Biomedical subjects

M Khalifa

Publications and source records attributed to M Khalifa.

At least 55 records · Page 3Linked to original sources

PubMed1977

Synthesis of some N-substituted salicylamides structurally related to certain antimicrobials.

The condensation of 5-nitrosalicoylchloride and 5-sulphamoylsalicylic acid with certain amines is described. Reacting the acid chloride with 3-amino-2-oxazolidone, 4-aminophenazone, thiosemicarbazide, 1-aminohydantoin and 2-aminopyridine yielded the correspondong N-substituted 5-nitrosalicylamides (1a-c), while with semicarbazide a disubstituted product type 2 was obtained. On the other hand, when 5-sulphamoylsalicylic acid was condensed with o-chloroaniline, m-chloroaniline and 4-aminophenazone in the presence of phosphorus trichloride, instead of affording the expected condensation products type 3, it yielded N1N5-disubstituted 5-sulphamoylsalicylamides (4a-c). The synthesized compounds were screened for antimicrobial activity.

Antifungal Agents↗

PubMed1977

Synthesis of certain 4-oxo-1.2.3.4-tetrahydroquinoline and benzazocine derivatives likely to possess analgesic activity.

Cyanoethylation of anthranilic acid afforded the N-cyanoethyl derivative which on treatment with ethanolic and methanolic hydrogen chloride yielded the corresponding diethyl and dimethyl esters respectively. Application of the Dieckmann's conditions to the N-acetyl derivatives of the two esters using sodium hydride and sodium ethoxide afforded different products. With the former, the expected products were obtained, while with the latter catalyst both esters furnished one and the same compound which was shown to be a benzazocine trione. The structure of the azocine was inferred from elemental analysis, spectroscopic data and formation of derivatives.

Analgesics↗

PubMed1977

Synthesis of certain benzo- and pyridodiazepines likely to possess tranquilizing effect.

The synthesis of certain 1.5-benzodiazepinediones, some of their oxygen-free analogues and a number of the 7-nitro derivatives is described. Condensation of 3.4-diaminopyridine with diethylmalonate instead of affording the expected pyridodiazepine, yielded an imidazopyridine, the structure of which was inferred from spectral data Nevertheless, the pyridodiazepine was obtained by condensing the diamino-heterocycle with malonyl dichloride.

Anti-Anxiety Agents↗

PubMed1977

Synthesis of some 3.4.5-trimethoxybenzyl derivatives of certain amino compounds likely to posses cns activity.

The condensation of 3.4.5-trimethoxybenzyl chloride with certain amines is described. Reacting the aralkyl chloride with 4-aminophenazone, 2-aminopyridine, piperidine, N-methylpiperazine, pyrrolidine and morpholine yielded the corresponding trimethoxybenzyl derivatives la--f. On the other hand, alpha-[3.4.5-trimethoxybenzamido]-glutarimide (2) was synthesized via the acylation of glutamic acid with trimethoxybenzoyl chloride, dehydration of the N-acyl derivative and finally imidation of the inner anhydride thus formed.

Aminopyrine↗

PubMed1976

Synthesis of certain spiro compounds.

The synthesis of certain N-substituted azaspirodiones and azaspiranes is described. Fusing equimolecular amounts of 2-oxaspiro [4.4]nonane-1.3-dione with a number of amino compounds afforded the corresponding N-substituted azaspirodiones. However, with certain o-substituted anilines, no condensation took place. Reduction of the N-haloaryl azaspirodiones gave the corresponding oxygen free compounds. Other azaspiranes were isolated as the quaternary methiodides. Applying the Mannich conditions to 2-azaspiro[4.4]nonane-1.3-dione yielded the N-Mannich bases.

Chemical Phenomena↗

PubMed1976

Synthesis of 1.2.3.4-tetrahydro-2.4-dioxoquinazoline derivatives for pharmacological study.

The condensation of 4-chloroanthranilic acid with several substituted monophenylureas is described. Reacting equimolecular amounts of the haloanthranilic acid with monophenylurea, p-tolylurea, p-methoxyphenylurea, p-ethoxyphenylurea, p-bromophenylurea, p-chlorophenylurea and m-chlorophenylurea--by fusion in a pressure bottle--yielded the corresponding 7-chloro-3-aryl-.2.3.4-tetrahydro-2.4-dioxoquinazoline (1a--g). On the other hand, o-substitute phenylureas, instead of affording the expected condensation products, yielded a compound which was shown to be 7-chlorobenzoyleneurea (2), the formation of which is accounted for.

Chemical Phenomena↗

PubMed1976

Synthesis and screening of some substituted 3.5-dioxopyrazolidines.

Seven new 3.5-dioxopyrazolidine derivatives, incorporating in their molecule a p-substituted benzoyl grouping, were synthesized. The preliminary screening of four selected compounds showed that 1-phenyl-2-[p-nitrobenzoyl]-4.4-diethyl-3.5-dioxopyrazolidine possesses a low order of antiinflammatory activity.

Animals↗

PubMed1976

Synthesis of some quinazolone derivatives structurally related to certain sedatives and hypnotics.

The preparation of certain 3-substituted derivatives of 3.4-dihydro-2-methyl-4-oxoquinazoline is described. The synthesis fo a quinazolone-barbituric acid derivative, in which the two constituting moieties are separated by methylene groups, was achieved by reacting 3-[B-haloethyl]-3.4-dihydro-2-methyl-4-oxoquinazoline with sodio malonic ester and subsequent cyclization of the ester so formed with urea. Attempts to introduce the alpha-glutaryl group at the position 3 of the quinazolone ring system via different routes were unsuccessful.

Barbiturates↗

PubMed1975

Synthesis of certain 3-aminoquinazolinone Schiff's bases structurally related to some biologically active compounds.

The condensation of 2-methyl-3-amino-4(3H)-quinazolinone and 2-phenyl-3-amino-4(3H)-quinazolinone with different aldehydes is described. Reacting equimolecular amounts of these two amino compounds with p-nitrobenzaldehyde, p-hydroxybenzaldehyde, cinnamaldehyde and 5-nitro-2-furfuraldehyde diacetate afforded the respective Schiff's bases. Condensation of benzaldehyde, anisaldehyde, p-dimethylaminobenzaldehyde and o-nitrobenzaldehyde with the former quinazolinone afforded the corresponding condensation products while with the latter no condensation took place. Furthermore, condensation of cinnamaldehyde with methylaminoquinazolinone in pyridine and in glacial acetic acid afforded the mono- and di-condensation products respectively while furfural, thiophenaldehyde, resorcinaldehyde, protocatechualdehyde, veratraldehyde, and salicylaldehyde, the condensation ended in failure.

Quinazolines↗

PubMed1975