of the 144 men exposed to P.T.B.P. who did not have vitiligo, only 2 had any abnormal liver-function tests. It seems possible that the liver damage is related to P.T.B.P.

Chemical Industry↗
PubMed1979

Synthesis and chemical carcinogen inhibitory activity of 2-tert-butyl-4-hydroxyanisole.

The title compound 1 was selectively synthesized in its pure isomeric form by means of the hydroxyl-protecting reagent dimethyl-tert-butylchlorosilane. Exclusive silylation occurred at the less hindered hydroxyl group of 3. Dimethyl sulfate methylation of 4 gave 5 in excellent yield. Compound 1 was then obtained by acid hydrolysis of 5. The two BHA isomers, 1 and 2, were tested on their inhibitory effects toward benzo[alpha]pyrene-induced neoplasia in the forestomach of the ICR/Ha mouse. Both isomers, when added to the diet, reduced the number of mice with tumors and the number of tumors per mouse. Isomer 1, which has the less hindered free hydroxyl group, showed higher inhibitory effect in the present experimental model.

Animals↗
PubMed1979

The effect of (6-D-(O-TERT-B)-Ser)-gonadoliberin-(1--9) nonapeptide-ethylamide on gonadotropin release in prepubertal boys.

(6-D-(o-tert-B)-Ser)-gonadoliberin-(1--9) nonapeptide-ethylamine, (HOE 766), a highly active LH-RH analogue, was studied with regard to its effects on the release of follicle stimulating hormone (FSH) and luteinizing hormone (LH) in 29 prepubertal boys given different doses (1 microgram, 2,5 microgram, 5 microgram or 7,5 microgram respectively). The effect of HOE 766 is dose dependent for FSH, but not for LH. There are important differences in the reaction of these young subjects from those of adults. Whereas LH levels barely rose, FSH secretion was superior to that seen in adults.

Child↗
PubMed1977

Metabolism of crufomate [(4-tert-butyl-2-chlorophenyl methyl methylphosphormidate)] by the rat.

Fifteen metabolites of crufomate (4-tert-butyl-2-chlorophenyl methyl methylphosphoramidate, I) were identified in the excreta from rats given single oral doses of I. Compound I was not detected in either the urine or the feces. The metabolic reactions observed were N-and O-demethylation, oxidations of the t-butyl moiety, replacement of the H-N-CH3 with an OH moiety, hydrolysis of the phosphoramidate moiety to yield the phenol, conjugation with glucuronic acid, and combinations of these reactions. No ring dehalogenation or ring substitution was observed.

Animals↗
PubMed1979

Metabolism of crufomate (4-tert-butyl-2-chlorophenyl methyl methylphosphoramidate) administered topically to a sheep.

A sheep dosed topically with 14C-crufomate (4-tert-butyl-2-chlorophenyl methyl methylphosphoramidate) excreted 45.5% of the 14C dose in the urine within 9 days. The feces contained 1.2% and the carcass 40.4% (this included the 37.7% of the dose remaining on the skin in the dosing area) of the dose. At sacrifice, the fat, liver, kidney, lung, and skin (where the dose was applied) contained the highest concentrations of 14C. Fourteen urinary metabolites were isolated and characterized by mass spectrometry. The metabolic reactions involved were oxidations of the t-butyl moiety, O-demethylation, replacement of the H-N-CH3 moiety with a hydroxyl group, oxidation of the N-methyl group to yield N-formyl phosphoramidates, hydrolysis of the phosphoramidate moiety to yield phenols, conjugation with glucuronic acid and combinations of these reactions.

Administration, Topical↗
PubMedDate not supplied

Antiarrhythmic properties of 5-(3-tert-butylamino-2-hydroxy)propoxy-3,4-dihydrocarbostyril hydrochloride (OPC-1085), a newly synthesized, potent beta-adrenoreceptor antagonist.

