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Biomedical subjects

M Movrin

Publications and source records attributed to M Movrin.

13 recordsLinked to original sources
PubMed1981

Binding (in vitro) of some antimitotic isatin derivatives to human serum albumin.

The binding of isatin and its mustard N-Mannich base, considerably biologically active compounds, to human serum albumin has been studied by equilibrium dialysis and ultrafiltration. The influences of ligand and macromolecule concentration, temperature and pH of the incubation medium have been demonstrated. The Scatchard plot of isatin binding to albumin shows a biphasic curve which indicates the presence of at least two different binding sites on albumin molecule. One site with a higher affinity, K1 = 2.25 X 10(3) M and n1= 25, and the other site with a lower affinity, i.e. higher capacity. In the cases of mustard Mannich base we could demonstrate the same type of curve, K1 = 2.20 X 10(5) M and n1 = 1.0, whereas another site has a lower affinity and greater number of binding sites.

Humans↗
PubMed1980

Biologically active Mannich bases derived from nitroxoline.

A series of compounds with various basic side chains were derived from 5-nitro-8-hydroxyquinoline (nitroxoline). Aminomethylation of nitroxoline led exclusively to the formation of o-substituted phenolic Mannich bases. Depending on the kind of the primary or secondary amine participating in the Mannich reaction differently substituted compounds were prepared in order to study the influence of the basic side chain on their biological activity. The compound with N-bis(2-hydroxyethyl)amino group exhibited the highest mitodepressant activity determined in a phyto test on Lepidium sativum L. Preliminary test for antibacterial and antifungal activities using standard test microorganisms indicate rather strong antimicrobial properties of several synthesized compounds.

Amines↗
PubMed1980

Antibacterial and antifungal activities of nitroxoline Mannich bases.

The in vitro activity of nitroxoline and its Mannich bases against bacteria and fungi was investigated. Nitroxoline and its derivative with diisopropylamine as an amino component, exhibited the highest antimicrobial activity. The optimum hydro/lipophilic properties (log P), both for antibacterial and antifungal activity, are about log P values of 2. The least effective compound was this nitroxoline Mannich base which has diethanolamine as an amino component.

Amines↗
PubMed1980

Effects of isatin N-Mannich bases on HeLa cells.

A congeneric series of 5-haloisatins was synthesised and tested for biological activity. Mannich bases and hydrazones of 5-chloro- and 5-iodoisatin were prepared and their structures were determined spectrophotometrically. Morphological deformations and inhibition of radiolabelled precursor incorporation into DNA were studied in HeLa cell culture; antimitotic activity was examined using a phyto test with Lepidium sativum L. I50 values were determined for the most interesting compounds. The results obtained can be interpreted in terms of the group contributions to the parent molecule. Introduction of iodine into the aromatic moiety of isatin (position 5) considerably increased inhibitory potency of the parent molecule. Furthermore, N-bis-(2-chloroethyl) and N-bis-(2-hydroxyethyl) groups, respectively, as amino components of some of the N-Mannich bases, markedly enhance the biological activities studied in this work.

Amines↗
PubMed1980

Structure-activity relationship of isatin Mannich bases and hydrazones.

35 isatin Mannich bases and hydrazones were tested fore their mitodepressant activity applying a phyto test with Lepidium sativum L. The obtained results were subjected to the Free-Wilson's analysis. Although calculated and experimentally determined mitodepressant activities differ considerably in some cases, there is a correlation (r = 0.94) between the studied structures and mitodepressant activities.

Amines↗
PubMed1980

Structural analogues of isatin and their antimicrobial activity.

A series of 5-haloisatins were aminomethylated in position 1 and hydrazino groups were introduced in position 3. Synthesized N-Mannich bases and hydrazones were biologically tested against various kinds of bacteria and fungi. Results from these in vitro studies showed a considerable growth inhibition of some gram negative bacteria caused by chlorinated N-Mannich bases of isatin. Comparing the inhibition zones of the halogenated isatin N-Mannich bases with structural analogues of nonhalogenated ones as well as with isatin itself, an increase in antimicrobial activity was observed, thus, indicating the importance of both substituents, namely, halogen in position 5 and an amino moiety in position 1. The most biologically active compound was found to be diisopropylamino-N-Mannich base of 5-chloroisatin.

Anti-Bacterial Agents↗
PubMed1979

Antibacterial and antifungal activities of isatin N-Mannich bases.

The antimicrobial and antifungal activities of 29 congeneric isatin N-Mannich bases were investigated by testing against standard test microorganisms and 21 pathogenic Gram-negative microorganisms. Considerable growth inhibition of Gram-negative bacteria and yeasts and slight inhibition of Gram-positive bacteria resulted when they were treated with the various N-Mannich bases of isatin and 5-nitroisatin, respectively.

Anti-Bacterial Agents↗
PubMed1979

[Biologically active azomethines. Delépine reaction with 1-chloromethylisatin; preparation of some 1-aminomethylisatinazomethines (author's transl)].

The authors describe the synthesis of I-aminomethylisatin (3) from [I-chloromethylisatin] (1) by means of the Delépine reaction. On condensation with aromatic aldehydes, 3 yields the azomethines 5--7. The azomethine 5 is converted into the corresponding thiosemicarbazone 9. Testing for mitodepressive activity showed that the compounds 5--7 are active. On testing in vitro for tuberculostatic effects, the compound 9 proved exceptionally potent.

Antitubercular Agents↗
PubMed1979

[Biologically active N-Mannich bases of isatin-3-(phenyl)-imines (author's transl)].

By the condensation of isatin and 5-nitroisatin with substituted aromatic amines, isatin- and 5-nitroisatin-3-(phenyl)-imines (azomethines) are formed which are converted into N-Mannich-bases by aminomethylation and may be formulated as azomethines with E configuration. A biotest of Lepidium sativum L. was used to prove mitodepressive properties. Some compounds showed a significant growth-inhibiting activity. It was found that a change in activity is produced by condensation on the carbon atom in position 3 and by aminomethylation on the nitrogen atom in the isatin nucleus.

Imines↗