Biomedical subjects

P Schenone

Publications and source records attributed to P Schenone.

At least 55 records · Page 3Linked to original sources

PubMed1990

3,5-Diphenyl-1H-pyrazole derivatives. VII--Esters, 2-dialkylaminoethyl ethers and N-substituted carbamates of 1-(2-hydroxy-3-phenoxypropyl)-3,5-diphenyl-1H-pyrazole with depressant and platelet antiaggregating activities.

The syntheses of 1-(2-hydroxy-3-phenoxypropyl)-3,5-diphenyl-1H-pyrazole 2 by reaction of 1-hydrazino-3-phenoxy-2-propranolol with dibenzoylmethane, of esters 3 and 2-dialkylaminoethyl ethers 4 starting from 2 as sodium salt and acyl chlorides or 2-chloroethyldialkylamines, respectively, as well as of N-aryl carbamates 5 by reaction of 2 with aryl isocyanates, are described. Some of the above compounds showed a considerable sedative effect in mice and a remarkable platelet antiaggregating activity in vitro, as well as moderate local anesthetic, analgesic and antiinflammatory activities in mice and rats.

Anesthetics, Local↗

PubMed1990

2H-[1]benzothiepino [5,4-b]pyran derivatives with local anesthetic and antiarrhythmic activities.

The synthesis of some N,N-disubstituted 4-amino-5,6-dihydro-3-phenyl-2H-[1]benzothiepino [5,4-b]pyran-2-ones by reaction of phenylchloroketene with a series of N,N-disubstituted (E)-4-aminomethylene-3,4-dihydro-1-benzothiepin-5(2H)-ones, followed by dehydrochlorination of the primary adducts with DBN, is described. The 4-methylphenylamino derivative showed a local anesthetic activity in mice superior to that of lidocaine and the 4-morpholino derivative showed an antiarrhythmic activity in rats comparable to that of quinidine.

Anesthetics, Local↗

PubMed1990

2H,5H-[1]benzothiopyrano [4,3-b]pyran derivatives with platelet antiaggregating activity.

The synthesis of some N,N-disubstituted 4-amino-3-phenyl-2H,5H-[1]benzothiopyrano [4,3-b]pyran-2-ones by reaction of phenylchloroketene with a series of N,N-disubstituted 3-aminomethylene-2,3-dihydro-4H-1-benzothiopyran-4-ones, followed by dehydrochlorination of the primary adducts with DBN, is described. Some of these compounds showed a strong platelet antiaggregating activity in vitro, superior to that of acetylsalicylic acid.

Anesthetics, Local↗

PubMed1990

4-Substituted 1-phenyl-1H-indazoles with analgesic, antiinflammatory, antipyretic and local anesthetic activities.

The synthesis of amides 3 and 4 starting from (1-phenyl-1H-indazol-4-yl)acetic and [(1-phenyl-1H-indazol-4-yl)oxy]acetic acids, respectively, as well as of 2-(1-phenyl-1H-indazol-4-yl)ethanamines 5 starting from 3, is described. Moreover, a number of 2-[(1-phenyl-1H-indazol-4-yl)oxy]ethanamines 7 and 3-[(1-phenyl-1H-indazol-4-yl)oxy]propanamines 8 were prepared starting from 1-phenyl-1H-indazol-4-ol. Some compounds 3, 4 and 7 showed an appreciable analgesic activity in mice, whereas compounds 4 were moderately active as antiinflammatory agents in rats. Some compounds 3, 4, 5, 7 and 8 showed also local anesthetic and a weak antipyretic activity in mice and rats, respectively.

Anesthetics, Local↗

PubMed1989

Amides of 1,3,3-trimethyl-n-[(2-pyridyl)methyl]-2-oxabicyclo [2.2.2]octan-6-amine with depressant and antiarrhythmic activities.

The synthesis of 1,3,3-trimethyl-N-[(2-pyridyl)methyl]-2- oxabicyclo [2.2.2]octan-6-amine (II) (exo, endo mixture) starting from 1,3,3-trimethyl-N-nitro-2-oxabicyclo [2.2.2]octan-6-imine (I), as well as of a series of amides (III) derived from the above amine, is described. Some compounds (III) showed remarkable depressant and antiarrhythmic activities in rats and mice, respectively, whereas the clofibric acid amide (III e) showed an appreciable hypolipidemic activity in rats. Moreover, the above compounds usually exhibited a moderate infiltration anesthesia in mice, as well as a weak hypotensive and bradycardic activity in rats.

Amides↗

PubMed1988

3,5-Diphenyl-1H-pyrazole derivatives. I--Esters and N-substituted carbamates of 1-(2-hydroxyethyl)-3,5-diphenyl-1H-pyrazole and its 4-bromo derivative with depressant, antiarrhythmic, analgesic and other activities.

