Search PubMed⌕ Search

SEARCH · Search PubMed

Results for “SULFAMIDE”

Search indexed PubMed citations on genomics, clinical trials, systematic reviews and public health. Explore titles, authors and supplied subject terms, then open the PubMed record.

Quote a phrase for an exact phrase match. Source license links do not imply unrestricted reuse.

At least 361 records · Page 20Linked to original sources
PubMed2006

Discovery of thiochroman derivatives bearing a carboxy-containing side chain as orally active pure antiestrogens.

In order to search for alternatives to the sulfoxide moiety in the long side chain of pure antiestrogens, several molecules that may interact with water in a fashion similar to ICI164,384 were designed and it was found that compounds with the carboxy, the sulfamide, or the sulfonamide instead of the sulfoxide moiety also functioned as pure antiestrogens. Interestingly, the compound possessing the carboxy moiety showed superior antiestrogen activity compared to ICI182,780 when dosed orally. Results of the pharmacokinetic evaluation indicated that the potent antiestrogen activity at oral dosing attributed to both the improved absorption from the intestinal wall and the metabolic stability of the compound in liver.

Administration, Oral↗
PubMed2006

Carbonic anhydrase inhibitors. Inhibition studies of the human secretory isoform VI with anions.

The unique secretory isozyme of human carbonic anhydrase (hCA, EC 4.2.1.1), hCA VI, has been cloned, expressed, and purified. The kinetic parameters for the CO(2) hydration reaction proved hCA VI to possess a k(cat) of 3.4x10(5)s(-1) and k(cat)/K(M) of 4.9x10(7)M(-1)s(-1) (at pH 7.5 and 20 degrees C). hCA VI has a significant catalytic activity for the physiological reaction, of the same order of magnitude as isoforms CA I or CA IX. A series of anions (such as bicarbonate, chloride, nitrate, etc.) were shown to inhibit the activity of the enzyme, with inhibition constants typically in the range of 0.60-0.90mM. The best hCA VI inhibitors were cyanide, azide, sulfamide, and sulfamate, with inhibition constants in the range of 70-90microM.

Acetazolamide↗
PubMed2006

[Antibiotic susceptibility of Vibrio cholerae 01: evolution after prolonged curative and preventive use during the 2004 cholera epidemics in Douala (Cameroon)].

UNLABELLED: Antibiotics were extensively used, both for curative as for prophylactic purposes, to prevent an explosive spread of the 2004 cholera epidemic in Douala. It was thus necessary to control the antibiotic susceptibility of Vibrio cholerae. OBJECTIVE: The authors had for aim to describe the epidemic, the use of antibiotics, and to follow the susceptibility of V. cholerae. DESIGN: The 14 hospitals in the study all used the same diagnostic, treatment, and preventive protocols, as well as in community practice with home visits. All cases were clinically confirmed and reported. Samples were systematically taken at the beginning and at the end of the epidemic, and randomly during the epidemic. Each identified strain was tested by the disk method for antibiotic susceptibility. RESULTS: Between January and September 2004, 5013 patients and 177,353 people in contact with the patients were given a single dose of doxycycline or amoxicillin for 3 days. Sixty-nine deaths were recorded (lethality 1.37%). One hundred (and) eleven strains of V. cholerae were identified in 187 samples. All of them were resistant to sulfamides and colistin, but susceptible to cyclins, betalactams, and fluoroquinolones, without any modification during the 8 months of follow-up. CONCLUSION: Despite the risk of a massive and prolonged use of antibiotics, strictly prescribed and controlled, no resistance developed in the identified strain. Chemoprophylaxis must follow rigorous protocols and be continuously monitored.

Anti-Bacterial Agents↗
PubMed2000

Multi-residue methodology for pesticide screening in wines.

