Titre du document / Document title

Synthesis, antiinflammatory and analgesic activity of new hexahydropyrimidine derivatives

Auteur(s) / Author(s)

KHAN M. S. Y. ⁽¹⁾ ; GUPTA M. ⁽¹⁾ ;

Affiliation(s) du ou des auteurs / Author(s) Affiliation(s)

⁽¹⁾ Department of Pharmaceutical Chemistry, Hamdard University, Hamdard Nagar, New Delhi, INDE

Résumé / Abstract

A number of potentially active hexahydropyrimidine derivatives of pharmaceutical interest have been synthesized. Various diSchiff's bases prepared by reacting different aromatic aldehydes with 1,3-diaminopropane were suitably reduced to give their tetrahydro derivatives which were then condensed with appropriate aldehydes to give a series of hitherto unreported hexahydropyrimidines. The resulting products were evaluated by oral route for their antiinflammatory activity. The activity of compounds 11, 23 and 4 was excellent and comparable to indomethacin. In addition to oral route of administration, the antiinflammatory activity of hexahydropyrimidine derivatives was also studied topically through transdermal gels. Compounds 11, 23, 4 and 22 produced significant inhibition in edema and showed good antiinflammatory activity comparable to diclofenac sodium gel (Relaxyl^R gel). All these compounds were also tested for their analgesic activity and their LD₅₀ determined. Compounds 11, 20 and 23 showed a comparable activity with aspirin. The MTD for all the compounds was found to be > 1800 mg/kg.

Revue / Journal Title

Pharmazie   ISSN 0031-7144   CODEN PHARAT 

Source / Source

2002, vol. 57, n^o6, pp. 377-383 (16 ref.)

Langue / Language

Anglais
Revue : Allemand

Editeur / Publisher

Govi, Eschborn, ALLEMAGNE  (1946) (Revue)

Mots-clés anglais / English Keywords

Vertebrata ; Mammalia ; Rodentia ; Aniline derivatives ; Tertiary amine ; Chlorine Organic compounds ; Benzenic compound ; Six membered ring ; Nitrogen heterocycle ; Pyrimidine derivatives ; Chemical synthesis ; Topical administration ; Percutaneous route ; Oral administration ; Chemotherapy ; Experimental disease ; Rat ; Animal ; Analgesic ; Antiinflammatory agent ; Structure activity relation ;

Mots-clés français / French Keywords

Vertebrata ; Mammalia ; Rodentia ; Pyrimidine(1,3-bis[2-chlorobenzyl]-2-[4-(diméthylamino)phényl]-perhydro) ; Pyrimidine(1,3-bis[3-chlorobenzyl]-2-[4-(diméthylamino)phényl]-perhydro) ; Aniline dérivé ; Amine tertiaire ; Chlore Composé organique ; Composé benzénique ; Cycle 6 chaînons ; Hétérocycle azote ; Pyrimidine dérivé ; Synthèse chimique ; Voie externe ; Voie percutanée ; Voie orale ; Chimiothérapie ; Pathologie expérimentale ; Rat ; Animal ; Analgésique ; Antiinflammatoire ; Relation structure activité ;

Mots-clés espagnols / Spanish Keywords

Vertebrata ; Mammalia ; Rodentia ; Anilina derivado ; Amina terciaria ; Cloro Compuesto orgánico ; Compuesto bencénico ; Ciclo 6 eslabones ; Heterociclo nitrógeno ; Pirimidina derivado ; Síntesis química ; Vía externa ; Vía percutánea ; Vía oral ; Quimioterapia ; Patología experimental ; Rata ; Animal ; Analgésico ; Antiinflamatorio ; Relación estructura actividad ;

Localisation / Location

INIST-CNRS, Cote INIST : 3582, 35400010164615.0050