The synthesis of 1-(2-hydroxyethyl)-3,5-diphenyl-1H-pyrazole (II) and its 4-bromo derivative (III) starting from chalcone epoxide, as well as of a series of esters and N-substituted carbamates derived from (II) and (III), is described. Some of these compounds showed remarkable depressant, antiarrhythmic and analgesic activities in mice and rats. Moreover, the above compounds usually exhibited moderate hypotensive, bradycardic and antiinflammatory activities in rats, infiltration anesthesia and hypoglycemic activity in mice, as well as a weak platelet antiaggregating activity in vitro.

Analgesics↗

PubMed1988

Synthesis and photobiological activity of new N,N-disubstituted 4-amino-3-chloroangelicins.

The synthesis of a series of new N,N-disubstituted 4-amino-3-chloroangelicins (4-amino-3-chloro-2H-furo[2,3-h]-1-benzopyran-2-ones) starting from N,N-disubstituted (E)-5-aminomethylene-6,7-dihydrobenzo[b]furan-4(5H)-ones is described. Their capacity of inhibiting DNA synthesis in Ehrlich ascites tumor cells by U.V.-A light irradiation as well as their phototoxic activity on guinea-pig skin have been studied and the data computed by probit analysis; the results are discussed in the light of the modifications introduced in the molecular structure.

Animals↗

PubMed1988

3,5-Diphenyl-1H-pyrazole derivatives. II--N-substituted 1-(2-aminoethyl)-3,5-diphenyl-1H-pyrazoles and their 4-bromo derivatives with analgesic and other activities.

The synthesis of N-substituted 1-(2-aminoethyl)-3,5-diphenyl-1H-pyrazoles and their 4-bromo derivatives (V) by reaction of primary and secondary amines with the tosylates of 1-(2-hydroxyethyl)-3,5-diphenyl-1H-pyrazole and its 4-bromo derivative is described. Some of compounds (V) showed a remarkable analgesic activity in mice. Moreover, the above compounds usually exhibited moderate hypotensive, bradycardiac and antiinflammatory activities in rats, infiltration anesthesia in mice, as well as a weak platelet antiaggregating activity in vitro.

Analgesics↗

PubMed1988

N,N-disubstituted 4-amino-(6-methoxy)-3-phenyl-2H-naphtho [1,2-b]pyran-2-ones with antiarrhythmic, platelet antiaggregating and local anesthetic activities.

The synthesis of title compounds (VI) by 1,4-cycloaddition of phenylchloroketene to N,N-disubstituted (E)-2-aminomethylene-3,4-dihydro-(6-methoxy)-1(2H)naphthalenones, followed by dehydrochlorination with DBN and dehydrogenation with Pd/C of the resulting cycloadducts, is described. Some compounds (VI) showed antiarrhythmic activity in rats higher or like that of quinidine and platelet antiaggregating activity in vitro like that of acetylsalycilic acid, as well as moderate infiltration anesthesia in mice and weak hypotensive, bradicardic and antiinflammatory activities in rats.

Anesthetics, Local↗

PubMed1988

Aminoethers of 1,3,3-trimethyl-5-(phenylmethylene)-2-oxabicyclo[2.2.2]octan-6-h ydroxy imine with antiarrhythmic activity.

The synthesis of beta-dialkylaminoethyl ethers (III a-f) and gamma-dialkylaminopropyl ethers (III g-l) starting from 1,3,3-trimethyl-5-(phenylmethylene)-2-oxabicyclo[2.2.2]octan-6- hydroxyimine (II) is described. beta-Diisopropylaminoethyl ether (III b) and gamma-piperidinopropyl ether (III i) showed an antiarrhythmic activity in rats similar to that of quinidine. Moreover, a number of ethers (III) showed weak hypotensive and bradycardic activity in rats and moderate infiltration anesthesia in mice.

Anesthetics, Local↗

PubMed1988

Acetic acids bearing the 1-phenyl-1H-indazole nucleus with analgesic and antiinflammatory activity.

The synthesis of [(1-phenyl-1H-indazol-4-yl)oxy]acetic acid (IV), (1-phenyl-1H-indazol-4-yl)acetic acid (IX) and (1,5,6,7)tetrahydro-1-phenyl-4H-indazol-4-iminooxy)acetic acid (XIII) starting from 1,5,6,7-tetrahydro-1-phenyl-4H-indazol-4-one (I) is described. These compounds showed a good antiinflammatory activity in rats, and an analgesic activity in mice similar or comparable to that of indomethacin.

Acetates↗

PubMed1988

Ureas and amides derived from N-(5-norbornen-2-ylmethyl) bornan-2-exo-amine with antiarrhythmic and other activities.

