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Information × Registration Number 0216U001777, 0113U000741 , R & D reports Title Search of effective toсolytics and selective detrusor spasmolytic drugs among heterocyclic structures with two atoms of Nitrogen. popup.stage_title Head Mochort Nikolay Antonovich; Demchenko Anatoly Mikhailovich, Registration Date 18-04-2016 Organization State Establishment "Institute of Pharmacology and Toxicology National Academy of Medical Science of Ukraine" popup.description2 The subjects of investigation are compounds for pharmacological treating of pathology states accompanied by smooth muscle spasm (namely: premature labour and overactive bladder). Study objective is to investigate tocolytic activity and detrusor selectivity of leader compounds among pyrimidine, quinazoline and azepine derivatives in vitro and in vivo with further finding out the most active structures for new drug design. It were done a virtual screening of cyclopenthane[d]pyrimidine, quinazoline, imidazo[1,2-a]azepine derivatives and chosen for further organic synthesis compounds with the highest probability of spasmolytic activity manifestation. The screening of spasmolytic activity among the cyclopenthane[d]pyrimidine, quinazoline, imidazo[1,2-a]azepine derivatives on isolated smooth muscle organs (uterus, bladder, thoracic part of aorta) had done and analysed. It was chosen two leader compounds acting on uterus (IFT_000316 and IFT_000194) and two leader compounds which affect bladder (IFT_000335 and IFT_000313). Leaders in tocolytic activity (IFT_000316 - 264±11 mcat/l; IFT_000194 - 265±35 mcat/l) demonstrate bigger influence on choline esterase activity than reference drug - nifedipine (220±29 mcat/l). Acute toxicity of leader compounds was studied and they were referred to III class of safety. In in vivo experiments it was detected that leader compounds do not affect blood pressure in rats with simultaneous decrease in cytometric parameters (IFT_000335 and IFT_000313) and tocolytic parameters (IFT_000316 andта IFT_000194). Product Description popup.authors Бобкова Людмила Станіславівна Геращенко Інна Василівна Демченко Анатолій Михайлович Демченко Сергій Анатолієвич Киричок Лора Михайлівна Мохорт Микола Антонович Пупишева Олена Володимирівна Хайрулін Андрій Рашидович Шуть Дмитро Миколайович popup.nrat_date 2020-04-02 Close