1. The antiarrhythmic properties of 5-(3-tert-butylamino-2-hydroxy)propoxy-3,4-dihydrocarbostyril hydrochloride (opc-1085) were compared with those of propranolol and pindolol using various kinds of preparations for experimental arrhythmia in dogs. 2. Although OPC-1085 was the most potent drug to antagonize adrenaline-induced arrhythmia in animals anaesthetized with either pentobarbitone sodium or halothane, it was scarcely effective on ouabain-induced arrhythmia in pentobarbitone sodium anaesthetized animals. 3. When these compounds were administered intravenously to conscious dogs 24 h after two-stage ligation of the anterior descending artery, ectopic ventricular beats of coronary ligation-induced arrhythmia were reduced while regular sinus beats were simultaneously increased. 4. OPC-1085 was very effective on aconitine-induced arrhythmia in dogs anaesthetized with pentobarbitone sodium. The effective dose was similar to that of propranolol but about fifteen times less than that of pindolol. 5. It is concluded that different potencies among these beta-adrenoreceptor antagonists against various kinds of experimental arrhythmias cannot be simply deduced from any one of the following properties; beta-adrenoreceptor antagonism, intrinsic myocardial stimulation, local anaesthetic and so-called quinidine-like effects.

Aconitine↗
PubMed1977

Pharmacodynamics of a new selective beta2-adrenergic bronchodilator 3-(4-methoxybenzylamino)-4-hydroxy-alpha-(tert. butylaminomethyl)-benzyl-alcohol, HCl (QH25).

The bronchodilator effect of QH25 (3-(4-methoxybenzylamino)-4-hydroxy-alpha-(tert. butylaminomethyl)benzylalcohol, HCl) a new beta2-adrenergic bronchodilator has been investigated in conscious guinea pigs and in anaesthetized guinea pigs and cats and compared to that of salbutamol and isoprenaline. In anaesthetized guinea pigs QH25 and isoprenaline were equipotent after intravenous administration, whereas salbutamol was four times less active. The same difference between QH25 and salbutamol was observed after intraduodenal administration. After oral administration in conscious guinea pigs QH25 was eight and five times more potent than salbutamol and isoprenaline respectively, whereas no difference was observed when the agents were administered as aerosols. The bronchodilator action of QH25 was apprxomately three times that of salbutamol in egg-albumine sensitized guinea pigs after oral administration. In anaesthetized cats the bronchodilator potency of QH25 was three times that of salbutamol and the same or slightly higher than that of isoprenaline. A half-life of 4 hours for the bronchodilator action in guinea pigs was determined for both QH25 and salbutamol after oral administration. The effect of QH25 and salbutamol on cardiovascular parameters i.e. chrono- and inotropic action and blood pressure decreasing effect in guinea pigs, cats and dogs was essentially the same whereas isoprenaline was from 5 to 30 times more potent. The potential tremorogenic action of QH25 estimated on the cat soleus muscle was eight times less than that of isoprenaline and the same or slightly less than that of salbutamol. From the experimental data it is concluded that QH25 has the same potency as isoprenaline as a bronchodilator agent but is more potent than salbutamol. Taking into account that isoprenaline is considerably more active on cardiovascular parameters and on the cat soleus muscle than QH25 which has the same or less effect than salbutamol on these parameters the data suggest that QH25 is a more selective bronchodilator agent than both isoprenaline and salbutamol.

Acetylcholine↗
PubMed1975

Pharmacological studies of 1-(o-chlorophenyl)-2-tert.-butylaminoethanol (C-78), a new bonchodilator.

The bronchodilating effects and other related pharmacological properties of 1-(o-chlorophenyl)-2-tert.-butylaminoethanol-hydrochloride (C-78) were studied in comparison with those of isoproterenol, salbutamol and clorprenaline. C-78 was found to produce a bronchodilating effect 2--10 times stronger and considerably weaker than clorprenaline and isoproterenol, respectively. However, the bronchodilating effect of C-78 was sustained more than 10 times as long as those of isoproterenol and sulbutamol and, especially on oral administration, it was much more potent. The bronchodilating effect of C-78 seems to be due to excitation of the adrenergic beta-receptor, and was antagonized by propranolol. The positive chronotropic and inotropic effects of C-78 on an isolated atrial preparation were less than 1/1000 as potent as those of isoproterenol. C-78 also decreased the tone of smooth muscle, such as the uterus, but its affinity for the bronchial muscle is much higher than for the uterus. C-78 showed strong anti-anaphylactic action and strongly promoted the tracheal ciliary movement. Anitussive effect was also demonstrated, though this was inferior to that of codeine, however, there was no influence on bronchosecretion.

Acetylcholine↗
PubMed1978

Antimutagenic effects of 2(3)-tert-butyl-4-hydroxyanisole and of antimicrobial agents.

