Pupysheva H. The search and myotropic spasmolytic activity of new heterocyclic nitrogen compounds and adamantylcontainig derivatives of 1-alkoxy-3-dialkylamino-2-propanol

Українська версія

Thesis for the degree of Candidate of Sciences (CSc)

State registration number

0413U002567

Applicant for

Specialization

  • 14.03.05 - Фармакологія

17-04-2013

Specialized Academic Board

Д 26.550.01

Institute of Pharmacology and Toxicology of the National Academy of Medical Sciences of Ukraine

Essay

The dissertation is based on the experimental research of myotropic spasmolytic effects of new synthesized heterocyclic nitrogen compounds and adamantylcontainig derivatives of 1-alkoxy-3-dialkylamino-2-propanol with previously predicted spectrum of pharmacological action by using the PASS program. As a result of previous computer prediction using the PASS, 42 new derivatives of 1H-cyclopenta[d]pyrimidine, thiazolo [4,5-d] pirydazin and adamantylcontainig derivatives of 1-alkoxy-3-dialkylamino-2-propanol were selected and synthesized, which must have the potential spasmolytic activity on blood vessels, uterus and urinary bladder, which could be realized through effects on ion channels, level of cAMP and cGMP, by activation adenylat and guanylate cyclase, inhibition different types of phosphodiesterases and changes activity of phosphatidylinositol-3-kinase. Taking into account the established myotropic spasmolytic activity, the ability to normalize bladder function under pathology conditions and low toxicity of IFT 35, it is considered appropriate to proceed further pre-clinical study of cyclopenta [d] pyrimidine derivative in order to create a new drug for the treatment of the overactive bladder.

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