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Chemoenzymatic synthesis of enantiomerically enriched diprophylline and xanthinol nicotinate.
Bioorg Chem
January 2021
Warsaw University of Technology, Faculty of Chemistry, Department of Inorganic Chemistry and Solid State Technology, Noakowskiego 3, 00-664 Warsaw, Poland.
A concise chemoenzymatic route toward enantiomerically enriched active pharmaceutical ingredients (API) - diprophylline and xanthinol nicotinate - is reported for the first time. The decisive step is an enantioselective lipase-mediated methanolysis of racemic chlorohydrin-synthon acetate, namely 1-chloro-3-(1,3-dimethyl-2,6-dioxo-1,2,3,6-tetrahydro-7H-purin-7-yl)propan-2-yl acetate, performed under kinetically-controlled conditions on a preparative 500 mg-scale. The best results in terms of reaction enantioselectivity (E = 14) were obtained for the enantiomers resolution performed with lipase type B from Candida antarctica immobilized on acrylic resin (CAL-B, Novozym 435) suspended in homophasic acetonitrile-methanol mixture.
View Article and Find Full Text PDFComparative results of treatment of thrombotic complications in the injured persons with combined trauma of trunk in two groups were adduced. The scheme of prophylax3 is and treatment of thrombotic complications was proposed; application of this scheme have permitted to reduce their rate in 5 times, from 54.5 to 11.
View Article and Find Full Text PDFInhibited proliferation of human umbilical artery smooth muscle cells by xanthinol nicotinate.
Med Biol Eng Comput
June 2016
Department of Pharmacy, The Second Affiliated Hospital of Harbin Medical University, 148 Baojian Road, Harbin, 150086, Heilongjiang Province, China.
Vascular smooth muscle cell proliferation is a key event in the development of hypertension, instant restenosis and other cardiac disorders. Inhibition of this proliferation could lead to better prevention and treatment of these diseases. This study was designed to investigate the effects and mechanisms of different concentrations of xanthinol nicotinate (XN) on human umbilical artery smooth muscle cell (HUASMC) proliferation in vitro.
View Article and Find Full Text PDFIntroduction: Sudden hearing loss is a clinical entity of ambiguously defined aetiology manifested by hearing loss of more than 30 dB on three contiguous frequencies occurring within 72 hours. The lack of standard therapy protocol led to the use of variety of different therapies, thus making difficult objective quantification of their effect.
Objective: The aim of the study was to present our experience in the treatment of sudden hearing loss with administration of vasoactive and corticosteroid therapy.
The study comprised a total of 107 patients (all men) after endured femoropopliteal bypass grafting above the genicular fissure with a synthetic stent graft manufactured by the Gore Company for stage IIB and III chronic arterial insufficiency of the lower extremities according to the Fontain-Pokrovsky classification. Group One I (control group) was composed of fifty-four patients permanently taking in the postoperative period at the out-patient stage pentoxiphylline (trental 400 mg 1 tablet 3 times daily) and xantinol nicotinate at a dose of 150 mg one tablet thrice daily. Group Two (Study Group) consisted of fifty-three patients taking after reconstructive vascular surgery at the out-patient stage in addition to pentoxiphylline and xantinol nicotinate acetylsalicylic acid (cardiomagnil 75 mg 1 tablet once daily).
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