Organophosphorus compounds with anti-inflammatory and analgesic activity (review)

1993 ◽  
Vol 26 (7-8) ◽  
pp. 565-575 ◽  
Author(s):  
V. Kh. Syundyukova ◽  
E. G. Neganova ◽  
B. K. Beznosko ◽  
E. N. Tsvetkov
Planta Medica ◽  
2013 ◽  
Vol 79 (13) ◽  
Author(s):  
GO Ajayi ◽  
O Salako ◽  
IM Mosebolatan

Planta Medica ◽  
2007 ◽  
Vol 73 (09) ◽  
Author(s):  
S Nualkaew ◽  
S Thongpraditchote ◽  
Y Wongkrajang ◽  
K Rattanamanee

2020 ◽  
Vol 258 ◽  
pp. 112936 ◽  
Author(s):  
Ahlem Karbab ◽  
Kamel Mokhnache ◽  
Soraya Ouhida ◽  
Noureddine Charef ◽  
Farida Djabi ◽  
...  

1974 ◽  
Vol 27 (4) ◽  
pp. 815 ◽  
Author(s):  
DJ Collins ◽  
LE Rowley ◽  
JM Swan

1-Hydroxy-1,2,3,4-tetrahydrophosphinoline 1-oxide (2a) was converted via the corresponding acid chloride (2b) into the 1-vinylphosphine oxide (3) which underwent a Michael-like addition with dimethylamine to give 1-(2'-dimethylaminoethyl)-1,2,3,4-tetrahydrophosphinoline 1-oxide (6). The successive reduction of (6) with trichlorosilane, and oxidation with sulphur afforded the phosphine sulphide (7). The reaction of 1-vinyl-1,2,3,4-tetrahydrophosphinoline 1-oxide (3) with N-bromosuccinimide followed by treatment with dimethylformamide gave 1-vinyl-1,2-dihydrophosphinoline 1-oxide which, under mild conditions, underwent Michael-like addition of amines to the vinyl group to give, for example, 1-(2'-propylaminoethy1)-1,2-dihydrophosphinoline 1-oxide. When heated in a sealed tube at 140-150° in water for 60 h this amine was converted into 4-propyl-1,2,3,4,5,6-hexa- hydro-1,5-methano-4,1-benzazaphosphocine 1-oxide. Several related tricyclic compounds including the corresponding phosphines and phosphine sulphides were synthesized. Several of the new aminophosphorus compounds were tested for analgesic activity.


2015 ◽  
Vol 21 (5) ◽  
pp. 273-278 ◽  
Author(s):  
Grażyna Chłoń-Rzepa ◽  
Agnieszka W. Jankowska ◽  
Małgorzata Zygmunt ◽  
Krzysztof Pociecha ◽  
Elżbieta Wyska

AbstractA series of new 8-alkoxy-1,3-dimethyl-2,6-dioxopurin-7-yl-substituted acetohydrazides and butanehydrazides 6–12 was synthesized and evaluated for the analgesic activity in two in vivo models: the writhing syndrome and the hot-plate tests. Among the investigated derivatives, compounds with N′-arylidenehydrazide moiety 9–12 show analgesic activity significantly higher than that of acetylsalicylic acid, which may indicate the importance of this structural element for analgesic properties. The lack of the activity in the hot-plate test may suggest that the analgesic activity of the newly synthesized compounds is mediated by a peripheral mechanism. The selected compounds 7 and 12 inhibit tumor necrosis factor α production in a rat model of lipopolysaccharide-induced endotoxemia, similarly to theophylline, which may confirm their anti-inflammatory properties.


Il Farmaco ◽  
2001 ◽  
Vol 56 (5-7) ◽  
pp. 455-457 ◽  
Author(s):  
Ada Trovato ◽  
Eugenio Raneri ◽  
Maria Kouladis ◽  
Olga Tzakou ◽  
Maria Fernanda Taviano ◽  
...  

Author(s):  
Sarath Sasi Kumar ◽  
Anjali T

Objective: In silico design and molecular docking of 1,2-benzisoxazole derivatives for their analgesic and anti-inflammatory activity using computational methods.Methods: In silico molecular properties of 1,2-benzisoxazole derivatives were predicted using various software’s such as Chemsketch, Molinspiration, PASS and Schrodinger to select compounds having optimum drug-likeness, molecular descriptors resembling those of standard drugs and not violating the ‘Lipinski rule of 5’. Molecular docking was performed on active site of nicotinic acetylcholine receptor (PDB: 2KSR) for analgesic activity and COX-2 (PDB: 6COX) for anti-inflammatory activity using Schrodinger under maestro molecular modelling environment.Results: From the results of molecular docking studies of 1,2-benzisoxazole derivatives, all the compounds showed good binding interactions with Nicotinic acetylcholine receptor and COX-2. Compounds 4a and 4c showed highest binding scores (-7.46 and-7.21 respectively) with nicotinic acetylcholine receptor and exhibited maximum analgesic activity. Compound 4a showed highest binding score (-7.8) with COX-2 and exhibited maximum anti-inflammatory activity.Conclusion: All the derivatives of 1,2-benzisoxazole showed good analgesic and anti-inflammatory activity as predicted using molecular docking on respective receptors.


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