Sulphonamides. IV. The Reaction of N-Heterocyclic Amines with Sulphonyl Halides

1952 ◽  
Vol 5 (2) ◽  
pp. 374
Author(s):  
SJ Angyal
Keyword(s):  
Heterocyclic Amines ◽  
Amino Group ◽  
Ring Nitrogen ◽  
Amino Derivatives ◽  
Cyclic Compounds ◽  
Derivatives Of

The hypothesis is advanced that the reaction of sulphonyl halides with amino-derivatives of nitrogen-containing cyclic compounds occurs on the ring-nitrogen (which is the more basic), followed either by reaction of the amino-group with another molecule of sulphonyl halide, or by migration of the sulphonyl group from the ring to the ammo-nitrogen. Several apparently anomalous cases of this reaction are explained.

Exchange of the amino group in ?-amino derivatives of sulfolane

1974 ◽  
Vol 10 (5) ◽  
pp. 538-540
Author(s):  
T. �. Bezmenova ◽  
P. G. Dul'nev
Keyword(s):  
Amino Group ◽  
Amino Derivatives ◽  
Derivatives Of

scholarly journals The antiseptic and trypanocidal action of some benzoylamino quinoline anil and styryl compounds

1933 ◽  
Vol 113 (783) ◽  
pp. 300-307 ◽  
Keyword(s):  
Inhibitory Concentration ◽  
Protein Solutions ◽  
Amino Group ◽  
Peptone Water ◽  
High Dilutions ◽  
Tertiary Amino ◽  
Amino Derivatives ◽  
Derivatives Of ◽  
Very High ◽  
Close Parallel

The antiseptic and trypanocidal properties of certain amino derivatives of 2-styryl quinoline have already been dealt with. Hitherto the substituent groups in the quinoline nucleus have been chiefly in the 6-position (Occasionally the 4-or 7-position) and have consisted of primary or tertiary amino, acyl-amino or carboxylamino groups. In the present series the 6-position is occupied by a primary, tertiary or acetylated para amino benzoylamino group. The methods of estimating antiseptic and trypanocidal action correspond with those previously used. The results are given in Table I. For reasons already stated (Ashley and others, p. 293), the antiseptic potency is represented by the inhibitory concentration of the substances. The anils in which the 6-amino group of the quinoline nucleus is arylated (Nos. 73, 422, 421) are all very powerfully antiseptic toward both staphylococcus and B. coli . In this respect they resemble the 2 p -dimethylamino anils in which the 6-position in the quinoline nucleus is occupied by an acyl-amino group (Nos. 59-69). Several of the styryl compounds also are fairly active antiseptics both for staphylococcus and B. coli . especially Nos. 426. 430. On comparing their effects with those of the non-benzoylated analogues bearing the same terminal groups in the side-chains, it appears that there is no close parallel between structure and action in the two series— of . Nos. 245, 87, 427, 21; 426, 24; 437, 90. Several of the benzoylamino compounds even in very high dilutions are precipitated in protein solutions (peptone water, serum); this is especially so with No. 430 and, to a less extent, with Nos. 421, 437, 422 and 245.

SOME DIRECTIONS IN THE MODIFICATION OF AZOLES

2020 ◽  
Vol 5 (443) ◽  
pp. 85-91
Author(s):  
Ibrayev M.K., ◽  
◽  
Takibayeva A.T., ◽  
Fazylov S.D., ◽  
Rakhimberlinova Zh.B., ◽  
...  
Keyword(s):  
13C Nmr Spectroscopy ◽  
Biologically Active Compounds ◽  
Biologically Active ◽  
Active Compounds ◽  
Synthesis Conditions ◽  
Alkaloid Cytisine ◽  
Azole Ring ◽  
Cyclic Compounds ◽  
New Compounds ◽  
Derivatives Of

This article presents studies on the targeted search for new derivatives of azoles, such as benzthiazole, 3,5-dimethylpyrazole, 1,3,4-oxadiazole-2-thione, 1,3,4-thiadiazole. The possibility of combining in one molecule of the azole ring with other cyclic compounds: the alkaloid cytisine, morpholine, furan and some arenes has been studied. To obtain new compounds, the reactions of bromination, acylation, and interaction with isothiocyanates were studied. Optimal synthesis conditions were studied for all reactions. It was found that the reaction of 4-bromo-3,5-dimethylpyrazole with isothiocyanates, in contrast to the previously written derivatives of anilines, takes a longer time and requires heating the reaction mixture. The combination of a pirasol fragment with halide substituents often results in an enhanced therapeutic effect. The synthesized 2-bromine-N-(6-rodanbenzo[d]thiazole-2-yl)acetamide, due to the alkylbromide group, is an important synth in the synthesis of new benzthiazole derivatives. Its derivatives combine in one molecule the rest of rhodanbenzthiazole with alkaloid cytisine and biogenic amine morpholine and are potentially biologically active compounds, since the molecule structure contains several pharmacophoric fragments: benzthiazole and alkaloid (amine) heterocycles, rhodane and urea groups. The mechanism of formation of 1,3,4-oxadiazole-2-tyons from hydrazides under action on them by carbon disulfide was studied and assumed. It was shown that dithiocarbamates in acidic medium decompose with the release of hydrogen sulfide and the formation of highly reactive isothiocyanate group. Then, intra-molecular cyclization occurs, with the formation of end products - 1,3,4-oxadiazole-2-thions. The structures of the synthesized compounds were studied by 1H and 13C NMR spectroscopy. All synthesized substances are potentially biologically active compounds, since they contain several pharmacophore fragments in their structure.

