Advances in the Chemistry of Anaesthetics (1961–1971)

Cherkasova, E. M.; Pryanishnikova, N. T.; Bogatkov, S. V.; Erkomaishvili, G. S.

doi:10.1070/rc1973v042n10abeh002772

Russ. Chem. Rev.

1973

DOI: 10.1070/rc1973v042n10abeh002772

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Advances in the Chemistry of Anaesthetics (1961–1971)

E. M. Cherkasova¹,

N. T. Pryanishnikova²,

S. V. Bogatkov³

et al.

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Cited by 8 publications

(3 citation statements)

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“…Indeed, the amides of benzilic acid (Ph 2 C(OH)C(O)NH 2 ), mandelic acid (PhCH(OH)C(O)NH 2 ), and a,a-diphenylacetic acid exhibit such activity [67]. On passage from a-phenylcarboxylic acids to N-phenylamides of these acids, the anticonvulsant activity is retained (this behavior is also observed in local anesthetics [68]). N-Phenyland N,N-diphenylamides of acetic acid exhibit anticonvulsant activity in both MES and corazole antagonist tests; the latter diphenylamide is comparable in this activity with compound III-10.…”

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confidence: 91%

“…Significant anesthetic action is produced by bisdialkylaminoalkyl esters of fatty dicarboxylic acids and by monodiethylaminoethyl ester of malonic acid. An increase in the anesthetic properties of carboxylic acids was observed upon modification of the base structure via the introduction of fragments of the type of Ad, cis-C 6 H 11 , Pr, and (as was already mentioned above) Ar, including the ring with substituents such as Ph, p-C 6 H 13 O-, p-PhOCH 2 CH 2 O - [68,70]. A branched hydrocarbon framework favors the appearance of anticonvulsant activity in carboxylic acid amides (examples are the well-known anticonvulsants such as valproic acid I-13, its amide, and the amides of adamantanecarboxylic acid and a,a-diphenylacetic acid).…”

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confidence: 93%

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Some aspects in the search for anticonvulsants (a review)

et al. 2004

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Functional organization of the central nervous system (CNS) relies upon a fine interplay between two principal processes involved in nervous activity: excitation and inhibition. Violation of this interaction leads to the development of cerebral pathologies. Both the excitation and inhibition processes are mediated by intercell and intracell chemical neurotransmitters (endogenous ligands). In particular, interference with the neuromediator function of only g-aminobutyric acid (GABA) causes a number of pathologies, primarily convulsive states, determining the symptomatics of disorders such as epilepsy, drug intoxication (strychnine, corazole, bemegride, novocain, organophosphorus compounds, insecticides, etc.), infectious diseases (meningitis, toxic influenza, tetanus, etc.), cerebral traumas, brain edemas, and others. In practice, such convulsions can be arrested using drugs belonging to various pharmacological groups, including pure anticonvulsants, barbiturates, bromides, tranquilizers, hypnotics, etc., which are capable of preventing the development or decreasing the intensity of convulsions, reducing the frequency of attacks, or eliminating the accompanying disturbances (loss of consciousness, behavioral and vegetative disorders, etc.).However, the group of anticonvulsants presently administered in practice contains no one highly effective drug of universal use. This is related not only to the variety of forms of the convulsive states, but also to the complexity of interactions between neuromediator systems, primarily those of inhibiting (GABA) and exciting amino acids [1 -5]. The continuous search for new anticonvulsants (see, e.g., [6 -20]) needs no additional justification. This paper addresses certain features and rules in the search for compounds possessing anticonvulsant activity.Biochemical disorders in CNS, which are capable of inducing the development of convulsions, include changes in (i) the transmembrane concentration gradients of sodium, potassium, calcium, and chlorine ions (factors providing for the membrane rest and action potentials), (ii) the energy balance in neurons, and (iii) the level and metabolism of synaptic mediators including GABA, glutamic and asparagic acids (ex-

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confidence: 91%

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confidence: 93%

Some aspects in the search for anticonvulsants (a review)

et al. 2004

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“…An increase in the anesthetic properties of carboxylic acids was observed upon modification of the base structure via the introduction of fragments of the type of Ad, cis-C 6 H 11 , Pr, and (as was already mentioned above) Ar, including the ring with substituents such as Ph, p-C 6 H 13 O-, p-PhOCH 2 CH 2 O - [68,70]. In some cases, anesthetic activity was observed for cycloalkylcarboxylic acid esters.…”

mentioning

confidence: 95%

Some aspects in the search for anticonvulsants (a review)

et al. 2004

View full text Add to dashboard Cite

Functional organization of the central nervous system (CNS) relies upon a fine interplay between two principal processes involved in nervous activity: excitation and inhibition. Violation of this interaction leads to the development of cerebral pathologies. Both the excitation and inhibition processes are mediated by intercell and intracell chemical neurotransmitters (endogenous ligands). In particular, interference with the neuromediator function of only g-aminobutyric acid (GABA) causes a number of pathologies, primarily convulsive states, determining the symptomatics of disorders such as epilepsy, drug intoxication (strychnine, corazole, bemegride, novocain, organophosphorus compounds, insecticides, etc.), infectious diseases (meningitis, toxic influenza, tetanus, etc.), cerebral traumas, brain edemas, and others. In practice, such convulsions can be arrested using drugs belonging to various pharmacological groups, including pure anticonvulsants, barbiturates, bromides, tranquilizers, hypnotics, etc., which are ca-pable of preventing the development or decreasing the intensity of convulsions, reducing the frequency of attacks, or eliminating the accompanying disturbances (loss of consciousness, behavioral and vegetative disorders, etc.).However, the group of anticonvulsants presently administered in practice contains no one highly effective drug of universal use. This is related not only to the variety of forms of the convulsive states, but also to the complexity of interactions between neuromediator systems, primarily those of inhibiting (GABA) and exciting amino acids [1 -5]. The continuous search for new anticonvulsants (see, e.g., [6 -20]) needs no additional justification. This paper addresses certain features and rules in the search for compounds possessing anticonvulsant activity.Biochemical disorders in CNS, which are capable of inducing the development of convulsions, include changes in (i) the transmembrane concentration gradients of sodium, potassium, calcium, and chlorine ions (factors providing for the membrane rest and action potentials), (ii) the energy balance in neurons, and (iii) the level and metabolism of synaptic mediators including GABA, glutamic and asparagic acids (ex-

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Esters of heterocyclic γ-amino alcohols

et al. 1975

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Advances in the Chemistry of Anaesthetics (1961–1971)

Cited by 8 publications

References 111 publications

Some aspects in the search for anticonvulsants (a review)

Some aspects in the search for anticonvulsants (a review)

Some aspects in the search for anticonvulsants (a review)

Esters of heterocyclic γ-amino alcohols

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