Pyrazole analogues of prazosin.

A series of analogues of prazosin, in which 1-methyl or 1-phenylpyrazole moieties were substituted for the furan ring, were synthesized and studied for their alpha 1-adrenoceptor antagonist activity. The role of the five member heterocyclic substructures in determining the affinity for the alpha 1-receptor is briefly discussed.

Role of galanin in the regulation of somatotrope and gonadotrope function in young ovulatory women.

The aim of the study was to elucidate the role of the neuropeptide galanin in the regulation of somatotropic and gonadotropic function in normal women. Thirteen normally ovulating (aged 28 to 40 years), non-obese (body mass index, 18.4 to 27.1 kg/m2) women with infertility due to a tubal or male factor were studied. Each woman underwent three tests: (1) bolus intravenous (IV) injection of growth hormone (GH)-releasing hormone (GHRH) (1-29)NH2 1 microgram/kg plus gonadotropin-releasing hormone (GnRH) 100 micrograms at time 0; (2) IV infusion of porcine galanin 500 micrograms in 100 mL saline from -10 minutes; and (3) bolus IV injection of GHRH(1-29)NH2 1 microgram/kg plus GnRH 100 micrograms at time 0 plus IV infusion of porcine galanin 500 micrograms in 100 mL saline from -10 to +30 minutes. All results are expressed as the mean +/- SEM. GH peak after GHRH was 14 +/- 5 micrograms/L; porcine galanin significantly increased serum GH (GH peak, 7.3 +/- 1.2) with respect to baseline levels. No significant differences were observed between either GH peak or GH absolute values after galanin as compared with GHRH alone. Porcine galanin significantly enhanced GH response to GHRH (peak, 31.4 +/- 4.4 micrograms/L) with respect to either GHRH or galanin alone. Luteinizing hormone (LH)/follicle-stimulating hormone (FSH) peaks after GnRH were 16.5 +/- 5.3 and 17.4 +/- 4 IU/L, respectively. Porcine galanin did not cause significant increases in serum LH and FSH levels with respect to baseline.(ABSTRACT TRUNCATED AT 250 WORDS)

Pyrazole sulfanilamides: nitroderivatives of 1-phenyl-3-sulfanilamidopyrazole. Note XVI.

Synthesis and structural characterization of 3 sulfanilamido-1-phenylpyrazoles bearing on 1-phenyl group nitro substituent o-, m-, p-positioned are reported. All derivatives are analysed through 1H and 13C NMR spectroscopy. The MIC values obtained against Escherichia coli are briefly discussed in terms of structure-activity relationship.

Cytotoxic activity of a series of heteroaryl-ONN-azoxy-sulphones and aryl sulphonylhydrazones.

Synthesis of heteroaryl-ONN-azoxysulphones and pyrazolyl-ONN-azoxycyanides was carried out by the action of the appropriate reagents on the corresponding nitroso derivatives. Pyrazolyl-ONN-azoxyamides were obtained by hydrolysis of the corresponding cyanides. Synthesis of the arylsulphonylhydrazones was carried out by reacting R-substituted phenyl-sulphonylhydrazines on the isomers of methylfuroxancarbaldehyde. Cytotoxic activity was assessed on HeLa cells. Some of the compounds tested inhibit the colony-forming ability of the tumor cells at low concentrations.

[Furazan sulfanilamides]. / Sulfanilamidi furazaniche.

Synthesis and antibacterial activity against Escherichia coli of a series of furazan sulfanilamides are reported. A structural activity relationship for these derivatives is also briefly discussed.

[Pyrazole sulfanilamides. XV. Nitroderivatives of 1-phenyl-4-sulfanilamidopyrazole]. / Sulfanilamidi pirazoliche. Nota XV-Nitroderivati dell'1-fenil-4-sulfanilamidopirazolo

The research on the change of antibacterial activity due to the introduction of a nitro group in the benzene nucleus linked at the heterocyclic nitrogen of N-phenylsulfanilamidopyrazoles is continued with the preparation of 1-(2'-nitrophenyl)-4-sulfanilamidopyrazole (IIa: -NO2 in 2'; R=-H), 1-(3'-nitrophenyl)-4-sulfanilamidopyrazole (IIb: -NO2 in 3'; R=-H) and 1-(4'-nitrophenyl)-4-sulfanilamidopyrazole (IIc: -NO2 in 4'; R=-H). By analogy with the results obtained for the derivatives of 4-sulfanilamidopyrazole (I) previously prepared, enhancement of the bacteriostatic activity in vitro against S. aureus and E. coli, have been observed in almost all the cases, especially with 1-(3-nitrophenyl)-4-sulfanilamidopyrazole (IIb).

[Pyrazolic sulfanilamides. XIV. Hydroxyderivatives of 1-phenyl-5-sulfanilamidopyrazole and of 1-phenyl-3-methyl-5-sulfanilamidopyrazole]. / Sulfanilammidi pirazoliche. XIV. Idrossiderivati dell'1-fenil-5-sulfanilammmidopirazolo e dell'1-fenil-3-metil-5-sulfanilammidopirazolo

A report is given of the variations in bacteriostatic activity on introduction of a hydrophilic group, the hydroxyl group (-OH), at positions 2',3' and 4' of the phenyl group linked to the heterocyclic nitrogen os 1-phenyl-5-sulfanilamidopyrazole (I: R = -H) and of 1-phenyl-3-methyl-5-sulfanilamidopyrazole (II: R = -H). The substances prepared for this purpose: 1-(hydroxyphenyl)-5-sulfanilamidopyrazoles (Ia)(Ib))(Ic)(-OH at 2', 3',4') and 1-(hydroxyphenyl)-3-methyl-5-sulfanilamidopyrazoles (IIa)(IIb)(IIc)(-OH at 2',3'4') in vitro tests of bacteriostatic activity against strains of S. aureus and E. coli gave the following results: See journal for results.