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Biomedical subjects

P Schenone

Publications and source records attributed to P Schenone.

At least 37 records · Page 2Linked to original sources
PubMed1992

3,5-Diphenyl-1H-pyrazole derivatives. X. N-substituted 1-(2-aminopropyl)- and 1-(3-amino-2-hydroxypropyl)-3,5-diphenyl-1H-pyrazoles with antiinflammatory and other activities.

The syntheses of 1-(2-hydroxypropyl)-3,5-diphenyl-1H-pyrazole 1 by reaction of 1-hydrazino-2-propanol with dibenzoylmethane and of N-substituted 1-(2-aminopropyl)-3,5-diphenyl-1H-pyrazoles 3 by reaction of primary and secondary amines with the tosylate of 1, as well as of N-substituted 1-(3-amino-2-hydroxypropyl)-3,5-diphenyl-1H-pyrazoles 6 starting from 3,5-diphenyl-1H-pyrazole, are described. Some compounds 3 and 6 showed remarkable antiinflammatory activity in rats, as well as weak analgesic, antipyretic, antiarrhythmic, hypotensive activities in mice and rats and moderate platelet antiaggregating effects in vitro.

Animals↗
PubMed1992

Cyclohepta[b]pyran derivatives with platelet antiaggregating and other activities.

The synthesis of some N,N-disubstituted 4-amino-6,7,8,9-tetrahydro-3-phenylcyclohepta[b]pyran-2(5H)-ones by reaction of phenylchloroketene with a series of N,N-disubstituted 2-aminomethylenecycloheptanones, followed by dehydrochlorination of the primary adducts with DBN, is described. Some compounds showed a platelet antiaggregating activity in vitro superior or comparable to that of acetylsalicylic acid, as well as weak local anesthetic, antiinflammatory and analgesic activities in mice and rats.

Analgesics↗
PubMed1992

1-Phenyl-1H-indazole derivatives with analgesic and anti-inflammatory activities.

The synthesis of 4-hydroxy-1-phenyl-1H-indazole-5-acetic acid 5 4-methoxy-1-phenyl-1H-indazole-5-yl-acetic acid 7 and 5-benzyl-1-phenyl-1H-indazol-4-ol 8, starting from 1,5,6,7-tetrahydro-1-phenyl-4H-indazol-4-one, is described. These compounds showed in mice an analgesic activity superior to that of acetylsalicylic acid and comparable to that of dipyrone; moreover, compound 5 exhibited an appreciable anti-inflammatory activity in rats. Grossbehavioral effects and acute toxicity in mice are also reported.

Analgesics↗
PubMed1992

3,5-Diphenyl-1H-pyrazole derivatives. IX. 2-substituted 4-phenyl-5-(3,5-diphenyl-1H-pyrazol-1-yl) pyrimidines with platelet antiaggregating and other activities.

The synthesis of 2-substituted 4-phenyl-5-(3,5-diphenyl-1H-pyrazol-1-yl)pyrimidines 4 a-e by reaction of 1-(1-dimethylaminomethylene-2-oxo-2-phenylethyl)-3,5-diphenyl-1H-pyrazol e with acetamidine, benzamidine, guanidine, guanidinaecetic acid and creatine, respectively, is described. The alpha-aminoacid derivatives 4 d and 4 e gave a series of amides 7 by coupling with primary or secondary amines in dimethylformamide (DMF) solution in the presence of diphenyl-phosphorylazide (DPPA) and triethylamine. Some compounds 4 and 7 showed a platelet antiaggregating activity in vitro superior or comparable to that of acetyl-salicylic acid, as well as moderate antihypertensive, local anesthetic, analgesic and antiinflammatory activities in rats and mice.

Anesthetics, Local↗
PubMed1991

5-substituted 4-isoxazolecarboxamides with platelet antiaggregating and other activities.

