ChemInform Abstract: Synthesis of New Pyrrole and Pyrrolo[2,3-d]pyrimidine Derivatives of Potential Antioxidant Activity.

ChemInform ◽  
2010 ◽  
Vol 42 (2) ◽  
pp. no-no
Author(s):  
Khairy Abdelhameed Mohsen El-Bayouki ◽  
Wahid Mohmoud Basyouni ◽  
Eslam Attya Mostafa
2010 ◽  
Vol 75 (8) ◽  
pp. 813-834 ◽  
Author(s):  
Khairy Abdelhameed Mohsen El-Bayouki ◽  
Wahid Mohmoud Basyouni ◽  
Eslam Attya Mostafa

New 2-amino-3-cyanopyrrole derivatives were prepared and converted to 7-deazapurines. 7-Deazaadenine 6 was synthesized by different methods and alkylated with alkyl iodides to afford the quaternized 3-alkylpyrrolopyrimidinium iodide salts 8. The latter salts were dequaternized to N-alkylpyrrolo[2,3-d]pyrimidin-4-amines 12. Compounds 12 were identical to the products obtained from reactions of 4-chloro-7-(4-fluorophenyl)-5-p-tolyl-7H-pyrrolo[2,3-d]pyrimidine 11 with methyl- or ethylamine in the presence of a catalyst. The thione 13 and its related 4-methylthio- and 4-ylcarbonothioate derivatives 14a, 14b were obtained. The triazolo- 17a–17e, benzenesulfonamido- 19, and tetrazolopyrrolopyrimidine 21 derivatives were synthesized. Several examples of the synthesized pyrrole- and pyrrolo[2,3-d]pyrimidine derivatives showed high to remarkable antioxidant scavenging activity as measured by their ability to scavenge the 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical


2019 ◽  
Vol 18 (10) ◽  
pp. 1417-1424 ◽  
Author(s):  
Emilia Naydenova ◽  
Diana Wesselinova ◽  
Svetlana Staykova ◽  
Ivan Goshev ◽  
Ljubomir Vezenkov

Background: Based on the structure of RC-121 (D-Phe-c (Cys-Tyr-D-Trp-Lys-Val-Cys)-Thr-NH2, - synthetic derivatives of somatostatin), some analogs were synthesized and tested for in vitro cytotoxic and antioxidant activity. Objectives: The new analogs were modifyed at position 5 with Dap (diaminopropanoic acid), Dab (diaminobutanoic acid) and Orn and at position 6 with the unnatural amino acids Tle (t-leucine). Methods: The in vitro cytotoxic effects of the substances were investigated against a panel of human tumor cell lines HT-29 (Human Colorectal Cancer Cell Line), MDA-MB-23 (Human Breast Cancer Cell Line), Hep G-2 (Human Hepatocellular Carcinoma Cell Line) and HeLa (cervical cancer cell line). The antioxidant capacities were tested by ORAC (Oxygen Radical Antioxidant Capacity) and HORAC (Hydroxyl Radical Averting Capacity) methods. Results: All substances expressed significantly higher antioxidant capacity by comparison with galic acid and Trolox. All substances showed considerable antioxidant capacity as well. Compound 2T (D-Phe-c(Cys-Tyr-DTrp- Dap-Tle-Cys)-Thr-NH2)had the highest antioxidant effect. The compound 4T (D-Phe-c(Cys-Tyr-D-Trp- Orn-Tle-Cys)-Thr-NH2) displayed antiproliferative effect on HeLa cells with IC50 30 µM. The peptide analog 3T (D-Phe-c(Cys-Tyr-D-Trp-Lys-Tle-Cys)-Thr-NH2) exerted the most pronounced inhibition on the cell vitality up to 53%, 56% and 65% resp. against MDA-MB-23, Hep G-2, HeLa in the higher tested concentration. Conclusion: The somatostatin analogs showed moderate influence on the vitality of different tumor cells and could be used in changing their pathology.


1992 ◽  
Vol 37 (1) ◽  
pp. 1-5 ◽  
Author(s):  
J.-M. Herdan ◽  
Liana Cira ◽  
Maria Giurginca ◽  
G. Ivan

ChemInform ◽  
2013 ◽  
Vol 44 (16) ◽  
pp. no-no
Author(s):  
Y. Kotaiah ◽  
N. Harikrishna ◽  
K. Nagaraju ◽  
C. Venkata Rao

2017 ◽  
Vol 0 (3(91)) ◽  
pp. 61-65
Author(s):  
V. A. Volkovoy ◽  
O. V. Sevrukov ◽  
S. V. Kolisnyk ◽  
N. V. Derkach ◽  
S. I. Kryzhna ◽  
...  

1993 ◽  
Vol 74 (3) ◽  
pp. 193-197
Author(s):  
Yu. D. Slabnov ◽  
D. A. Valimukhametova ◽  
A. P. Tsibulkin ◽  
R. F. Khamitov

The effect of xymedon on immunologic indices and external respiration function in combined treatment of patients with acute pnemonia is studied. The use of xymedon in the presence of basis therapy in patients with lingering pneumonia with reduced immunologic reactivity exerts a stimulating effect on the indices of cellular and humoral immunity. This effect is revealed in the stabilization period of pneumonia accompanied by positive clinicoroentgenologic shifts, provides a higher increase of the indices of external respiration function, reduces the terms of recovery of patients. Xymedon does not cause side effects. The drug may be recommended for a wider use in the clinic in patients with unspecific diseases of the lungs.


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