Administration of the antioxidants 2(3)-tert-butyl-4-hydroxyanisole (BHA) and ethoxyquin (1,2-dihydro-6-ethoxy-2,2,4-trimethylquinoline) with the diet resulted in a marked decrease in the levels of mutagens present in mice treated with benzo(a)pyrene. This was reflected in the results of the host-mediated assay and determinations of the mutagenic activities of the urine, with the use of the sensitive tester strains TA100 and TA98 of Salmonella typhimurium his- developed by Ames and coworkers. Treatment with BHA was effective also in reducing the mutagenic activities in vivo of hycanthone, three other antischistosomal compounds, metronidazole, diazepam, and mebendazole. These effects were accompanied by increases in the thiol levels of some tissues. The production of mutagenic metabolites of two other antischistosomal drugs, 4-isothiocyano-4'-nitrodiphenylamine and oxamniquine, was not reduced by BHA treatment. However, such reductions in mutagenicity could be achieved by the administration of enteric antibacterial agents, implicating the role of intestinal microorganisms in the mutagenic activation of certain chemical agents. Combined treatment of mice with BHA and enteric antimicrobial agents reduced the levels of mutagens derived from metronidazole by more than 90%, and the combined treatments were more effective than was either treatment alone.

Animals↗
PubMed1979

[Synthesis of the fragments A1-,, A9-15 and A16-21 of ovine insulin A chain using the S-tert-butylmercapto residue for thiol protection (author's transl)].

The following paper describes the synthesis of the fragments A1-8, A9-15 and A16-21 of the ovine insulin A chain using the S-tert-butylmercapto residue for thiol protection. The synthesized fragments, which showed a good solubility in organic solvents, were partially deprotected with trifluoracetic acid and converted to the corresponding S-sulfonates quantitatively by oxidative sulfitolyses at pH 7.6.

Animals↗
PubMed1977

Pharmacological studies of o-chloro-alpha-[(tert.-butylamino)methyl]benzylalcohol hydrochloride (C-78), a new bronchodilator. III. Actions on the nervous systems and miscellaneous organs.

Pharmacological effects of o-chloro-alpha-[(tert.-butylamino)methyl]benzylalcohol hydrochloride (C-78) on the nervous systems and miscellaneous organs were studied. 1. Through a low dosage of C-78 had little influence on the central nervous system, a high dosage of C-78 had a little slow-waving effect on the spontaneous EEG in rabbits, inhibitory action of the convulsion caused by pentetrazol or electroshock in mice and anti-pyrogenic action in rabbits. C-78 also dose-dependently inhibited the increase of motility caused by amphetamine in mice. 2. Only high concentrations of C78 had a local anesthetic action on the cornea and the skin of the back in guinea pigs. 3. C-78 significantly increased non-esterified fatty acids (NEFA) and glucose contents of blood in rabbits, but these actions were inhibited by propranolol. Another, high dosage of C-78 had anti-ulcer and anti-inflammatory action. From the results of the previous experiments and this study, it was concluded that C-78 is a new beta 2-receptor stimulating drug where beta 2-receptor selectivity is greater than that of isoproterenol, salbutamol and clorprenaline.

Analgesics↗
PubMed1979

The inotropic and chronotropic responses of isolated canine atrium to 5-(3-tert.-butylamino-2-hydroxy)propoxy-3,4-dihydrocarbostyril hydrochloride (carteolol).

Direct effects of 5-(3-tert.-butylamino-2-hydroxy) propoxy-3,4-dihydrocarbostyril hydrochloride (carteolol) on chronotropic and inotropic activity were investigated in seventeen isolated atrium preparations which were suspended in a bath and perfused with arterial blood from the heparinized donor dog. Carteolol has little adrenergic beta-receptor stimulating effect in doses which block prominent positive chronotropic and inotropic effects of norepinephrine. At relatively larger doses, however, carteolol produced a long-lasting positive chronotrophic and inotropic effect. At extremely larger doses, carteolol produced a negative inotropic effect with little or slight negative chronotropic effect. In propranolol-treated preparations, carteolol induced less positive effects. Propranolol-induced negative chronotropic and inotropic effects were significantly reduced by treatment with carteolol. From these results, carteolol has not only potent beta-adrenoceptor blocking property but also sympathomimetic activity, and different beta 1-type cardiac adrenergic receptors may probably be suggested.

Animals↗