The synthesis of a series of 5-substituted 4-isoxazolecarboxamides by reaction of eight 5-substituted 4-isoxazolecarbonyl chlorides with pyrrolidine, piperidine, morpholine and 4-trifluoromethylaniline is described. Some of these amides showed platelet antiaggregating activity in vitro slightly inferior to that of acetylsalicylic acid, as well weak antiinflammatory, analgesic and antipyretic activities in rats and mice.

Aniline Compounds↗
PubMed1991

omega-Dialkylaminoalkyl esters of 3-dialkylamino-4,7,7-trimethyl-N-phenylbicyclo[2.2.1] hept-2-ene-2-iminothiolic acids with local anesthetic activity.

A series of omega-dialkylaminoalkyl esters of 3-dialkylamino-4,7,7-trimethyl-N-phenylbicyclo[2.2.1]hept-2-ene-2- iminothiolic acids 3 was prepared by reaction of 4,7,7-trimethyl-3-(dimethylamino or 1-piperidinyl)-N-phenylbicyclo[2.2.1] hept-2-ene-2-thiocarboxamides with a number of omega-chloroalkyldialkylamines in the presence of sodium hydride in DMF or benzene solution. Some esters 3 showed an appreciable local anesthetic activity in mice.

Anesthetics, Local↗
PubMed1991

2H-pyrano[3,2-d]-1-benzoxepin derivatives with platelet antiaggregating and other activities.

The synthesis of some N,N-disubstituted 4-amino-5,6-dihydro-3-phenyl-2H-pyrano[3,2-d]-1-benzoxepin-2 -ones by reaction of phenylchloroketene with a series of N,N-disubstituted (E)-4-aminomethylene-3,4-dihydro-1-benzoxepin-5(2H)-ones, followed by dehydrochlorination of the primary adducts with DBN, is described. Some of these compounds showed a platelet antiaggregating activity in vitro slightly superior to that of acetylsalicylic acid, as well as weak local anesthetic and antiinflammatory activities in mice and rats, respectively.

Anesthetics, Local↗
PubMed1991

Benzo[6,7]cyclohepta[1,2-b]pyran derivatives with platelet antiaggregating and other activities.

The synthesis of some N,N-disubstituted 4-amino-6,7-dihydro-3-phenylbenzo[6,7]cyclohepta[1,2-b]pyran-2(5H) -ones by reaction of phenylchloroketene with a series of N,N-disubstituted 6-aminomethylene-6,7,8,9-tetrahydro-5H-benzocyclohepten-5-ones, followed by dehydrochlorination of the primary adducts with DBN, is described. Some compounds showed a platelet antiaggregating activity in vitro superior or comparable to that of acetylsalicylic acid, as well as a weak local anesthetic activity in mice and antiinflammatory activity in rats.

Anesthetics, Local↗
PubMed1991

3,5-Diphenyl-1H-pyrazole derivatives. VIII. N-substituted 3-(4-hydroxy-3,5-diphenyl-1H-pyrazol-1-yl)-propanamides, -propanamines and 2-(4-hydroxy-3,5-diphenyl-1H-pyrazol-1-yl)ethanamines with platelet antiaggregating, hypotensive, antiarrhythmic and other activities.

The synthesis of N,N-disubstituted 3-(4-hydroxy-3,5-diphenyl-1H-pyrazol-1-yl)-propanamides and -propanamines, starting from 4-benzoyloxy-3,5-diphenyl-1H-pyrazole, and of N-substituted 2-(4-hydroxy-3,5-diphenyl-1H-pyrazol-1-yl)ethanamines, starting from 4-acetoxy-1-(2-hydroxyethyl)-3,5-diphenyl-1H-pyrazole, is described. Some of the above compounds showed a platelet antiaggregating activity in vitro superior or comparable to that of acetylsalicylic acid, as well as moderate hypotensive, antiarrhythmic, local anesthetic, sedative and antiinflammatory activities in rats and mice.

