Baylis-Hillman reaction assisted parallel synthesis of 3,5-disubstituted isoxazoles and their in vivo bioevaluation as antithrombotic agents.
The solution-phase parallel synthesis involving reactions of Baylis-Hillman products of 3-substituted-5-isoxazolecarbaldehydes with nucleophiles and their in vivo antithrombotic evaluations are described along with the results of in vitro platelet aggregation inhibition assay of a few compounds. Results of the detailed evaluation of one of the compounds as an inhibitor of platelet aggregation are also presented.
Batra
S
S
Division of Medicinal Chemistry, Central Drug Research Institute, Lucknow 226 001, India. batra-san@yahoo.co.uk
Roy
A K
AK
Patra
A
A
Bhaduri
A P
AP
Surin
W R
WR
Raghavan
S A V
SA
Sharma
P
P
Kapoor
K
K
Dikshit
M
M
D000818:Animals; D000991:Antithrombins / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D004353:Drug Evaluation, Preclinical; D005260:Female; D007555:Isoxazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D013058:Mass Spectrometry; D051379:Mice; D011817:Rabbits; D051381:Rats; D017207:Rats, Sprague-Dawley
D000991:Antithrombins; D007555:Isoxazoles