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Biomedical subjects

A Carotti

Publications and source records attributed to A Carotti.

At least 127 records · Page 7Linked to original sources
PubMed1985

Quantitative structure-activity relationships of cysteine hydrolases. Ficin hydrolysis of X-phenyl-N-methanesulfonyl glycinates.

The hydrolysis of ficin of 33 X-Phenyl-N-methanesulfonyl glycinates has been studied. The resulting Km-values have been used to derive a quantitative structure-activity relationship (QSAR). The QSAR for ficin is compared with QSAR for other cysteine hydrolases. The comparisons show that although there are specific differences, overall the reaction mechanisms are very similar.

Benzene Derivatives↗
PubMed1985

Variant Philadelphia translocation in an immunologically and clinically typical case of chronic myeloid leukaemia.

Cytogenetic analysis of bone marrow from a chronic myeloid leukemia patient in chronic phase revealed a classical Philadelphia chromosome from a complex translocation t(2;9;22). The break points on 9 and 22 were, apparently, the same as for the standard translocation (9;22). However, whereas the terminal band of 9 (9q34) was translocated in the usual site, that is on 22q-, the tract deleted from 22 was present on band p13 of chromosome 2. The finding of this rare 22 translocation in classical CML would seem to support the hypothesis that the crucial event in the pathogenesis of CML is the translocation of band 9q34, that contains the c-abl oncogene, onto the Ph' chromosome, rather than the translocation of the tract deleted from 22 to some other chromosome site.

Aged↗
PubMed1984

[Connectivitis-like pathologies. Incomplete or initial connectivitis?].

Several cases of pathology comparable to connective tissue diseases, but not belonging to any of the established and well known classes are presented. Clinical and laboratory data were not always sufficiently indicative of connectivitis and in these cases the initial diagnostic doubt was never resolved even after months or years of follow-up. The advisability of early immunological therapy despite such doubts is then discussed.

Adrenal Cortex Hormones↗
PubMed1984

Papain hydrolysis of X-phenyl-N-methanesulfonyl glycinates: a quantitative structure-activity relationship and molecular graphics analysis.

The hydrolysis of 32 X-phenyl-N-methanesulfonyl glycinates by papain was investigated. It was found that the variation in the Michaelis constants could be rationalized by the following correlation equation: log 1/Km = 0.61 pi '3 + 0.46 MR4 + 0.55 sigma + 2.00 with a correlation coefficient of 0.945. In this expression, pi '3 is the hydrophobic constant for the more lipophilic of the two possible meta substituents, MR4 is the molar refractivity of 4-substituents, and sigma is the Hammett constant summed for all substituents. Using this equation, we designed, synthesized, and successfully predicted Km for a new congener intended to maximize binding (1/Km). The interactions involved in enzyme-substrate binding, as characterized by the correlation equation, are interpreted using a computer-constructed color three-dimensional-graphics molecular model of the enzyme active site. The nonenzymatic hydrolysis (both acid and basic) of phenyl hippurates yield rate constants which are well correlated by Hammett equations; however, log k for both acid and alkaline hydrolysis are not linearly related to log 1/Km or log kcat/Km.

Binding Sites↗
PubMed1984

Actinidin hydrolysis of substituted-phenyl hippurates: a quantitative structure-activity relationship and graphics comparison with hydrolysis by papain.

The hydrolysis of 29 phenyl hippurates (XPhOCOCH2NHC(=O)C6H5) by the cysteine protease actinidin has been studied and a quantitative structure-activity relationship (QSAR) has been formulated: log 1/Km = 0.74 sigma + 0.50 pi'3 + 0.24MR4 + 2.90. In this expression Km is the Michaelis constant, sigma is the Hammett constant, pi'3 is the hydrophobic parameter for the more hydrophobic of the two meta substituents, and MR4 is the molar refractivity of para substituents. The QSAR for actinidin is compared with a similar one obtained for another cysteine plant protease papain. A color stereo computer graphics model constructed from the X-ray crystallographic coordinates of actinidin is compared with those of our previously reported models for papain.

