Research of antiherpes activity of aminopropanol-2 derivatives
Introduction. Chemotherapy and chemoprophylaxis are some of the main and often the only possible ways to effective control of viral infections. Therefore, the study of antiviral properties of new substances with the known chemical structure is one of the main ways to create new antiviral agents.
The aim of the study – to research the antiherpes activity of new aminopropanol-2 derivatives against the herpes simplex virus (HSV) antigenic type 1, strain VC.
Research Methods. Antiherpes activity was determined in 8 aminopropanol-2 derivatives: norbornyl containing substance (compound No. 51), substance with cyclic substituents in alkoxi group (compound No. 48), substances with alicyclic substituents in alkoxi group (compounds No. 46, 47, 49, 50, 52 and 53). Evaluation of antiherpes activity of the studied compounds was performed in vitro on cell culture VNK (growing culture of hamster kidney). Ability to reduce of virus infectious titer and chemotherapeutic index (HTI) of the studied compounds was determined.
Results and Discussion. It is established that the compound No. 53 inhibits HSV-I reproduction in 2 lg ID50 at a concentration of 1.56 µg/ml. HTI of compound No. 53 is equal to 64, which describes it as an effective inhibitor of HSV-I reproduction. Some antiherpes action in compounds No. 46, 47 and 51 was identified also, their HTI were 8, 4 and 4 respectively. Substances No. 48, 49, 50 and 52 do not show the antiherpes action.
Conclusions. Among all tested aminopropanol-2 derivatives the compound No. 53 with clear antiherpes properties was determined. Compound No. 53 belongs to the substances with alicyclic substituents in alkoxi group and has such chemical formula: 1-(2-methyl-3-butinox)-3-(126.96.36.199-tetramethyl piperidine)-2-propanol hydrochloride. Compound No. 53 as alicyclic substituent in alkoxy group contains 2-methyl-3-butene, and amine moiety of this substance contains the radical 188.8.131.52 – tetramethylpiperidine. The obtained results will be useful in establishing the natural relationships "structure-activity", also it can be used to create active compounds with certain characteristics.
Dzublik I. V. (eds.). (2004). Posibnik z himioterapii virusnih infekcij [ Guide chemotherapy of viral infections]. Kyiv: Olprint [in Ukrainian].
Looker K. J., Garnett GP. (2005). A systematic review of the epidemiology and interaction of herpes simplex virus types 1 and 2. Sex. Transm. Infect., 81(2), 103–107.
Coleman J.L., Shukla D. (2013). Recent advances in vaccine development for herpes simplex virus types I and II. Hum Vaccin Immunother., 9(4), 729–735.
Wilson A.C., Mohr I.. (2012). A cultured affair: HSV latency and reactivation in neurons. Trends Microbiol., 20, 604-11.
Kasjan L.I., Palchikov V. A. (2010). Aminospirty s karkasnimy fragmentami. Sintez, reakcii I puti ispolzovanija [The amino alcohols of frame fragments. Synthesis, reactions and ways of using]. Jurn. Org. Himii - Journal Organic Chemistry, 46(1), 7-43 [in Russian].
Alimardanov Kh. M., Sadygov O. A. & Suleimanova E. T. (2009). Sintez i issledovanie antimikrobnih svojstv aminometilirovanih proizvodnih C6−C7 alkil diolov [Synthesis and Examination of Antimicrobial Properties of Aminomethylated Derivatives C6−C7 of Alicyclic Diols]. Jurnal prikladnoj himii - Journal of Applied Chemistry, 82(7), 1121-1125 [in Russian]
Korotkiy Yu.V., Vrinchanu N.O. & Dronova M.L. (2015). Sintez, antibakterialna ta antifungalna aktivnist pohidnih 1|4 (1,1,3,3, tetrametylbutyl) fenoxi|3 dialkilamino 2 propanol [Synthesis, antibacterial and antifugul activity of derivatives of 1|4 (1,1,3,3, tetrametylbutyl) fenixi|3 dialkilamino 2 propanol]. Farmacevtichnij jurnal - Pharmaceutical journal,1, 56-62 [in Ukrainian].
Stefanov A.V. (eds.). (2001). Vivchennja fntivirusnoi dii potencijnih likarskih zasobiv. Metodichni rekomendacii [Study of the antiviral action of potential medical remedies. Method. recommendations]. Kyiv [in Ukrainian].
Muthannan A.R. (2016). Determination of 50% endpoint titer using a simple formula. World J. Virol., 5(2), 85-86.
Volyansky Yu. l., Gritsenko I. S. & Shirobokov V. P. (2004). Vivchennja Specifichoi activnosty protimicrobnih likarskih zasobiv. Metodichni rekomendacii [Study of the specific activity of antimicrobial drugs. Method. Recommendations]. Kyiv [in Ukrainian].
Copyright (c) 2017 Medical and Clinical Chemistry
This work is licensed under a Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 International License.