Organic Chemistry: Current Research
Open Access

New (aminomethylene) bisphosphonates obtained from heterocyclic amines and their biological activity

4^th European Organic Chemistry Congress

March 01-03, 2018 | London, UK

Patrycja M Petruczynik and PaweÃ?Â? Kafarski

WrocÃ?Â?aw University of Science and Technology, Poland

Posters & Accepted Abstracts: Organic Chem Curr Res

Abstract :

Bisphosphonic acids are stable analogues of inorganic pyrophosphate, wherein an oxygen bridge P-O-P is replaced by substituted carbon atom. (Aminomethylenebisphosphonates) have found wide applications as therapeutic agents in the treatment of diseases associated with dysfunction of the calcium metabolism, such as: osteoporosis, Paget's disease or hypercalcemia. Recently, most literature reports concentrate on new biological properties of these com-pounds, especially their evaluation as inhibitors of enzymes being the targets for drug development. The three-component condensation between amines, triethyl orthoformate and diethyl phosphate is perhaps the simplest and most commonly used preparation of N-substituted (aminomethylene) bisphosphonic acids. The studies have shown that application of heterocyclic amines. Such as triazole derivatives or purine base, in three-component condensation can give unexpected products having very interesting chemical structure. The biological studies have been shown that these compounds can play a role as potential antiosteoporotic agent in the treatment of diseases associated with calcium metabolism. Recent Publications 1. Miszczyk P, Wieczorek D, GaÃ?Â?Ã?Â?zowska, Dziuk, Wietrzyk, et al. (2017) Reaction of 3-Amino-1,2,4-triazole with diethyl phosphite and triethyl orthoformate: acid-base properties and antiosteoporotic activities of the products. Molecules 22:254. 2. Chmielewska E and Kafarski P (2016) Physiologic activity of bisphosphonates-recent advances. Open Pharm. Sci. J. 3:56. 3. DÃ?Â?browska E, BurzyÃ?Â?ska, Mucha A, Matczak-Jon E, Sawka-Dobrowolska W, et al. (2009) Insight into the mechanism of three component condensation leading to aminomethylenebisphosphonates. J. Organomet. Chem. 694:3806.

Biography :

Patrycja M Petruczynik is a PhD student in the Department of Bioorganic Chemistry at Wroclaw University of Technology. She has her expertise in synthesis of biologically active of (aminomethylene) bisphosphonates and aminophosphonates. She has tested and isolated unexpected products in three component condensation of amines, diethyl phosphate and triethyl orthoformate and explained of mechanism reaction.
Email:patrycja.petruczynik@pwr.edu.pl