Anesthetics↗
PubMed1991

5-[4-(omega-dialkylaminoalkoxy)phenylmethylene] -1,3,3-trimethyl-2-oxabicyclo[2.2.2]octan-6-ones with platelet antiaggregating and other activities.

The synthesis of 5-[4-(omega-dialkylaminoalkoxy)phenylmethylene]- 1,3,3-trimethyl-2-oxabicyclo[2.2.2]octan-6-ones 3 by reaction of some 4-(omega-dialkylaminoalkoxy)benzaldehydes with (+)-1,3,3-trimethyl-2-oxabicyclo [2.2.2]octan-6-one in the presence of sodium methoxide is described. Some aminoethers 3 showed platelet antiaggregating activity in vitro superior or comparable to that of acetylsalicylic acid, as well as weak antiarrhythmic activity in rats and moderate infiltration anesthesia in mice.

Anesthetics, Local↗
PubMed1991

omega-Dialkylaminoalkyl ethers of 5-(arylmethylene)-1,3,3-trimethyl-2- oxabicyclo[2.2.2]octan-6-hydroxyimines with platelet antiaggregating and other activities.

The synthesis of omega-dialkylaminoalkyl ethers 3 by the reaction of some 5-(arylmethylene)-1,3,3-trimethyl-2-oxabicyclo[2.2.2]octan-6- hydroxyimines as sodium salts with the appropriate omega-chloroalkyldialkylamine in DMF solution is described. Some aminoethers 3 showed strong platelet antiaggregating activity in vitro superior to that of acetylsalicylic acid, as well as weak antiarrhythmic activity in rats and moderate infiltration anesthesia in mice.

Anesthetics, Local↗
PubMed1991

2H-pyrano[2,3-f]quinazoline derivatives with platelet antiaggregating and other activities.

The synthesis of some N,N-disubstituted 4-amino-5,6-dihydro-3,8-diphenyl-2H-pyrano[2,3-f]quinazolin- 2-ones by the reaction of phenylchloroketene with a series of N,N-disubstituted (E)-6-aminomethylene-7,8-dihydro-2-phenylquinazolin-5(6H)-ones, followed by dehydrochlorination of the primary adducts with DBN, is described. The methylbenzylamino and diphenylamino derivatives showed platelet antiaggregating activity in vitro superior to that of acetylsalicylic acid. The 1-pyrrolidinyl derivative showed appreciable local anesthetic activity in mice, whereas the whole series of compounds exhibited weak antiinflammatory activity in rats.

Anesthetics, Local↗
PubMed1990

3,5-Diphenyl-1H-pyrazole derivatives. IV--N,N-disubstituted 3-(3,5-diphenyl-1H-pyrazol-1-yl)propanamides and 3-(3,5-diphenyl-1H-pyrazol-1-yl)propanamines with sedative, platelet antiaggregating and local anesthetic activities.

The synthesis of N,N-disubstituted 3-(3,5-diphenyl-1H-pyrazol-1-yl)propanamides 2 a-d and 3-(3,5-diphenyl-1H-pyrazol-1-yl)propanamines 3 a-d starting from 3-(3,5-diphenyl-1H-pyrazol-1-yl)propanoic acid is described. Some of the above compounds showed considerable sedative and local anesthetic activities in mice, as well as a remarkable platelet antiaggregating activity in vitro. Moreover, the above compounds usually exhibited moderate analgesic and antiinflammatory activities in mice and rats, respectively.

Amides↗
PubMed1990

3,5-Diphenyl-1H-pyrazole derivatives. V--1-Acetyl-4-hydroxy-3,5-diphenyl-2-pyrazoline esters, 4-hydroxy-3,5-diphenyl-1H-pyrazole esters and N-substituted 4-(3-amino-2-hydroxy-1-propoxy)-1-methyl-3,5-diphenyl-1H-pyrazoles with antiarrhythmic, sedative and platelet antiaggregating activities.

