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Design, Characterization, and Hematopoietic Efficacy of a Fluorinated Pyrazolopiperidine Inclusion Complex
Автор(ы)
Guldana Daulet
Assel Yu. Ten
Raushan B. Koizhaiganova
Lyailya Baktybayeva
Tolganay Zharkynbek
Alexey Zazybin
Т. М. Сейлханов
Valery M. Dembitsky
V. К. Yu
Дата публикации
11 октября 2025 г.
Тип
journal article
Издатель
Multidisciplinary Digital Publishing Institute
Журнал
Том
30
Выпуск
20
Первая страница
4047
Последняя страница
4047
ISSN
1420-3049
Аннотация
A novel inclusion complex of a fluorinated pyrazolopiperidine derivative (5-benzyl-7-(2-fluorobenzylidene)-2,3-bis(2-fluorophenyl)-3,3a,4,5,6,7-hexahydro-2H-pyrazolo [4,3-c]pyridine hydrochloride, PP·HCl) with β-cyclodextrin (PPβCD) was designed, synthesized, and characterized as a potential therapeutic agent for chemotherapy-induced myelosuppression and lymphopenia. Encapsulation of PP within β-cyclodextrin increased aqueous solubility by approximately 3.4-fold and improved dissolution rate by 2.8-fold compared with the free compound. Structural analysis using IR, ^1H/^13C NMR, and TLC confirmed the formation of a stable 1:1 host–guest complex, and the disappearance of free PP signals further supported complete encapsulation. In vivo evaluation in a cyclophosphamide-induced myelosuppression model demonstrated that PPβCD accelerated hematopoietic recovery, restoring leukocyte and erythrocyte counts 35–40% faster than methyluracil, without any signs of systemic toxicity. These findings indicate that β-cyclodextrin complexation significantly enhances solubility, dissolution, and biological efficacy of the pyrazolopiperidine scaffold, supporting further preclinical development of PPβCD as a supportive therapy for chemotherapy-related hematological complications.
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