A multi-residue solid-phase microextraction/gas chromatography/electron-capture detection method for pesticide screening (nine organochlorine, eleven organophosphorous and a tiadiazine insecticides, a benzoylurea acaricide and a halogenated sulfamide fungicide) in wine was developed. Fiber coating, extraction time and temperature, exposure of the fiber to the headspace or to the liquid phase and the ethanol effect on pesticides extraction were the parameters studied. The best results were obtained for a 100 microm poly(dimethylsiloxane) fiber, with 30 min immersion, in a 3 ml sample, at 45 degrees C. Pesticides extraction yield from aqueous spiked solutions was studied, for different ethanol concentrations (9%, 12.5% and 20%, v/v), which are representative of the main types of Portuguese wines. Calibration curves for extracted standards gave linear responses for all the pesticides, except dichlorvos, mevinphos, disulfoton and methidathion. Average detection limits were lower than 5 ppb and no significant interference from the matrix was found in the conditions studied, except for buprofezin.

Chromatography, Gas↗
PubMed2003

Pulmonary nocardiosis in heart transplant recipients: treatment and outcome.

BACKGROUND: Nocardial infections typically affect patients receiving immunosuppressants, occurring early after surgery in 3% to 40% of heart transplant (HTx) recipients. The emergence of antibiotic resistance and occurrence of disease recurrences in AIDS population has engendered controversy about the treatment for immunodepressed HTx patients. METHODS: We present a retrospective study of the diagnosis, treatment and outcome of 560 HTx recipients between 1984 and 2002. RESULTS: Among the five cases of Nocardia infection (0.9%), three cases developed late after HTx (between 3.1 and 11 years follow-up). All patients had pulmonary disease and one in addition had subcutaneous nodules. Microbiological diagnosis required open lung biopsy in one case. All patients were treated primarily with trimethoprim-sulphamethoxazole, but evidence of resistance to sulfonamides led us to change the antimicrobial combination in two cases. Four patients who received one year of antibiogram-guided therapy showed complete healing without recidivism. Three patients died, all due to non-related causes, at follow-ups between 1 and 5 years. In one case a cutaneous recurrence of disease was attributed to noncompliance. CONCLUSIONS: Nocardiosis in current HTx is less common than previously reported. Its incidence seems to be delayed in time with modern immunosuppressants. Given the high incidence of sulfamide resistance, treatment must be guided by antibiotic sensitivity. We believe that maintenance therapy for a whole year is the appropriate option in order to avoid recidivism in this population.

Anti-Bacterial Agents↗
PubMed1997

Genetic predisposition to drug-induced hepatotoxicity.

Drug-induced hepatitis is uncommon and generally unpredictable. Hepatotoxicity may be related to the drug itself, or to chemically reactive metabolites which can bind covalently to hepatic macromolecules and may lead to either idiosyncratic, toxic hepatitis or to immunoallergic hepatitis. There is now evidence indicating that genetic variations in systems of biotransformation or detoxication may modulate either the toxic or sensitizing effects of some drugs. Thus, the genetic deficiency in a particular hepatic cytochrome P 450 isozyme (CYP 2D6) is involved in per-hexiline liver injury. The deficiency in CYP 2C19 might also contribute to Atrium hepatotoxicity. Slow acetylation related to N-acetyltransferase 2 deficiency contributes to sulfonamide hepatitis. The genetic deficiency in glutathione synthetase may increase the susceptibility to several drugs including acetaminophen. A constitutional deficiency in another cell defense mechanism, still not characterized, seems to increase significantly the risk of hepatotoxicity with halothane, phenytoin, carbamazepine, phenobarbital, sulfamides and amineptine.

Acetylation↗
PubMed2001

Structure-activity relationships in platelet-activating factor (PAF). 11-From PAF-antagonism to phospholipase A(2) inhibition: syntheses and structure-activity relationships in 1-arylsulfamido-2-alkylpiperazines.

