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Biomedical subjects

G Falcone

Publications and source records attributed to G Falcone.

At least 145 records · Page 8Linked to original sources

Synthesis of N-[4-(propyl)cyclohexyl]-amides with anti-inflammatory and analgesic activities.

Seventeen (un)substituted N-[4-(propyl)cyclohexyl]-amides (6a-h, 7a-h and 8) were synthesized and tested as anti-inflammatory and analgesic agents. The substituents on the aromatic ring were chosen in order to study the influence of electron-withdrawing or electron-donating residues, that change the electronic density on the aromatic moiety. The pharmacological results allow drawing some preliminary considerations on structure-activity relationships.

Amides↗

O-[2-hydroxy-3-(dialkylamino)propyl]ethers of (+)-1,7,7-trimethyl bicyclo[2.2.1]heptan-2-one oxime (camphor oxime) with analgesic and antiarrhythmic activities.

A novel series of O-[2-hydroxy-3-(dialkylamino)propyl]ethers of (+)-camphor oxime was prepared and tested for its cardiovascular, analgesic and anti-inflammatory properties. No significant anti-inflammatory and hypotensive activities were displayed by any of the compounds, whereas several of them are reasonably active as antiarrhythmic and analgesic agents.

Acetates↗

Preparation of new 5-aroylamino substituted 3-nicotinoyl/isonicotinoyl-1,3,4-thiadiazol-2(3H)-ones with anti-inflammatory activity.

A series of 1,3,4-thiadiazol-2(3H)-ones (2a-j) with a nicotinoyl/isonicotinoyl group in position 3 and an aroylamino substituent in position 5 of the ring was prepared and evaluated for antipyretic and anti-inflammatory activities. All the title compounds and in particular 2e, 2i and 2j exhibited anti-inflammatory activity and were devoid of antipyretic properties.

Analgesics, Non-Narcotic↗

Synthesis and anti-inflammatory activity of esters derived from 5-aryl-1,2-dihydro-2-(2-hydroxyethyl)-3H-1,2,4-triazole-3-thiones.

Some aliphatic and aromatic esters 2a-l were prepared starting from 5-aryl-1,2,4-triazoline-3-thiones bearing a 2-hydroxyethyl chain in position 2. The title compounds were evaluated for antipyretic and anti-inflammatory activities. Nearly all derivatives and in particular 2f, 2h, 2k exhibited antiphlogistic properties but were lacking in antipyretic activity.

Analgesics, Non-Narcotic↗

Synthesis of angelicin heteroanalogues: preliminary photobiological and pharmacological studies.

A series of angelicin heteroanalogues, in which the furan was replaced by thiophene or a 1-substituted pyrazole moiety, was synthesised in order to obtain potential therapeutic agents with antiproliferative and/or other biological activities. In general, the antiproliferative activity of the new thioangelicin, tested in different biological substrates, appeared to be higher than that of the angelicin, the natural parent compound, but lower than that of 8-MOP, the furocoumarin ordinarily used in PUVA therapy and photopheresis. Thioangelicin 6 induced strong inhibition of T2 bacteriophage infectivity and was able to significantly repress the DNA synthesis in Ehrlich ascites cells and the clonal growth in HeLa cells. The pyrazolocoumarins did not show any noticeable effect upon UVA irradiation in all the biological systems considered. All the new angelicin heteroanalogues appeared to be free of the known phototoxicity of furocoumarins on the skin. The pyrazolocoumarins have also been tested as anti-inflammatory, analgesic, antipyretic, local anaesthetic, anti-arrhythmic and platelet anti-aggregating agents by standard procedures. In this class of derivatives, 10a showed good anti-inflammatory and antipyretic properties, while 9a and 11a showed significant local anaesthetic activity.

Animals↗

Antiinflammatory agents: new series of N-substituted amino acids with complex pyrimidine structures endowed with antiphlogistic activity.

A series of N-methyl-N-pyrimidin-2-yl glycines 2a-e, having the pyrimidine ring fused with a cyclohexane [N-methyl-N-(5,6,7,8-tetrahydroquinazolin-2-yl)glycine], cyclohexene [N-methyl-N-(5,6-dihydroquinazolin-2-yl)glycine], 1,2,3,4-tetrahydronaphthalene [N-methyl-N-(5,6-dihydrobenzo[e]quinazolin-2-yl)glycine], benzopyrane [N-methyl-N-(5-phenyl-5H-[1]benzopyrano[4,3-d]pyrimidin-2-yl)glyci ne] and benzothiopyrane [N-methyl-N-(5H-[1]benzothiopyrano[4,3-d]pyrimidin-2-yl)glycine] ring, was prepared and tested for antiinflammatory activity. With the same purpose a number of N-5H-[1]benzopyrano[4,3-d]pyrimidin-2-yl substituted amino acids 3a-e, having a different chain length and branching were also synthesized and tested. All the described products 2 and 3 showed an appreciable antiphlogistic activity, particularly 2b and 2c.

Amino Acids↗

The v-myc oncogene is sufficient to induce growth transformation of chick neuroretina cells.

A number of studies have shown that full transformation of non-established rodent fibroblasts can be efficiently achieved in vitro by the concerted action of two oncogenes belonging to different complementation groups. Extension of the two-genes carcinogenesis model to other differentiated cell types, presumably endowed with different controls of growth, is desirable for a better understanding of questions such as the host cell selectivity of oncogene action. A recent report claimed that cooperation between two oncogenes, v-myc and v-mil, is required to achieve transformation of chicken embryo neuroretina cells, which are characterized by a limited growth capacity in monolayer culture. Here we present evidence that the v-myc oncogene alone is sufficient to induce growth transformation of glial and neuronal precursor cell types from chick neuroretina. We also report that induction of transformation by v-myc is accompanied by faithful preservation of some of the differentiated functions of the chick cells.

Animals↗

[Splenic infarction caused by vascular pedicle torsion].

We report a case of a spleen infarction caused by the vascular pedicle torsion. A 25 year-old-man, heterozygous for HbS, presented with severe abdominal pain especially in the left upper quadrant in front and in the back, fever other symptoms related to acute abdomen. First we excluded most common disease (occlusive one and hematologic one) through conform investigation, then we suspected a spleen problem. So we did further investigation with ultrasonography which showed splenomegaly and the spleen looked twisted with its hilum in contact with previous abdominal wall, moreover (here were are as of decreased signal intensity characteristic of splenic infarction under the capsule and some blood in the Douglas pouch. The patient underwent splenectomy urgently. During the intervention we saw a splenomegaly like the ultrasonography showed, moreover there were a long twisted vascular pedicle and many areas of infarctions, some of which had ruptured causing emoperitoneum. The surgical intervention was successful and the clinical spectrum was solved. The splenic infarction might be clinically silent or to represent a surgical emergency. In front a case of acute abdomen, after exclusion of most common etiology, we underline the importance to suspect a spleen suffering, especially vascular one, when (here was no history of trauma. Considering this fact, a simple not invasive examination like ultrasonography is able to confirm this kind of hypothesis and to give soon information to make the surgical choose.

Adult↗

In vitro fertilization as an out-patient procedure.

A new, non invasive method for IVF/ET is discussed. Twenty infertile patients were involved in an outpatient procedure; less risk for them, because of local anaesthesia and low costs for the clinic are the most remarkable advantages of this procedure. Four normal ongoing pregnancies followed this treatment.

Ambulatory Care↗