Synthesis of new representatives of 11,12-dihydro-5H-5,11-epoxybenzo[7,8]oxocino[4,3-b]pyridines – structural analogues of integrastatins A, B

2021 ◽  
Vol 45 (7) ◽  
pp. 3559-3569
Author(s):  
Ivan V. Kulakov ◽  
Alena L. Stalinskaya ◽  
Semyon Y. Chikunov ◽  
Yuri V. Gatilov
Keyword(s):  
Structural Analogues ◽  
Ring Oxidation ◽  
Methylene Group

The reaction of 3,5-diacetyl-2,6-dimethylpyridine with substituted salicylic aldehydes leads to the formation of the epoxybenzooxocine ring. Oxidation of the methylene group with H2SeO3 opens ways to obtaining structural analogs of natural integrastatins A, B.

EHT study of reactivity of methylene group in 1-methyl-1,4-dihydronicotinamide

1980 ◽  
Vol 45 (9) ◽  
pp. 2425-2432
Author(s):  
Jiří Krechl ◽  
Josef Kuthan
Keyword(s):  
Heterocyclic Ring ◽  
Covalent Bonds ◽  
Electronic Mechanism ◽  
Methylene Group ◽  
Plane Form ◽  
Reaction Profile

It has been demonstrated that the EHT method predicts an almost plane form of the heterocyclic ring in 1-methyl-1,4-dihydronicotinamide I (R = CH3) and also reflects satisfactorily character of the covalent bonds in the 4-methylene group. An attempt has been made of calculation of the reaction profile of elimination of the centre 4', and electronic mechanism of its splitting off is discussed.

Supramoleküle aus Kronenethern und geminalen Sulfonen: Synthese von vier binären Komplexen und Kristallstruktur von (CH2CH2O)4·2H 2C(SO2C2H5)2/Supramolecules of Crown Ethers with Geminal Sulfones: Synthesis of Four Binary Complexes and Crystal Structure of (CH2CH2O )4·2H2C(SO2C2H5)2

1995 ◽  
Vol 50 (7) ◽  
pp. 1018-1024 ◽  
Author(s):  
Axel Michalides ◽  
Dagmar Henschel ◽  
Armand Blaschette ◽  
Peter G. Jones
Keyword(s):  
Monoclinic Space Group ◽  
Triclinic Space Group ◽  
Space Group ◽  
X Ray ◽  
X Ray Crystallography ◽  
H Nmr ◽  
Binary Complexes ◽  
Cyclic Polyethers ◽  
Adjacent Unit ◽  
Methylene Group

In a systematic search for supramolecular complexes involving all combinations of the cyclic polyethers 12-crown-4 (12C4), 15-crown-5 (15C 5), 18-crown-6 (18C 6) and dibenzo- 18-crown-6 (DB -18C6), and the geminal di- or trisulfones H2C(SO 2Me)2, H2C (SO2Et)2 and HC (SO2Me)3-n (SO2Et)n (n = 0 -3 ) , only the following four complexes could be isolated and unequivocally characterized by elemental analysis and 1H NMR spectroscopy: [(12C4){H2C (SO2Et)2}2] (3), [(18C6){H2C (S O2Me)2}] (4), [(DB -18C 6){H2C (SO2Et)2}] (5) and [(D B -18C 6)2{HC (SO2Me )(SO2Et)2}3] (6). The structure of 3 (triclinic, space group P1̄) consists of crystallographically centrosymmetric formula units, in which the disulfone molecules are bonded on each side of the ring by two C -H ··· O(crown) interactions originating from the central methylene group (H···O 213 pm) and from the methylene group of one EtSO2 moiety ( H ··· O 237 pm). Formula units related by translation are connected into parallel strands by a third type of reciprocal C -H ···O bond (H ···O 232 pm) between the second H atom of the central methylene group and a sulfonyl oxygen atom of the adjacent unit. The structure of 4 (monoclinic, space group C2/c) showed severe disorder of the crown ether and could not be refined satisfactorily. Compounds 5 and 6 crystallized as long and extremely thin fibres, indicative of linear-polymeric supramolecular structures; single crystals for X-ray crystallography were not available.