1-Benzoyl-2-alkyl piperazines are strong inhibitors of Group I and II secreted PLA(2)s. An improvement of their activity was obtained by replacing the amide function by a sulfamide and by introduction of electrodonor substituents on the para position of the benzenesulfonyl moiety. Neither the position on one of the carbon of the piperazine ring nor the absolute configuration of this carbon have an effect on the affinity for one or the other group of PLA(2), but the lipophilicity remains for these series an essential parameter. In addition structure-activity relationships allow new hypothesis on interaction of these piperazine derivatives with the catalytic site of PLA(2)s.

Animals↗
PubMedDate not supplied

[Mefloquine and halofantrine, new therapeutic drugs of malaria].

Mefloquine and halofantrine are quinine-related aminoalcohols recently introduced for the oral treatment (both drugs) and oral chemoprophylaxis (mefloquine) of malaria. Soon after these new drugs were launched the volume of sales testified to the need for alternative treatments in view of the resistance of Plasmodium falciparum to a variety of drugs, including chloroquine, amodiaquine and sulfadoxine-pyrimethamine. Quinine remains effective but it is difficult to handle. Both mefloquine and halofantrine are remarkably effective against the intraerythrocytic pathogenic forms of malaria; they also have a rapid and prolonged action and a low toxicity. Halofantrine is sometimes incompletely absorbed. Neurological side-effects, usually moderate, have been reported with mefloquinone. Partial cross-resistance has been demonstrated within each class of antimalarials: aminoalcohols, amino-4-quinoleins (chloroquine, amodiaquine) and antifolics-antifolinics (sulfamides, pyrimethamine, proguanil), but not between the classes. Further studies are necessary concerning the absorption and tolerability of mefloquine and halofantrine, as well as the regional level of P. falciparum sensitivity to these new drugs.

Animals↗
PubMedDate not supplied

Anaphylaxis to oral furosemide.

Furosemide, one of the most used diuretic drugs, rarely induces type-1 allergic reactions It is included in the non-aromatic sulfonamides but a cross-reactivity mechanism between this group and the sulfonamides antibiotics, has not been clearly demonstrated. A 24-year-old woman, 10 minutes after the intake of one pill of Seguril 40mg experienced oral itching, generalized urticaria, facial angioedema, dyspnea and hypotension. She recovered after the administration of parental adrenaline, methyl-prednisolone and dyphenhydramine. An skin prick test with furosemide (10 mg/ml) was negative. The intradermal skin tests were positive to furosemide (1 %) as well as sulfamethoxazole (0.03 mg/ml), with 10 atopic and non-atopic negative controls. The patient rejected the performance of an oral challenge test with sulfamethoxazole. IgE-mediated reactions to furosemide are infrequent, but it could be the cause of life-threatening reactions. We have reported a case of anaphylaxis after the oral administration of furosemide with a demonstrated hypersensitivity mechanism through the positive intradermal skin test. The previous administration of the drug could probably the mechanism of sensitization, but the positive intradermal test to sulfamethoxazole would open the hypothesis of a cross-reactivity between non-aromatic and antimicrobial sulfonamides. It could be necessary an oral challenge test with furosemide in allergic patients to sulfamides.

Administration, Oral↗
PubMed2001

Neonatal screening for congenital toxoplasmosis in a cohort of 165 women infected during pregnancy and influence of in utero treatment on the results of neonatal tests.

The aim of this study was to determine the performances of methods used for the neonatal diagnosis of congenital toxoplasmosis. We included 165 pregnant women infected during pregnancy over a 10-year period. Fifty-seven cases of congenital toxoplasmosis were demonstrated (34.5%). Neonatal diagnosis gave positive results in 50 cases (88%). Parasites were isolated from placenta or cord blood in 61% of the infected newborns, more frequently from placenta (60%) than from cord blood (43%). This method was the only criterion of infection in 18% of these infected infants. The detection of specific IgM and IgA antibodies performed on 42 sera of infected infants allowed the diagnosis of congenital infection in 34 cases (81%). IgA antibodies were more frequently detected (60%) than specific IgM (50%). Neonatal and prenatal screening were carried out for 143 pregnant women. This combination diagnosed 39 of 40 infected infants (98%). Prenatal diagnosis identified 30 of 40 cases (75%). Nine cases were diagnosed through neonatal screening and one case with the postnatal follow-up. When prenatal diagnosis was positive, pyrimethamine and sulfadoxine were administered to the mothers (25 cases) in addition to spiramycin. Toxoplasma gondii was less frequently isolated in the placenta and the cord blood of these women (32% and 19%, respectively) than in women treated by spiramycin alone (83% and 63%) proving the antiparasitic action of these drugs. In conclusion, neonatal screening combining parasite detection in placenta and immunological methods on cord blood is essential particularly when prenatal diagnosis is negative. Therefore, when this diagnosis is positive, a treatment with pyrimethamine and sulfamide can be started in the first month of life.