The synthesis of title compounds by reaction of camphor nitrimine with (5-norbornen-2-yl)methylamine, followed by NaBH4 reduction of the resulting imine to N-substituted isobornylamine (IV) and reaction of (IV) with alkyl and aryl isocyanates or acyl chlorides, is described. Some ureas and amides are endowed with antiarrhythmic activity in rats superior or comparable to that of quinidine, whereas benzamide (V o) showed an appreciable hypoglycemic activity in mice. Moreover, compounds (V) exhibited in general moderate hypotensive, bradycardic and antiinflammatory activities in rats, as well as a weak infiltration anesthesia in mice.

Amides↗

PubMed1987

1-substituted 5-dialkylaminomethyl-1,5,6,7-tetrahydroindazol-4-ones with antiinflammatory and analgesic activity.

The synthesis of 1-phenyl- and 1-methyl-5-dialkylamino-methyl-1,5,6,7-tetrahydroindazol-4-ones (III) and (IV) by Mannich reaction of the corresponding 1-substituted 1,5,6,7-tetrahydroindazol-4-ones (I) and (II) is described. Some compounds (III) showed a good antiinflammatory and analgesic activity in rats and mice, respectively. Infiltration anesthesia in mice and antiacetylcholine activity in vitro are also reported.

Acetylcholine↗

PubMed1987

Isonicotinates, nicotinates and clofibrates of N-methyl-N-(2-hydroxyethyl or 3-hydroxypropyl)--1,3,3-trimethylbicyclo [2.2.1]heptan-2-endo-amine with hypocholesterolemic and hypolipidemic activity.

The synthesis of isonicotinic, nicotinic and clofibric esters (III a, b, c) and (IV a, b, c) starting from N-methyl-N-(2-hydroxyethyl or 3-hydroxypropyl)-1,3,3-trimethylbicyclo [2.2.1] heptan-2-endo-amine is described. In general these esters showed a normolipemic activity in rats; in particular, the isonicotinic ester (IV a) showed a hypocholesterolemic activity higher than that of clofibric acid.

Animals↗

PubMed1987

N'-acyl-N,N-(1,3,3-trimethylbicyclo [2.2.1]hept-2-ylidene)benzamidines with hypotensive activity.

The reaction of fenchone nitrimine (I) with benzamidine gave in good yield N,N-(1,3,3-trimethylbicyclo [2.2.1]hept-2-ylidene)benzamidine (II), which by acylation afforded N'-acyl-N,N-(1,3,3-trimethylbicyclo[2.2.1]hept-2-ylidene)benzam idines (III a-f) in excellent yields. Compounds (III) showed a moderate hypotensive activity in rats and a weak local anesthetic activity by infiltration in mice. Effects on heart rate and antiarrhythmic activity in rats are also reported.

Amidines↗

PubMed1987

N-acyl-N'-methyl-N-(1,3,3-trimethylbicyclo[2.2.1]hept-2-yl) benzamidines with hypotensive activity.

Lithium aluminium hydride reduction of N-phenoxycarbonyl-N,N-(1,3,3-trimethylbicyclo[2.2.1]-hept-2- yl)benzamidine (II), which afforded the N-acyl derivatives (III a-f) in good yields. Compounds (II) and (III) showed a moderate hypotensive activity in rats. Local anesthetic activity by infiltration in mice, effects on heart rate and antiarrhythmic activity in rats are also reported.

Amidines↗

PubMed1987

Esters of N-(2-hydroxy-1,1-dimethylethyl)-1,7,7-trimethylbicyclo[2.2.1] heptan-2-exo-amine with hypotensive activity.

The synthesis of title compounds by reaction of camphor nitrimine with 2-amino-2-methylpropanol, followed by NaBH4 reduction of the resulting imine to the aminoalcohol (III) and esterification of (III) with aliphatic and aromatic acyl chlorides in pyridine solution, is described. Phenyl carbamate (V) was also prepared by reaction of (III) with phenyl isocyanate. Some esters and (V) showed a moderate hypotensive activity in rats. Effects on heart rate and antiarrhythmic activity in rats, as well as infiltration anesthesia in mice, are also reported.

Amines↗

PubMed1987

alpha-(1H-imidazol-1-ylmethylene)ketones with antimycotic activity.

A series of title compounds were synthesized starting from heterocyclic alpha-hydroxymethyleneketones and 1,1'-carbonyldiimidazole and tested against gram-positive and gram-negative bacteria, as well as fungi. 7,8-Dihydro-6-(1H-imidazol-1-ylmethylene)-2-phenylquinazolin -5(6H)-one showed a remarkable activity against Candida krusei.

Antifungal Agents↗