The synthesis of 1-acetyl-4-hydroxy-3,5-diphenyl-2-pyrazoline esters 3, 4-hydroxy-3,5-diphenyl-1H-pyrazole esters 5 and N-substituted 4-(3-amino-2-hydroxy-1-propoxy)-1-methyl-3,5-diphenyl-1H-pyrazoles 7, starting from 4-hydroxy-3,5-diphenyl-2-pyrazoline is described. Some of compounds 3, 5 and 7 showed a considerable antiarrhythmic and sedative activity in rats and mice, respectively, as well as a remarkable in vitro platelet antiaggregating activity. Moreover, the above compounds usually exhibited moderate antihypertensive, local anesthetic, analgesic and antiinflammatory activities in rats and mice.

Analgesics↗
PubMed1990

1-phenyl-1H-pyrazole derivatives with antiinflammatory, analgesic and antipiretic activities.

Reaction of ethyl or methyl 2-dimethylaminomethylene-3-oxoalkanoates 2 with phenylhydrazine gave the corresponding esters of 5-substituted 1-phenyl-1H-pyrazole-4-carboxylic acids 3 in high yields. Esters 3 were hydrolyzed to the relative carboxylic acids 4, which were converted by heating to 5-substituted 1-phenyl-1H-pyrazoles 5 in excellent yields. Reaction of methyl 5,5-dimethyl-3-dimethylaminomethylene-2,4-dioxohexanoate with phenylhydrazine afforded methyl 1-phenyl-4-pivaloyl-1H-pyrazole-5-carboxylate 8 b, which was converted as above to the corresponding carboxylic acid 10 b and this to 1-phenyl-4-pivaloyl-1H-pyrazole 11 b. Starting from 5-methoxymethyl-1-phenyl-1H-pyrazole, 1-phenyl-1H-pyrazole-5-acetic acid 18 and its alpha-methyl derivative 19 were also synthesized. Compounds 18, 19, 10 b and 11 b showed a strong antiinflammatory activity in rats; the same compounds in general as well as 8 b, showed appreciable analgesic and antipyretic activities in mice and rats, respectively.

Animals↗
PubMed1990

Omega-dialkylaminoalkyl ethers of 3-exo-dialkylamino-(Z)-camphoroximes with antiarrhythmic and local anesthetic activities.

The synthesis of 3-exo-dialkylamino-(Z)-camphoroximes 7 starting from a mixture of 3-endo- and 3-exo-bromocamphornitrimine, hydroxylamine hydrochloride and excess secondary amine (dimethylamine, pyrrolidine, piperidine or morpholine) is described. Compounds 7 gave a series of omega-dialkylaminoalkyl ethers 9, 10 and 11 by reaction of 7 as sodium salts with omega-chloroalkyldialkylamines in DMF solution. Some of compounds 9, 10, 11 showed an appreciable antiarrhythmic and local anesthetic activity in rats and mice, respectively.

Amines↗
PubMed1990

3,5-Diphenyl-1H-pyrazole derivatives. VI--Esters and 2-dialkylaminoethyl ethers of 1(2-hydroxy-2-phenylethyl)-3,5-diphenyl-1H-pyrazole and N,N-disubstituted 1-(2-amino-2-phenylethyl)-3,5-diphenyl-1H-pyrazoles with depressant and platelet antiaggregating activities.

The syntheses of 1-(2-hydroxy-2-phenylethyl)-3,5-diphenyl-1H-pyrazole 1 by reaction of 2-hydrazino-1-phenylethanol with dibenzoylmethane, of esters 2 and 2-dialkylaminoethyl ethers 3 starting from 1 as sodium salt and acyl chlorides or 2-chloroethyldialkylamines, respectively, as well as of N,N-disubstituted 1-(2-amino-2-phenylethyl)-3,5-diphenyl-1H-pyrazoles 5 by reaction of secondary amines with the tosylate of 1, 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↗