Synthesis, Docking Studies into CDK-2 and Anticancer Activity of New Derivatives Based Pyrimidine Scaffold and Their Derived Glycosides

2019 ◽  
Vol 19 (13) ◽  
pp. 1093-1110 ◽  
Author(s):  
Adel A.H. Abdel Rahman ◽  
Ibrahim F. Nassar ◽  
Amira K.F. Shaban ◽  
Dina S. EL-Kady ◽  
Hanem M. Awad ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Human Liver ◽  
Docking Studies ◽  
Cyclin Dependent Kinase ◽  
Binding Interaction ◽  
Enzyme Active Site ◽  
Human Liver Cancer ◽  
Amino Derivatives ◽  
Activity Behavior ◽  
Derivatives Of

Background & Objective:New diaryl-substituted pyrimidinedione compounds, their thioxo derivatives as well as their bicyclic thiazole compounds were synthesized and characterized.Methods:The glycosylamino derivatives of the synthesized disubstituted derivatives of the pyrimidine scaffold were also prepared via reaction of the N3-amino derivatives with a number of monosaccharides followed by acetylation.Results:The anticancer activity of the synthesized compounds was studied against human liver cancer (HepG2) and RPE-1cell lines. Compounds 2a, 2b, 3a and 12 showed potent activities with IC50 results comparable to that of doxorubicin.Conclusion:Docking investigations into Cyclin-dependent kinase 2 (CDK-2) enzyme, a potential target for cancer medication, were also reported showing the possible binding interaction into the enzyme active site to support their activity behavior.

Thermal cyclocondensations of 3-N(4- and 5-benzimidazolyl and benztriazolyl)amino derivatives of 2-propenoic acid

1987 ◽  
Vol 52 (12) ◽  
pp. 2918-2925 ◽  
Author(s):  
Viktor Milata ◽  
Dušan Ilavský
Keyword(s):  
Uv Spectra ◽  
Propenoic Acid ◽  
Amino Derivatives ◽  
Derivatives Of ◽  
C Nmr ◽  
Ir And Uv Spectra

The cyclization of 3-N(4- and 5-benzimidazolyl and benztriazolyl)amino-2-cyano- and 2-ethoxycarbonyl-2-propenoate esters Ia, b-IVa, b under the conditions of the Gould-Jacobs reaction leads to angularly ring-fused substituted imidazo or triazolo[4,5-f] (V, VI) and [4,5-h] (VII, VIII) quinolines, respectively. The esters Vb-VIIIb have been transformed into the corresponding chloroderivatives Vc-VIIIc. 3-N(5-Benzimidazolyl and 5-benztriazolyl)amino-2-cyano-2-propenenitriles are cyclized in the presence of aluminium(III) chloride to give the aminoquinolines Vd, VId. The structure of the products has been characterized by their 1H, 13C NMR, IR, and UV spectra.

ChemInform Abstract: SYNTHESIS AND ANTITUMOR ACTIVITY OF 6-OXO-7-AMINO DERIVATIVES OF 5H-PYRIDO(2,3B)- AND 5H-PYRIMIDO(4,5B)(1,4)THIAZINES

1985 ◽  
Vol 16 (15) ◽  
Author(s):  
N. I. TRAVEN' ◽  
YU. A. ERSHOVA ◽  
A. S. SOKOLOVA ◽  
V. A. CHERNOV ◽  
T. S. SAFONOVA
Keyword(s):  
Antitumor Activity ◽  
Amino Derivatives ◽  
Derivatives Of

Synthesis of amino derivatives of resorcinols by a biogenetically similar scheme

1973 ◽  
Vol 22 (5) ◽  
pp. 1077-1082
Author(s):  
A. A. Akhrem ◽  
A. M. Moiseenkov ◽  
F. A. Lakhvich
Keyword(s):  
Similar Scheme ◽  
Amino Derivatives ◽  
Derivatives Of

Synthesis of 4-Amino Derivatives of 5-Oxoproline

2007 ◽  
Vol 2007 (25) ◽  
pp. 4257-4266 ◽  
Author(s):  
Victor P. Krasnov ◽  
Alexey Yu. Vigorov ◽  
Irina A. Nizova ◽  
Tatyana V. Matveeva ◽  
Alexander N. Grishakov ◽  
...  
Keyword(s):  
Amino Derivatives ◽  
Derivatives Of

Analogs and derivatives of tenoxicam. 1. Synthesis and antiinflammatory activities of analogs with different residues on the ring nitrogen and the amide nitrogen

1987 ◽  
Vol 30 (4) ◽  
pp. 678-682 ◽  
Author(s):  
Dieter Binder ◽  
Otto Hromatka ◽  
Franz Geissler ◽  
Karl Schmied ◽  
Christian R. Noe ◽  
...  
Keyword(s):  
Amide Nitrogen ◽  
Ring Nitrogen ◽  
Derivatives Of
Sign in / Sign up

Export Citation Format

Share Document