Animals↗
PubMed1997

Fractionation of RNA polymerase II transcription factors from HeLa cell nuclear extracts by affinity chromatography on "DNA-like" phosphorylated polystyrene.

It was previously shown that phosphorylated cross-linked polystyrene derivatives specifically interacted with anti-DNA antibodies and anti-phospholipid antibodies present in the sera of systemic lupus erythematosus patients. These resins are potential candidates as stationary phases in affinity chromatography. We wondered whether these biospecific resins might allow the fractionation of DNA binding proteins such as RNA polymerase II transcription factors from HeLa cell nuclear extracts. Indeed, these proteins play a major role in gene regulation in mammalian cells and their purification still requires numerous steps. To study the biospecificity of DNA-like phosphorylated polystyrene derivatives, ethanolamine sulfamide crosslinked polystyrene derivatives were phosphorylated at various rates and HeLa cell nuclear extracts were adsorbed on these resins. Adsorbed proteins were eluted with increasing concentrations of aqueous potassium chloride. Collected fractions were characterized by sodium dodecyl sulfate-polyacrylamide gel electrophoresis (SDS-PAGE) and the biological activities of the eluted transcription factors were tested by in vitro transcription assay. Results showed that the elution of transcription factors depended on the substitution rate in phosphoester groups of the resins. It appears that specific interactions were developed between the polymers and the transcription factors. Moreover, the eluted transcription factors kept their biological activity. These results lead us to propose the purification of RNA polymerase II transcription factors using the phosphorylated polystyrene resins as stationary phases.

Base Sequence↗
PubMed2004

[Toxoplasmosis seroconversion in pregnant women. The differing attitudes in France].

INTRODUCTION: Since 1992 France has been running a toxoplasmosis prevention program based on the serological detection of infections during pregnancy. In the absence of a consensus, the seroconversions discovered are managed in different ways, varying from one centre to another. OBJECTIVE: To describe the habits of the specialised centres in France and propose means to reduce the heterogeneity. METHODS: A survey using a questionnaire mailed to the centres of parasitology in France specialised in the management of toxoplasmosis seroconversion during pregnancy. RESULTS: All the 30 centres surveyed replied. Five of them do not provide recommendations for treatment and were excluded from analysis. The attitudes of the 25 other centres varied greatly with regard to the indications for therapeutic abortion and amniocentesis, treatment protocols with pyrimethamine and sulfamides, as well as in the frequency of sonographical monitoring. CONCLUSION: In the absence of National guidelines, the management of seroconversions discovered during the prenatal prevention of congenital toxoplasmosis program is left to the discretion of the specialised centre. This results in variations from one town to the next. This heterogeneity underlines the lack of knowledge on the most efficient and acceptable means of preventing and treating congenital toxoplasmosis. In order to improve this situation, the French parasitologists have launched a program of consensual meetings aimed at harmonising the treatment protocols and identifying the points that require further studies.

Adult↗
PubMed2003

Carbonic anhydrase inhibitors: inhibition of human and murine mitochondrial isozymes V with anions.