Cysteine Endopeptidases↗
PubMed1984

Structure-activity relationship of the ficin hydrolysis of phenyl hippurates. Comparison with papain, actinidin, and bromelain.

A study of the hydrolysis of 30 substituted-phenyl hippurates by the enzyme ficin has been made. From the results the following quantitative structure--activity relationship (QSAR) has been derived: log 1/Km = 0.79 pi'3 + 0.58 sigma + 0.28 MR4,5 + 3.70. In this expression Km is the Michaelis constant, pi'3 refers to the more hydrophobic of the two meta substituents, and MR4,5 is the molar refractivity of substituents in the 4- and 5-positions of the phenyl ring. This QSAR is compared with those from papain, actinidin, bromelain B, and bromelain D.

Bromelains↗
PubMed1982

Antihypertensive activity of once daily metoprolol alone and with chlorthalidone and comparison with a twice daily regimen.

In a multicentre, double-blind (DB), within-patient study, the antihypertensive effectiveness and tolerability of two oral administration schedules of metoprolol (M) 100 mg b.i.d. versus 200 mg once daily (o.d.), were investigated in 103 outpatients with mild to moderate essential hypertension. The study lasted 14 weeks and was divided into 3 periods: a) a weeks of single-blind (SB) placebo wash-out; b) 4 weeks of SB administration of M 100 mg b.i.d.; at the end of the second week of this period, chlorthalidone (C) 25 mg was added in patients with a recumbent diastolic blood pressure (BP) still greater than 95 mmHg and was continued throughout the following period; and c) DB cross-over administration of M 200 mg/d for 4 weeks on a b.i.d. schedule and 4 weeks on a once daily schedule. In comparison with pretreatment values, heart rate and systolic and diastolic BP were reduced (p less than 0.001) by both M administration schedules; there was no differences between the once and twice daily treatment regimens. During M once daily, betablockade was still maintained over 24 hours or longer, as the heart rate remained significantly lower than the basal value. In 57 patients, C was added at the end of the second week of SB M administration, and a further decrease in BP was observed; again, there was no significant change during once and twice daily M administration. Unwanted effects during M treatment were of minor severity, and the majority occurred when C, too, was added.

Administration, Oral↗
PubMed1981

A fixed combination of oxprenolol slow-release and chlorthalidone once daily in treatment of mild to moderate hypertension.

In a multicenter, single-blind, interpatient study, 103 outpatients with mild to moderate hypertension were given, after 2 weeks of placebo wash-out, 160 mg oxprenolol slow-release in fixed combination with chlorthalidone (20 mg per tablet) (SROC 160) once daily or conventional oxprenolol (80 mg) in fixed combination with chlorthalidone (10 mg per tablet) (COC 80) twice daily for 8 weeks. Throughout the study 22 of 51 patients on SROC 160 and 24 of 51 on COC 80 received 1 tablet once daily and, respectively, 1 tablet twice daily. The remaining patients of both groups double the corresponding dosage after the first 4 weeks. Systolic and diastolic blood pressure decreased on both treatments without and difference observed between the groups. Diastolic blood pressure normalization was achieved in both groups in the same number of patients (35). Minor side effects occurred on both treatments: only one patient on SROC 160 interrupted the study due to severe dizziness and fatigue. The advantages are discussed as regards patient's compliance with administration of fixed combination SROC 160 once daily in treatment of mild to moderate hypertension.

Adult↗
PubMed1980

[A comparative evaluation of metoprolol and methyldopa in hypertension therapy (author's transl)].

