80 research outputs found
Ternary Copper(II) Complexes With Indomethacin, a Potent Non-Steroidal Antiinflammatory Drug. Crystal Structure of Bis (Dimethylformamide)-Tetrakis[1-(4-Chlorobenzoyl)-5-Methoxy-2-Methyl-1-H-Indole-3-Acetato]Dicopper(II). Antiinflammatory Properties and Prevention of Gastrointestinal Side Effects by Nanocapsules
Two ternary copper(ll) complexes of indomethacin [1-(4-chlorobenzoyl)-5-methoxy-2-
methyl-1-H-indole-3-acetic acid] called hereafter lndo, were prepared and characterized by single
crystal X-ray diffraction. The first complex Cu2(Indo)4(DMF)2 I crystallizes in space group P-1 (a =
10.829(2), b = 13.379(2), c = 16.491(3) Å; α = 105.58(2), β = 101.06(2), γ = 106.96(2)°; V= 2104.6(6) Å3, Z= 1). The title molecule is a centrosymmetric binuclear complex, with Cu atoms
bridged by the carboxylate moieties of four indomethacinate ligands. The four nearest O atoms
around each Cu atom form a square planar arrangement with the square pyramidal coordination
completed by the O atom of N,N′-dimethylformamide. Daily administration for seven days of 1 mg/kg
of indomethacin, I and I encapsulated into liposomes induces a weak inflammation of rat gastrointestinal
tract. I was less inflammatory than indomethacin but the better protection was brought by
encapsulation of the compound. This might be of interest in sustained therapies of chronic
inflammatory diseases
In Vivo Nitric Oxide Synthase Inhibitors Can Be Deprived of This Activity: Unexpected Influence of the Tetrachloroplatinate(II) Counteranion. Crystal Structures of Bis(S-Methyl-Isothiouronium)-N,N′-Bis(3-Guanidinopropyl)Piperazinium and Hexamidinium Tetrachloroplatinates(II) Salts
The synthesis and crystal structures of bis(S-methylisothiouronium) (MSTUH)+, N,N′-bis((3-
guanidinopropyl)piperazinium (PipeC3GuaH4)4+ and hexamidinium (HexaH2)2+ tetrachloro platinate(ll) salts ( called hereafter PtMSTU, PtPipeC3Gua and PtHexa respectively ) were
investigated. These compounds contain the “amidine” function ( - C(=NH)NH2 ) in which the H
atoms supplied by the acid have become attached to the imino group of each terminal amidino
function. Moreover, in PtPipeC3Gua, the nitrogen atoms of the chair-piperazine moiety are also
protonated. The influence of tetrachloroplatinate(ll) counteranion ( versus sulfate, nitrate and
diisethionate ) in the in vivo nitrite inhibition by the (MSTUH)+, (PipeC3GuaH4)4+ and (HexaH2)2+ cations was investigated. The three tetrachloroplatinate(ll) salts, unexpectedly, do not inhibit
significantly the in vivo nitrite production in comparison with the other salts (sulfate, nitrate and
diisethionate and their corresponding previous countercations) which exhibit NO synthase
inhibition, especially bis(S-methylisothiouronium) sulfate, a selective and potent inducible NO
synthase (iNOS) inhibitor commonly used as standard
In Vivo Inhibition of Nitric Oxide Synthase by Bisisothiouronium and Bisguanidinium Salts
Peer Reviewe
Effect of an Encapsulated Anti-Elastase Compound on Experimental Gingival Inflammation in the Rat
Peer Reviewe
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