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Biomedical subjects

M Di Bella

Publications and source records attributed to M Di Bella.

At least 37 records · Page 2Linked to original sources
PubMed1983

Synthesis and antimicrobial activity of monoalkylcarbamic and thiocarbamic esters of 3-mercapto-1,2,4-benzothiadiazine-1,1-dioxide and of its Bz-derivatives.

A new series of monoalkylcarbamic esters of 3-mercapto-1,2,4-benzothiadiazine-1,1-dioxide (I) and of its 6-chloro- and 5,7-dichloroderivatives [compounds (II leads to XVI)] and a series of monoalkylthiocarbamic esters of (I) [compounds (XVII leads to XIX)] were synthesized and evaluated in vitro for antimicrobial activity. All the substances studied have been found to possess an inhibiting action on one or more strains of mycetes of the genus Candida and on some strains of Gram-positive bacteria belonging to the genus Staphylococcus. Moreover, some compounds have shown a bacteriostatic effect on a strain belonging to the genus Streptococcus. None of the substances tested was active on Gram-negative schizomycetes.

Anti-Bacterial Agents↗
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

[Antimicrobial activity of derivatives of 1,2,4-benzothiadiazine-1,1-dioxide. VIII].

The antimicrobial activity of a series of fluoro derivatives of benzothiadiazine and sulfonamides was studied. The compounds tested can be grouped as: a) 3-alkylmercapto derivatives of 6-trifluoromethyl-1,2,4-benzothiadiazine-1,1-dioxide (III leads to VI); the 3-mercapto precursor (VII) and the related 3-picolinic salt (VIII); b) 3-trifluoromethyl derivatives of 1,2,4-benzothiadiazine-1,1-dioxide and of its benzene substituted derivatives (IX leads to XVI); c) trifluoroacetylaminobenzenesulfonamides (XVII leads to XXV). Two of the 3-alkylmercapto compounds [(V) and (VI)] showed marked inhibitory activity against some strains of Staphylococcus, Streptococcus and Diplococcus. None of the compounds tested proved active against Gram-negative schizomycetes (genera Salmonella, Shigella, Escherichia, Proteus, Pseudomonas, Enterobacter, Klebsiella, Serratia, Yersinia, Providencia) or against yeasts (Candida).

Benzothiadiazines↗
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↗
PubMed1979

[Antimicrobial effect of derivatives of 1,2,4-benzothiadiazin-1,1-dioxide. VII].

Series of alkyl derivatives of the following have been prepared: 5,7-dichloro- [compounds (II leads to V)], 6-methyl- [compounds (VI leads to IX)] and 6-methoxy-3-mercapto-1,2,4-benzothiadiazine-1,1-dioxide [compounds (X leads to XIII)]. The products were tested for antimicrobial activity. Studies were also made of the corresponding 3-mercapto precursors (XIV, XV, XVI) and the relative 3-picolinium salts (XVII, XVIII, XIX) and also of the 3-picolinium salts of 6-chloro-, 7-chloro- and 6,7-dichloro-3-mercapto-1,2,4-benzothiadiazine-1,1-dioxide (XX, XXI, XXII). Some of the 3-alkylmercapto compounds, and especially the 5,7-dichloro derivative, inhibited various strains of Gram-positive bacteria of the genus Staphylococcus, while the same substances proved much less effective against the genera Streptococcus and Diplococcus. Antimicrobial activity appeared to be influenced by the length of the alkyl chain as well as by the nature and position of the substituents on the benzene ring. The compounds proved inactive against the Gram-negative schizomycetes (Salmonella, Shigella, Escherichia, Proteus, Pseudomonas. Enterobacter, Klebsiella, Serratia, Yersinia, Providencia) and against yeasts (Candida) with the exception of compound (V) which showed slight bacteriostatic action against three strains of Candida albicans.

Anti-Bacterial Agents↗
PubMed1978

[Bromination of 3-amino-1,2,4-benzothiadiazine-1,1-dioxide].

The bromination of 3-amino-1,2,4-benzothiadiazine-1,1-dioxide (1) in N,N-dimethylformamide has been studied. Depending on the operating conditions the reaction produces 7-bromo-3-amino-1,2,4-benzothiadiazine-1,1-dioxide (II) or 5,7-diabromo-3-amino-1,2,4-benzothiadiazine-1,1-dioxide (III). Derivatives halogenated at the nitrogen were not isolated in any of the experiments.

Benzothiadiazines↗
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↗
PubMed1975

[Iodo-derivatives of 2-aminobenzensulfonamide and 1,2,4-benzothiadiazine-1,1-dioxide].

A series of iodo derivatives of 2-aminobenzensulfonamide and its derivatives has been prepared by reaction with iodine chloride in N,N-dimethylformamide or N,N-dimethylacetamide. The structure of each compound was confirmed by transformation with formic acid into the corresponding 1,2,4-benzothiadiazine and comparison with the same compounds prepared via the Sandmeyer reaction starting form amino derivatives of known structure. It was found that the iodination reaction in N,N-dimethylformamide, can lead, depending on the nature of the starting material, to the formation of benzothiadiazine derivatives apparently generated from sulfonamide via a formylation reaction due to N,N-dimethylformamide.

Benzene Derivatives↗