The antihypertensive effect and the tolerability of the cardioselective beta-blocking drug metoprolol, in comparison to methyldopa, were assessed in 119 hypertensive patients (73 WHO stage 1 and 46 WHO stage 2). After 2 weeks of placebo wash-out, the patients were randomly allocated to treatment with either of the two drugs: metoprolol up to 200 mg bid, and methyldopa up to 500 mg bid, for 6 weeks. Periodical clinical, biochemical, haematological, radiological and electrocardiographical measurements were performed. In respect to pre-treatment values, heart rate, both in lying and standing position, was significantly reduced (P less than 0.01) only in the metoprolol group, while systolic and diastolic blood pressures were significantly reduced (P less than 0.01) with both drugs in both positions. Asymptotic regression analysis showed that velocity of blood pressure reduction was comparable with both drugs. In the lying position, the diastolic blood pressure reduction obtained with metoprolol was significantly greater (P less than 0.05) in respect to that obtained with methyldopa. In general, side effects were few and of mild severity: mainly bradycardia in the metoprolol group and dizziness and fatigue in the methyldopa group. After the formal end of the double-blind trial, 36 patients, 14 in the metoprolol group and 22 in the methyldopa group, were treated in open conditions with metoprolol alone; after an average period of 6.5 weeks, diastolic blood pressure was significantly reduced (P less than 0.05) only in the group previously treated with methyldopa. In conclusion, metoprolol is a well tolerated and effective antihypertensive agent, which may be safely used in patients with mild to moderate hypertension.

Adult↗
PubMed1980

Antihypertensive activity of a fixed combination of oxprenolol and chlorthalidone in mild to moderate arterial hypertension.

In a multicentre double-blind study, 92 out-patients with mild to moderate hypertension who had a resting blood pressure greater than or equal to 160/100 mmHg after a two-weeks' placebo wash-out were treated for 6 weeks with a fixed combination of oxprenolol 80 mg + chlorthalidone 10 mg per tablet or chlorthalidone alone (1 tablet = 10 mg). Five patients were drop-outs, 19 out of 44 patients on fixed combination and 7 out of 43 on chlorthalidone were given only 1 tablet b.i.d. throughout the study; the remaining doubled the corresponding dosage after the first 2 weeks. Resting and standing systolic and diastolic blood pressure decreased on both treatments, the reductions being significantly more marked on fixed combination in comparison to chlorthalidone alone (p < 0.01 and p < 0.05). The systolic blood pressure decrease was significantly greater on fixed combination from the first week of treatment (p < 0.05). Normalization of diastolic blood pressure was reached more frequently on fixed combination (73%) than on chlorthalidone (49%) (p < 0.05). Side-effects were recorded in 14 out of 44 patients treated with fixed combination and in 14 out of 43 treated with chlorthalidone. The advantages of treating patients with mild to moderate hypertension with a fixed combination of beta-blocker and diuretics are discussed.

Chlorthalidone↗
PubMed1979

[Atrial arrhythmic disease. Presentation of 16 cases and diagnostic, prophylactic and therapeutic considerations].

The auricle arhythmic illness (exhibition of 16 cases with diagnostic, prophilactic and therapeutic considerations). The Authors make a report on sixteen cases seen in the last four years, after distinguishing between the simple kind (which explicates by BS, BSA, AS) and the complex one, in which can be found bradycardy, tachiarithmy, and asystoly. They also stress its meaning compared with other heart illnesses by a statistic point of view. They stress moreover the radiotelemetric monitoring of every suspicious case and the follow-up of the sinus node work by pacing. The treatment of every case with demand pacemakers is recommended.

Adult↗
PubMed1977

[Theophylline and theobromine derivatives of nitrogen heterocyclic compounds].

7-Theophylline derivatives with 4,6-dihydroxy-5-pyrimidinyl-, 3-oxopiperazinylmethyl- and 4-methyl-3,5-dioxopiperazinylmethyl substituents are described: they can be viewed as structural analogues of a nucleic base pair in the Hoogsteen arrangement; theobromine could be converted into the 1-(3,5-dioxo-4-pyrazolidinyl) derivative, similarly analogous to a base pair in the Watson-Crick arrangement.

Heterocyclic Compounds↗