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Design, Synthesis, and Screening of Triazolopyrimidine–Pyrazole Hybrids as Potent Apoptotic Inducers

An efficient synthesis of novel 3‐(3‐aryl‐1‐phenyl‐1H‐pyrazol‐4‐yl)‐5,7‐dimethyl‐[1,2,4]triazolo[4,3‐a]‐pyrimidines was accomplished by the oxidation of pyrimidinylhydrazones by using organoiodine(III) reagent. All new triazolopyrimidine derivatives bearing the pyrazole scaffold were screened to evaluate them as a reproductive toxicant in the testicular germ cells of goat (Capra hircus). This study aimed at assessing the cytological and biochemical changes in testicular germ cells after the exposure to triazolopyrimidines in a dose‐ and time‐dependent manner. Histomorphological analysis, fluorescence assays, apoptosis quantification, and terminal deoxynucleotidyl transferase dUTP‐mediated nick‐end labeling (TUNEL) assays were performed to determine cytological changes, whereas thiobarbituric acid‐reactive substance (TBARS) and ferric reducing antioxidant power (FRAP) assays were carried out to measure the oxidative stress in triazolopyrimidines treated germ cells. The parallel use of these methods enabled us to determine the role of triazolopyrimidines in inducing apoptosis as a consequence of cytogenetic damage and oxidative stress generated in testicular germ cells of goat.

Organoiodine(III)‐mediated oxidative methodology was used to design and synthesize triazolopyrimidine–pyrazole hybrid derivatives. The newly synthesized compounds were screened for their cytotoxicity and genotoxicity in goat (Capra hircus) testicular germ cells. The cytological changes and oxidative stress levels in treated germ cells were determined to assess the role of triazolopyrimidines in inducing apoptosis by cytogenetic damage and oxidative stress.

Autoren:   Raj Kamal, Vipan Kumar, Ravinder Kumar, Jitender K. Bhardwaj, Priyanka Saraf, Priya Kumari, Vikas Bhardwaj
Journal:   Archiv der Pharmazie
Band:   350
Ausgabe:   11
Jahrgang:   2017
Seiten:   n/a
DOI:   10.1002/ardp.201700137
Erscheinungsdatum:   16.10.2017
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