Naslov
1, 3-Benzoxazin-2, 4-dione and 1, 4-Benzoxazin-2, 3-dione Derivatives

Autori
Movrin, Marija ; Maysinger, Dušica ; Jadrijević-Mladar, Milena

Vrsta, podvrsta i kategorija rada
Sažeci sa skupova, sažetak, znanstveni

Izvornik
FIP-85 Abstracts, Programme of Oral and Poster Communications, 45th International Congress of Pharmaceutical Sciences / - Montréal, 1985, 173-173

Skup
45th International Congress of Pharmaceutical Sciences

Mjesto i datum
Montréal, Kanada, 02.09.1985. - 06.09.1985

Vrsta sudjelovanja
Poster

Vrsta recenzije
Međunarodna recenzija

Ključne riječi
1; 3-Benzoxazin-2; 4-diones; 1; 4-Benzoxazin-2; 3-diones; Synthesis; Biological activity; Topological indices; QSAR

Sažetak
A series of 1, 3-benzoxazin, 2, 4-diones and 1, 4-benzoxazin-2, 3-diones have been synthesized and then tested for their antimitotic and antimicrobial activity. Benzoxazin-diones were prepared by oxidation of isatin and 5-nitro-isatin. Acting as H-active hetercyclic compounds benzoxazin-diones were either aminomethylated or condensed with monosubstituted hydrazines, thiosemicarbazide and several aromatic amines and subsequently aminomethylated. In vitro studies of the synthesized compounds with incorporated basic side chains similar to alkilating agents showed considerably antimitotic activity. The compounds with an aminoacid side chains were also active. Mannich bases with D, L-alanine proved to be more active than those ones containing L-alanine. The glycinamide analogue showed significantly higher mitodepressant activity than the corresponding glycine-ester derivative. The same benzoxazine derivatives tested against variety of standard microorganisms exhibited only weak bacteriostatic activity. It is interesting to note that the increase in relative molecular mass of the synthesized compounds is correlated reasonably well with the theoretically calculated topological indices.

Izvorni jezik
Engleski

Znanstvena područja
Farmacija

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