Synthesis and Pharmacological Evaluation of Novel Pyrazolyl Piperidine Derivatives as Effective Antiplatelet Agents

The synthesis and antiplatelet activity of substituted pyrazolyl piperidine derivatives (3a–n) are described. These compounds were synthesized by an improved ring opening reaction of 2‐arylidene quinuclidinone using hydrazine hydrate under mild conditions. They were characterized and screened for th...

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Published inJournal of heterocyclic chemistry Vol. 54; no. 2; pp. 1279 - 1286
Main Authors Soni, Jigar Y., Tamboli, Riyaj S., Giridhar, Rajani, Yadav, Mange Ram, Thakore, Sonal
Format Journal Article
LanguageEnglish
Published HOBOKEN Wiley 01.03.2017
Wiley Subscription Services, Inc
Subjects
Chemistry
Chemistry, Organic
Physical Sciences
Science & Technology
ASPIRIN
ALPHA-7
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Summary:The synthesis and antiplatelet activity of substituted pyrazolyl piperidine derivatives (3a–n) are described. These compounds were synthesized by an improved ring opening reaction of 2‐arylidene quinuclidinone using hydrazine hydrate under mild conditions. They were characterized and screened for their in vitro antiplatelet profile in human platelet aggregation using adenosine diphosphate as agonist. Investigation of structure activity relation revealed interesting results. Among these synthesized derivatives (3a–n), compounds 3a, 3c, 3j, and 3l exhibited excellent activity, while 3c was the most potent one. Based on IC50 values, it was observed that most of the compounds possessed antiplatelet aggregation activity superior to the reference drug Aspirin.
ISSN:0022-152X
1943-5193
DOI:10.1002/jhet.2703