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Biomedical subjects

L Raffa

Publications and source records attributed to L Raffa.

At least 19 recordsLinked to original sources
PubMed1989

Heteroarylalkanoic acids with possible antiinflammatoric activities. Part 6: 3-(4H-1,2,4-benzothiadiazine-1,1-dioxide-3-yl-thio)-propanoic acid derivatives.

A series of 3-(4H-1,2,4-benzothiadiazine-1,1-dioxide-3-yl-thio)-propanoic acids was synthesized in order to study their possible antiinflammatory in comparison with the corresponding lower homologues and isosters previously studied. Most of the compounds proved effective against carrageenan-induced plantar oedema. The possible influence of some chemico-physical parameters on the occurrence of this biological activity was investigated.

Animals↗
PubMed1989

Heteroarylalkanoic acid with possible antiinflammatory activities. Note VII.

A series of 3-(4H-1,2,4-benzothiadiazine-1,1-dioxide-3-ylamino)-propanoic acids was synthesized in order to study their possible antiinflammatory activity and to compare it with the corresponding homologous or isoster series previously studied. Of particular interest is parent compound 1, which is unsubstituted in the benzenoid moiety and exerts a very marked inhibitory effect on carrageenan-induced plantar oedema greater than that observed for any of the terms of the other series hitherto studied. The possible influence of some chemico-physical parameters on the occurrence of this antiinflammatory activity is investigated.

Animals↗
PubMed1988

Cardiovascular activity of 1,2,4-benzothiadiazine-1,1-dioxide derivatives. Part 10(3): Dialkylamino-, pyrrolidyl- and morpholyl-alkyl-derivatives of 3-amino-1,2,4-benzothiadiazine-1,1-dioxide, 7- or 5,7-halogen substituted.

A series of dialkylamino, pyrrolidyl and morpholyl-alkyl-derivatives of 3-amino-1,2,4-benzothiadiazine-1,1-dioxide, 7- or 5,7-halogen substituted in the benzenoid moiety, was prepared and their cardiovascular activity studied. Most of the substances in question were capable of inducing a significant decrease in mean arterial blood pressure; some of them tended to increase pulse pressure or to cause bradycardia, an effect which was noted particularly in the case of compound 10 which reduced heart-rate by 85%. The structure/activity relationship of these substances, of the 6- and 6,7-halogen substituted isomers and of their corresponding non-substituted progenitors is examined.

Animals↗
PubMed1983

[Cardiovascular action of 1,2,4-benzothiadiazine-1,1-dioxide derivatives. IX].

A series of quaternary ammonium salts of 3-alkylaminoderivatives of 1,2,4-benzothiadiazine-1,1-dioxide were prepared and tested for cardiovascular activity. Almost all the substances tested proved to have some measure of depressant activity on arterial pressure and the most interesting compounds in this respect were (XII), (XIII), (XV) and (XIX) for which hypotensive values between 60 and 70% with respect to the base level were recorded. Compound (XV) also caused increase in the differential pressure and decrease of cardiac frequency. The later however was increased by some other compounds [(XII), (XVIII)]. The structure-activity relationships are discussed taking into account also the activity of the parent tertiary amines.

Animals↗
PubMed1982

[Sulfonamides with central nervous system action. V].

A series of 2-nitro and 2-aminobenzenesulfon-N-acylamides variously substituted on the benzene ring were prepared and tested for anticonvulsant activity (electro shock, pentamethylenetetrazole). Some of the compounds tested gave some measure of protection against convulsions induced by electric shock. The importance of the trifluoromethyl substituent in this effect was demonstrated.

Animals↗
PubMed1981

[Heteroarylalkanoic acids with potential anti-inflammatory activity. II].

A series of (1,2,4-benzothiadiazin-1,1-dioxide-3-yl)acetic acids was prepared so that antiinflammatory activity could be tested. Some of the compounds synthetized showed marked activity against plantar edema induced by carrageenin and/or dextran. It was found that in this series antiinflammatory activity is related to the nature of the substituents on the benzene ring as well as their number, dihalogen substitution being the most favourable modification and dichlorosubstitution in particular giving the compounds most active against both types of edema.

Acetates↗
PubMed1979

[Cardiovascular effect of 1,2,4-benzothiadiazine-1,1-dioxide derivatives. VIII].

A series of carboxy- and carbomethoxyalkyl derivatives of 3-amino-1,2,4-benzothiaidazin-1,1-dioxide either substituted or unsubstituted in the benzene ring [compounds (I leads to XVIII)] was prepared and tested for cardiovascular activity. It was found that the introduction of a carboxy-or carbalkoxy-group in the omega position of 3-alkylamino derivatives of 1,2,4-benzothiadiazine-1,1-dioxide usually causes marked decrease or abolition of the cardiovascular activity shown by the parent compounds. The negative effect on the pressor trace (hypotension and increase in differential pressure) is more frequent and significant than that on bradycardial activity.

Animals↗
PubMed1979

[Heteroarylalkanoic acids with potential anti-inflammatory activity].

A series of (3-oxodihydro-1,2,4-benzothiadiazin-1,1-dioxide-3-yl)acetic acids [compounds of type (A)] and (1,2,4-benzothiadiazin-1,1-dioxide-3-yl)oxyacetic acids [compounds of type (B)] were synthesised and tested for antiinflammatory activity. Preliminary tests showed certain compounds to have a significant level of antiinflammatory activity in rat paw edema induced by carrageenan. It was found that the antiinflammatory activity of this series of compounds depends on the nature, number and position of the substituents on the benzene ring.

Acetates↗
PubMed1978

[Cardiovascular action of 1,2,4-benzothiadiazine-1,1-dioxide derivatives. VI].

A series of 3,4-dihydro derivatives of 6-chloro-, 7-chloro-, 5,7-dichloro-, 6,7-dichloro-, 5,7-dibromo-, 5-nitro-7-chloro-, 7-nitro-, 7-amino-1,2,4-benzothiadiazine-1,1-dioxide, various substituted on the heterocyclic carbon, was prepared and tested for cardiovascular activity. It was found that in this series of compounds cardiac activity predominates and is exclusively of the depressant type. Bradycardial activity seems to be affected both by the nature of the substituent on the heterocyclic carbon atom and by the substituents on the benzene ring. An alkyl chain of three carbon atoms, normal or alpha-ethylsubstituted, on C3 and the presence of a chlorine atom in positions 6 or 7 seem to be the most significant structural features for this activity. Some of the substances tested showed a pressor effect (hypotension and/or increase in differential pressure).

Animals↗
PubMed1978

[Cardiovascular action of 1,2,4-benzothiadiazine-1,1-dioxide derivatives. VII].

A series of dimethylamino-, diethylamino-, pyrrolidyl- and morpholylalkyl derivatives of 3-amino-1,2,4-benzothiadiazine-1,1-dioxide (compounds I leads to XX) was prepared and tested for cardiovascular activity. It was found that substitution of the alkyl group with the above mentioned groups in 3-amino-1,2,4-benzothiadiazine-1,1-dioxide derivatives in most cases causes marked dissociation of hypotensive activity from bradycardial activity and also disappearance or great reduction in the effect on differential pressure. It was also found that hypotensive activity is particularly dependent on the nature of the basic chain in the two components: length of the carbon chain between the two nitrogens and nature of the basic grouping. For the first component a chain of three carbon atoms seems the most effective and for the second the diethylamino group seems the most favourable. In addition, substituents in the benzene ring influence hypotensive activity, often positively, and 6,7-dichlorosubstitution in some compounds also affects the increase of differential pressure.

Animals↗