PubMed Health⌕ Search

Biomedical subjects

C Pellerano

Publications and source records attributed to C Pellerano.

18 recordsLinked to original sources
PubMed1998

High affinity central benzodiazepine receptor ligands: synthesis and structure-activity relationship studies of a new series of pyrazolo[4,3-c]quinolin-3-ones.

A large series of 2-aryl(heteroaryl)-2,5-dihydropyrazolo[4,3-c]quinolin- 3-(3H)-ones, carrying appropriate substituents at the quinoline and N2-phenyl rings, were prepared and tested as central benzodiazepine receptor ligands. Results from structure-affinity relationship studies were in full agreement with previously proposed pharmacophore models and, in addition, quantitative structure-activity analysis gave further significant insight into the main molecular determinants of high benzodiazepine receptor affinity. The intrinsic activity of some active ligands was also determined and preliminary discussed.

Animals↗
PubMed1994

New 1-[quinolyl(4)]-1,2,3-triazoles: synthesis and evaluation of antiinflammatory and analgesic properties. II.

Several 1-[quinolyl(4)]-1,2,3-triazoles were synthesized by 1,3-dipolar cycloaddition of 4-azidoquinolines with activated methylene compounds. The synthesized compounds, tested for antiinflammatory and analgesic activities, resulted moderately active as antiinflammatories, but with a very interesting analgesic activity, sometimes higher than that of indomethacin, used as reference drug. Some of the triazole derivatives were evaluated also as antimicrobial, but none of them exhibited activity.

Analgesics↗
PubMed1994

New 1-[quinolyl(4)]-1,2,3-triazoles: synthesis and evaluation of antiinflammatory and analgesic properties. I.

The synthesis of new 1-[quinolyl(4)]-1,2,3-triazoles is reported. These have been obtained by reacting 4-azidoquinolines with ethyl p-nitrobenzoylacetate. The synthesized compounds, tested for antiinflammatory and analgesic activities, results moderately active as antiinflammatories, but with a very interesting analgesic activity, sometimes higher than that of indomethacin, used as reference drug.

Analgesics↗
PubMed1993

Pyrazolo[4,3-c]quinolines, synthesis and specific inhibition of benzodiazepine receptor binding. Note II.

Two new series of 2-arylpyrazolo[4,3-c]quinolin-3-ones (6,8-difluoro- and 7,9-dichloro-derivatives) have been synthesized and tested for their ability to displace [3H]flunitrazepam from rat brain membranes. Several compounds possess comparable and sometimes higher affinity for central benzodiazepine receptors than that of diazepam. Some selected compounds were also tested in vivo in the anti-pentylenetetrazol test; some anticonvulsant activity resulted for the 6,8-difluoroderivatives only.

Animals↗
PubMed1993

New quinoline derivatives: synthesis and evaluation for antiinflammatory and analgesic properties--Note II.

The synthesis of new halogenated series of 4-anilinoquinoline-3-carboxylic acids, N-[3-carboxyquinolyl(4)]anthranilic acids and their corresponding esters is reported. These have been obtained by reacting 4-chloro-3-carbethoxy-quinolines with variously substituted anilines and methyl anthranilate respectively. The synthesized compounds were tested for antiinflammatory and analgesic activities; some of them showed a good analgesic activity, sometimes higher than that of indomethacin, used as reference drug.

Aniline Compounds↗
PubMed1992

Quinolinehydrazones as inhibitors of retroviral reverse transcriptase.

The inhibitory activity of a series of 2- and 4-quinolinehydrazones on retroviral reverse transcriptase has been studied on enzymes from M-MuLV, RAV-2, and on a crude lysate of HIV-1, assuming the first two enzymes as potential models of the third. The highest activity is mainly found in lipophilic, water soluble 4-quinolinehydrazones. The inhibitory activity of these compounds decreases in changing from the M-MuLV to the RAV-2, and HIV-1 enzymes, in this order.

Cell Survival↗
PubMed1990

New quinoline derivatives: synthesis and evaluation for antiinflammatory and analgesic properties--Note I.

New 4-anilinoquinoline-3-carboxylic acids, N-[3-carboxyquinolyl (4)]anthranilic acids and their corresponding esters were synthetized by reacting 4-chloro-3-carbethoxyquinolines with substituted anilines and methyl anthranilate respectively. All the compounds were tested for antiinflammatory and analgesic activities. Some derivatives showed a significant antiinflammatory activity comparable to that of indomethacin.

Analgesics↗
PubMed1985

[Quinolylhydrazones with potential antimicrobial and antiparasitic activity].

Quinolinehydrazones prepared by condensation of hydrazinoquinolines with 1-phenyl-2,5-dimethyl-3-pyrrolcarboxaldehyde, 2-chloro-4-dimethylaminobenzaldehyde and 2,6-dichlorobenzaldehyde are described. All compounds were tested in vitro for antimicrobial activity, the results obtained are shown and discussed. The quinolinehydrazones of the 1-phenyl-2,5-dimethyl-3-pyrrolcarboxaldehyde were tested in vivo against Hymenolepis nana and Taenia taeniaeformis and proved inactive.

Aminoquinolines↗
PubMed1985

[Tridentate N-N-N chelating systems as potential antitumor agents].

Tridentate chelating agents, as potential antitumor agents, were prepared by condensing 2-quinolylhydrazines, 2-pyridylhydrazine and 2-benzothiazolylhydrazine with pyridine-2-aldehyde, 6-methylpyridine-2-aldehyde, 2-acetylpyridine and 2-benzoylpyridine. All compounds were tested against Lymphocytic leukemia P388. The active pyridine-2-aldehyde-4-methyl-2-quinolylhydrazone [1-(4'-methyl-2'-quinolyl)-3-(2'-pyridyl)-1,2-diaza-2-propene] (I d) was also tested against other experimental tumors and proved inactive.

Animals↗
PubMed1975

Anticestode quinolinehydrazones.

One hundred and seven 4-quinolinehydrazones were synthesized and tested in vivo against the tapeworm Hymenolepis nana. Twenty-five derivatives showed significant cestocidal activity; structure-activity correlations were performed using Free-Wilson methodology. Two compounds, 2,6-dimethyl-4-[(3-pyridinylmethylene)hydrazino]quinoline and 2,6-dimethyl-4-[2p][(6-methyl)pyridinylmethylene]hydrazino)quinoline, predicted to be maximally active, effected 100% reduction of H. nana in mice at 200 mg/kg, p.o.

Animals↗