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Improved multicomponent, one‐pot synthesis of functionalized tetrahydropyrans cardiovascular dysfunction regulators
Author(s) -
Aggile Kadirappa,
Alagumuthu Manikandan,
Kumar Pramod,
Napoleon Ayyakannu Arumugam
Publication year - 2020
Publication title -
journal of heterocyclic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.321
H-Index - 59
eISSN - 1943-5193
pISSN - 0022-152X
DOI - 10.1002/jhet.3876
Subject(s) - chemistry , docking (animal) , reagent , enzyme , renin–angiotensin system , inflammation , pharmacology , angiotensin converting enzyme , combinatorial chemistry , biochemistry , organic chemistry , medicine , nursing , blood pressure
A simple, efficient, and straightforward one‐pot three‐component synthesis of functionalized tetrahydropyrans ( 6a‐l ) is carried‐out in the presence of an inexpensive and environmentally benign Eaton's reagent as a catalyst to discover some ACE inhibitors and anti‐inflammatory agents. Angiotensin‐converting enzyme (ACE) is highly involved in the renin‐angiotensin system and often directly associated with cardiovascular dysfunction via inflammation. Thus, the cardiovascular protective effect of newly synthesized tetrahydropyrans ( 6a‐l ) was evaluated through ACE inhibition, human red blood cell (HRBC) membrane stabilization, and molecular docking studies. As the results complied, compounds 6e and 6f were identified as effective ACE inhibitors. Docking studies, HRBC based anti‐inflammatory assay, and SAR studies revealed that compounds 6e and 6f could be good anti‐inflammatory agents apart from ACE inhibitors.