The Application of Molecularly Imprinted Polymers to Solid-Phase Extraction

2014 ◽  
Vol 893 ◽  
pp. 283-286
Author(s):  
Hong Ying Pei ◽  
Gui Jun Shen ◽  
Yu Du
Keyword(s):  
Solid Phase Extraction ◽  
Molecularly Imprinted Polymers ◽  
Biological Samples ◽  
Solid Phase ◽  
Phase Extraction ◽  
Molecularly Imprinted ◽  
Imprinted Polymers ◽  
Structural Analogues ◽  
Environmental And Biological Samples

A benefit of imprinted polymers is the possibility to prepare sorbents with selectivity pre-determined for a particular substance, or group of structural analogues. The application most close to a wider acceptance is probably that of solid phase extraction for clean-up of environmental and biological samples. The technique of molecularly imprinted polymers to solid phase extraction (MISPE) is performance and high selectively, compared with traditional sorbents. In this paper, the preparation and application of MIPs would be reviewed.

The Effect of Practolol, In Vitro Generated Metabolites of Practolol and Chemical Analogues on the Rate of Growth of Human Skin Fibroblasts

1984 ◽  
Vol 12 (2) ◽  
pp. 89-97
Author(s):  
Graham R. Elliott ◽  
H.E. Amos ◽  
James W. Bridges
Keyword(s):  
Human Skin ◽  
Psoriasis Patient ◽  
Skin Fibroblasts ◽  
Human Skin Fibroblasts ◽  
Cell Type ◽  
Normal Human Skin ◽  
Rate Of Growth ◽  
Structural Analogues ◽  
Normal Human

The rate of growth of normal human skin fibroblasts was inhibited in a dose related, reversible, fashion by practolol (N-4-(2-hydroxy)-3 (1-methyl)-aminopropoxyphenylacetamine) (ID50 1.35 ± 0.14 x 10-3M), propranolol (1-(isopropylamino)-3(1-naphthyl-oxy)-2-propranolol) (ID50 0.145 ± 0.02 x 10-3M) and paracetamol (N-(4-hydroxyphenyl) acetamide) (ID50 0.85 ± 0.2 x 10-3M). Skin fibroblasts isolated from a psoriasis patient were more sensitive towards practolol (ID50 0.48 ± 0.14 x 10-3M) and propranolol (ID50 0.032 ± 0.002 x 10-3M), but less sensitive towards paracetamol (ID50 1.3 ± 0.07 x 10-3M). In vitro generated metabolites of practolol, using normal or Arochlor 1254-pretreated hamster liver preparations, and structural analogues of practolol had no effect upon the growth of either cell type.

Pyrimidine Syntheses. I. Reaction of s-Triazine with Imidates and Amidines Containing an Acidic α-Methylene Group

1962 ◽  
Vol 27 (2) ◽  
pp. 548-551 ◽  
Author(s):  
FRED C. SCHAEFER ◽  
K. ROBERT HUFFMAN ◽  
GRACE A. PETERS
Keyword(s):  
Methylene Group

Synthesis, molecular modeling study, preliminary antibacterial, and antitumor evaluation of N-substituted naphthalimides and their structural analogues

2012 ◽  
Vol 22 (5) ◽  
pp. 2360-2375 ◽  
Author(s):  
Adel S. El-Azab ◽  
Amer M. Alanazi ◽  
Naglaa I. Abdel-Aziz ◽  
Ibrahim A. Al-Suwaidan ◽  
Magda A. A. El-Sayed ◽  
...  
Keyword(s):  
Molecular Modeling ◽  
Molecular Modeling Study ◽  
Structural Analogues ◽  
Antitumor Evaluation ◽  
Modeling Study
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