Synthesis of new derivatives of 10H-benzo[b]pyridazino[3,4-e][1,4]thiazines

2015 ◽  
Vol 21 (4) ◽  
pp. 215-218 ◽  
Author(s):  
Zahra Arghiani ◽  
Seyed Mohammad Seyedi ◽  
Mehdi Bakavoli ◽  
Mohsen Nikpour
Keyword(s):  
Secondary Amine ◽  
Inhibitory Activity ◽  
Sequential Treatment ◽  
Derivatives Of ◽  
Sodium Amide

AbstractNew 10H-benzo[b]pyridazino[3,4-e][1,4]thiazines were prepared and evaluated for inhibitory activity against soybean 15-lipoxygenase enzyme. These compounds were synthesized by the sequential treatment of 4-bromo-3,6-dichloropyridazine with 2-aminothiophenol and a secondary amine with the subsequent heterocyclization in the presence of sodium amide.

Synthesis of N4-Substituted Derivatives of 1-[2-(Phosphonomethoxy)ethyl]cytosine and Its Diisopropyl Ester as a Model Reaction for the Synthesis of N4-Substituted Derivatives of Cidofovir

2005 ◽  
Vol 70 (12) ◽  
pp. 2066-2074 ◽  
Author(s):  
Šárka Chalupová ◽  
Antonín Holý ◽  
Milena Masojídková
Keyword(s):  
Secondary Amine ◽  
Model Reaction ◽  
Aqueous Methanol ◽  
Derivatives Of ◽  
Amine Salts

We have studied the reaction of 1-[2-(phosphonomethoxy)ethyl]cytosine (1) and its diisopropyl ester (2) with triethylammonium hydrogensulfite in 60% aqueous methanol. In the presence of some primary or secondary amine salts, at 25-70 °C, this reaction affords transaminated derivatives 4a-4e and 5a, 5b as main products accompanied by uracil compounds. However, with certain amines the reaction failed.

Synthesis and investigation of viral-inhibitory activity of nitrogen-containing derivatives of adamantane

1991 ◽  
Vol 25 (7) ◽  
pp. 485-488 ◽  
Author(s):  
Yu. N. Klimochkin ◽  
I. K. Moiseev ◽  
G. V. Vladyko ◽  
L. V. Korobchenko ◽  
E. I. Boreko
Keyword(s):  
Inhibitory Activity ◽  
Derivatives Of

Synthesis and antibacterial evaluation of novel Schiff's base derivatives of nitroimidazole nuclei as potent E. coli FabH inhibitors

RSC Advances ◽  
2014 ◽  
Vol 4 (97) ◽  
pp. 54217-54225 ◽  
Author(s):  
Xin Zhang ◽  
Chetan B. Sangani ◽  
Li-Xin Jia ◽  
Pi-Xian Gong ◽  
Fang Wang ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Schiff’S Base ◽  
E Coli ◽  
Derivatives Of ◽  
Antibacterial Evaluation ◽  
Potent Inhibitory Activity

Series of novel Schiff's base derivatives have been synthesized. Compound 10q showed the most potent inhibitory activity (IC50 = 2.6883 μM).

Derivatives of 3′-and 5′-Deoxyadenosine: Their Inhibitory Activity against DNA Viruses

Chemotherapy ◽  
1980 ◽  
Vol 26 (5) ◽  
pp. 316-322 ◽  
Author(s):  
Barbara Grytzmann ◽  
M. Morr ◽  
R. Wigand
Keyword(s):  
Inhibitory Activity ◽  
Dna Viruses ◽  
Derivatives Of

Glutathione S-Transferase, Acetylcholinesterase Inhibitory and Antibacterial Activities of Chemical Constituents of Barleria prionitis

2007 ◽  
Vol 62 (4) ◽  
pp. 580-586 ◽  
Author(s):  
Kalhari S. Kosmulalage ◽  
Shamsulhaq Zahid ◽  
Chibuike C. Udenigwe ◽  
Sarfraz Akhtar ◽  
Athar Ata ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Chemical Constituents ◽  
Ethanolic Extract ◽  
Antibacterial Activities ◽  
Spectroscopic Studies ◽  
Sri Lankan ◽  
Glutathione S Transferase ◽  
Ache Inhibitory Activity ◽  
Phytochemical Studies ◽  
Derivatives Of

Phytochemical studies on the ethanolic extract of Barleria prionitis of Sri Lankan origin have resulted in the isolation of a new compound, balarenone (1), along with three known compounds, pipataline (2), lupeol (3) and 13,14-seco-stigmasta-5,14-diene-3-α-ol (4). The structures of 1 - 4 were elucidated with the aid of extensive NMR spectroscopic studies. Compounds 1 - 4 showed moderate inhibitory activity against glutathione S-transferase (GST) and acetylcholinesterase (AChE). Compounds 1, 2 and 4 also exhibited antibacterial activity against Bacillus cereus and Pseudomonas aeruginosa (25 μg/disk). Three different derivatives of compound (2), 7,8-epoxypipataline (5), 8- amino-7-hydroxypipataline (6) and 7,8-dibromopipataline (7) were synthesized to evaluate them for GST and AChE inhibitory activities. Household microwave radiations were used to synthesize compound (6). Among all tested compounds, 8-amino-7-hydroxypipataline (6) exhibited a significant AChE inhibitory activity with an IC50 value of 36.8 μM.

Synthesis and MDR inhibitory activity evaluation of derivatives of schizandrin A

2010 ◽  
Vol 12 (7) ◽  
pp. 549-556 ◽  
Author(s):  
Xiao-Xia Liang ◽  
Geng-Tao Liu ◽  
Qiao-Hong Chen ◽  
Hua Sun ◽  
Dong-Lin Chen ◽  
...  
Keyword(s):  
Inhibitory Activity ◽  
Activity Evaluation ◽  
Derivatives Of

Synthesis and Biological Evaluation of Acetylcholinesterase Inhibitor Macakurzin C and Its Derivatives

Synlett ◽  
2015 ◽  
Vol 26 (08) ◽  
pp. 1131-1134 ◽  
Author(s):  
Hyoungsu Kim ◽  
Seung-Hoon Baek ◽  
Hongjun Jang
Keyword(s):  
Inhibitory Activity ◽  
Acetylcholinesterase Inhibitor ◽  
Biological Evaluation ◽  
Hydroxyl Groups ◽  
Structural Requirements ◽  
Ache Inhibitory Activity ◽  
Synthesis And Biological Evaluation ◽  
Derivatives Of

The derivatives of macakurzin C containing a modified D ring and protected C(3)/C(5)-hydroxyl groups were synthesized and their in vitro AChE inhibitory activity and neurotoxicity were evaluated to identify the structural requirements for the activities. The results indicated that C(3)-benzyl-protected derivative has a more potent AChE inhibitory activity (IC50, 2.6 μM) and a less neurotoxicity (GI50, >100 μM) than synthetic macakurzin C (IC50, 9.1 μM; GI50, 16.6 μM).

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