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Title: Metal free synthesis, docking studies and antimicrobial screening of novel isomeric pyridine substituted thiazole derivatives
Authors: Suryawanshi, Manjusha
Patil, Amar
Bholay, Avinash
Bobade, Vivek
Keywords: Heteroarylation;Pyridine;Thiazole;Pharmacokinetic
Issue Date: Sep-2018
Publisher: NISCAIR-CSIR, India
Abstract: Library of isomeric pyridine substituted thiazole derivatives have been synthesized and characterized. Heteroarylation of pyridine is a considerable challenge as it is an electron poor ring and the arylation is even more difficult at C-3 of pyridine. A methodology has been formulated for thiazole ring at all the three positions of pyridine i.e. at C-2, C-3, C-4 without employing any metal catalyst. All thiazole derivatives contain an isomeric pyridyl ring attached at the non reactive C-2 position while the C-4 position is substituted with electron donating or withdrawing 4-substituted phenyl ring. Pharmacokinetic properties of these derivatives have been studied using Lipinski’s Rule of Five (RO5) to predict the bioactivity score. Almost all compounds follow the criteria for orally active drugs and hence show good drug like properties. Derivatives which contain electron withdrawing groups are found to exhibit good docking score and moderate biological activities.
Page(s): 1179-1188
ISSN: 0975-0983(Online); 0376-4699(Print)
Appears in Collections:IJC-B Vol.57B(09) [September 2018]

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