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Biomedical subjects

F Nicolò

Publications and source records attributed to F Nicolò.

7 recordsLinked to original sources
PubMed2001

Nickel(II) 2,6-diacetylpyridine bis(isonicotinoylhydrazonate) and bis(benzoylhydrazonate) complexes: structure and antimycobacterial evaluation. Part XI.

The reaction of 2,6-diacetylpyridine (dap) and isonicotinoyl- or benzoylhydrazide leads to bishydrazones H(2)dapin (1a) and H(2)dapb (1b), respectively. The condensation can either take place as a bimolecular kinetic process between the two reactants or as a monomolecular metal-templated synthesis in the presence of nickel(II) ions. In the latter case the reaction products are charged 2,6-diacetylpyridine bis(hydrazone) nickel(II) complexes, which can be easily deprotonated to neutral hydrazonates. Diffractometric analysis of one of these [Ni(dapb)](2) (8b) has shown a binuclear structure with two octahedral nickel(II) ions bridged by two helicoidal dap (bishydrazonates) in a spheroidal structure of C(2V) symmetry. The synthesized complexes 8 are promising as antimycobacterial agents against M. tuberculosis H37Rv. In particular, 8b displays significant activity (MIC=0.025 microg/mL) 10-fold higher than rifampin and equal to isoniazid, while its ligand is ineffective. Compound 8b is also capable of reducing HIV-induced cytopathogenic effect in human T(4 )lymphocytes.

Antitubercular Agents↗
PubMed1998

Synthesis, structure and in vitro anti-human immunodeficiency virus activity of novel 3-methyl-1H,3H-thiazolo[3,4-a]benzimidazoles.

A series of novel 1-aryl-3-methyl-1H,3H-thiazolo[3,4-a]benzimidazoles, TBZ analogues, were synthesized and investigated as anti-human immunodeficiency virus (HIV) agents in order to study the effects of structural modifications on antiviral activity and cytotoxicity. They were proved to inhibit significantly HIV-1 replication in vitro without showing inhibitory activity on HIV-2 or simian immunodeficiency virus. Their potency was influenced by the presence of suitable substituents in the phenyl ring at C-1 as well as by their stereochemical characteristics. In fact, the most active compound of the series was the trans-1-(2,6-difluorophenyl)-3-methyl-1H,3H-thiazolo[3,4- a]benzimidazole, in which the butterfly-like conformation is stabilized by two intramolecular hydrogen bonds between the fluorine atoms and H-1 and H-3. This was made possible by the trans arrangement of C-1 and C-3 substituents, as shown by X-ray and NMR analysis.

Anti-HIV Agents↗
PubMed1997

Anti-HIV agents. V. Synthesis, structure and in vitro anti-HIV activity of novel 1H,3H-naphtho[2',3':4,5]imidazo[1,2-c]thiazoles.

A series of 1H,3H-naphtho[2',3':4,5]imidazo[1,2-c]thiazoles, TBZ analogues, was prepared in order to explore the influence on anti-HIV activity of the spatial requirements of the hydrophobic moiety fused to imidazothiazole system. In spite of a butterfly-like conformation evidenced by X-ray analysis of compound 4g, the results of in vitro screening suggest that the replacement of the benzene fused ring by the naphthyl moiety negatively influences the activity of analogous thiazolobenzimidazole derivatives, some of which are potent non-nucleoside HIV-1 RT inhibitors.

Anti-HIV Agents↗
PubMed1985

Influence of blood temperature on vascular stability during hemodialysis and isolated ultrafiltration.

We tested the hypothesis that differing temperature (T) changes in extracorporeal blood circuit might partly account for the difference in vascular stability (VS) between isolated ultrafiltration (UF) and simultaneous UF-hemodialysis (HD). The study was carried out in 6 patients who presented frequent episodes of symptomatic hypotension during the routine dialytic sessions. During simultaneous UF-HD with dialysate T set at 37.5 degrees C (standard HD), blood reentered the patients with a T of about 2 degrees C higher, whereas during isolated UF (standard UF) 2 degrees C lower, than at its exit. These extracorporeal blood T changes were reciprocated by warming the venous line in isolated UF (warm UF) and by setting the dialysate at 34.5 degrees C in simultaneous UF-HD (cold HD). During warm UF mean arterial pressure (MAP) fell and heart rate (HR) increased nearly as much as during standard HD. Vice versa, during cold HD MAP and HR remained nearly as stable as during standard UF. It is concluded that the T changes in blood flowing through the extracorporeal circuit largely account for the differing VS between isolated UF and simultaneous UF-HD.

Adult↗
PubMed1983

Blood temperature and cardiovascular stability in hemofiltration.

Temperature (T) changes in the blood flowing through the extracorporeal circuit markedly affect cardiovascular tolerance to fluid removal during either hemodialysis (HD) and isolated ultrafiltration. In this study we investigated the effect of blood T changes during postdilutional hemofiltration (HF). To this purpose we compared the changes in mean arterial pressure (MAP) and heart rate (HR) during HF and HD carried out at equivalent T of blood in the venous segment of the extracorporeal circuit. Results show that HF entails some heat loss from blood flowing in the extracorporeal circuit; if heat loss is made similar, HD affords nearly as much blood pressure protection as HF does. On the other hand at equivalent heat gain, HF causes nearly as much hypotension as HD does. We conclude that blood T changes in the extracorporeal circuit affect vascular stability (VS) even in HF. The marginal benefit of HF over HD, still observed at equalized T changes, remains to be elucidated.

Blood↗