In addition to sulfonamides, metal complexing anions represent the second class of inhibitors of the zinc enzyme carbonic anhydrase (CA, EC 4.2.1.1). The first inhibition study of the mitochondrial isozyme CA V (of murine and human origin) with anions is reported here. Inhibition data of the cytosolic isozymes CA I and CA II as well as the membrane-bound isozyme CA IV with a large number of anionic species such as halides, pseudohalides, bicarbonate, nitrate, hydrosulfide, arsenate, sulfamate, and sulfamidate and so on, are also provided for comparison. Isozyme V has an inhibition profile by anions completely different to those of CA I and IV, but similar to that of hCA II, which may have interesting physiological consequences. Similarly to hCA II, the mitochondrial isozymes show micro-nanomolar affinity for sulfonamides such as sulfanilamide and acetazolamide.

Animals↗
PubMed2002

omega-(Imidazol-4-yl)alkane-1-sulfonamides: a new series of potent histamine H(3) receptor antagonists.

omega-(1H-Imidazol-4-yl)alkane-1-sulfonamides were prepared and found to be potent histamine H(3) receptor antagonists. High receptor affinity and a low difference in the data between the bioassays were achieved with 5-(1H-imidazol-4-yl)pentane-1-sulfonic acid 4-chlorobenzylamide (16). Good in vitro profiles were also obtained for 2-hydroxysulfonamide and vinylsulfonamide analogues. This complements and completes the existing set of imidazole-based sulfonamides and sulfamides.

Animals↗
PubMed2003

Hydroxyurea is a carbonic anhydrase inhibitor.

The interaction of hydroxyurea with the cytosolic isozymes of carbonic anhydrase (CA), hCA I and hCA II has been investigated by means of kinetic and spectroscopic techniques. Hydroxyurea acts as a weak, non-competitive inhibitor of both isozymes, for the 4-nitrophenyl acetate esterase activity, with inhibition constants around 0.1 mM for both isozymes. The spectrum of the adduct of hydroxyurea with Co(II)-hCA II is similar to the spectra of tetrahedral adducts (such as those with sulfamide, acetazolamide or cyanamide), proving a direct interaction of the inhibitor molecule with the metal center of the enzyme, whose geometry remains tetrahedral. Based on the X-ray crystal structure of the adducts of hCA II with ureate and hydroxamate inhibitors, the hypothetical binding of hydroxyurea is proposed to be achieved in deprotonated state, with the nitrogen atom coordinated to Zn(II), and the OH group of the inhibitor making a hydrogen bond with Thr 199. This binding may be exploited for the design of both CA as well as matrix metalloproteinase (MMP) inhibitors, since hydroxyurea is the simplest compound incorporating a hydroxamate functionality in its molecule. Indeed, such inhibitors of the sulfonylated amino acid hydroxamate type have been generated, with potencies in the low nanomolar range for both type of enzymes, CAs and MMPs.

Carbonic Anhydrase Inhibitors↗
PubMed2004

Expanding the scope of C-H amination through catalyst design.

Analysis of the mechanism for Rh-mediated C-H amination has led to the development of a remarkably effective dinuclear Rh catalyst derived from 1,3-benzenedipropionic acid. This unique complex, Rh2(esp)2, is capable of promoting both intra- and intermolecular C-H oxidation reactions, and in all cases is superior to Rh2(O2CtBu)4. For the first time, C-H insertion is described with urea and sulfamide substrates to give 1,2- and 1,3-diamine derivatives, respectively. In addition, intermolecular amination of benzylic and secondary C-H bonds is shown to proceed efficiently even under conditions in which the starting alkane is employed as the limiting reagent.

Journal Article↗
PubMed2005

Copper(II) acetate promoted intramolecular diamination of unactivated olefins.

A concise method for the synthesis of cyclic sulfamides and vicinal diamines is presented. This method is enabled by Cu(OAc)2 and demonstrates a new transformation for this metal. Both five- and six-membered vicinal diamine-containing heterocycles have been synthesized in good to excellent yields, and substrate-based asymmetric induction has been achieved. This is the first reported example of intramolecular diamination of olefins.

Journal Article↗