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Please use this identifier to cite or link to this item: http://repository.iitr.ac.in/handle/123456789/1620
Title: Synthesis of pyrimidine and condensed pyrimidine derivatives and their evaluation for anti-inflammatory activity
Authors: Sondhi S.M.
Singh J.
Agrawal S.K.
Saxena A.K.
Roy, Partha
Published in: Medicinal Chemistry Research
Abstract: Condensation of various amines (Ia-c) with 4-isothiocyanato-4-methyl-2- pentanone (2a) at room temperature gave tetrahydropyrimidinethiones (3a-c) whereas condensation of 1a-e with 3-isothiocyanatobutanal at room temperature gave tetrahydropyrimidinethiones (4a-e). Amines 1a, d, f-i on condensation with 4-isothiocyanato-4- methyl-2-pentanone (2a) by heating under reflux for 8 h at pH ? 4 (for 1a, d) and at RT (for 1f-i) gave dihydropyrimidinethiones 5a-b and 5c-f, respectively. Condensation of 1f with 3-isothiocyanatobutanal gave dihydropyimidinethione 6. When isothiocyanate (2a) and phenylenediamine derivatives 1g, h were heated under reflux at pH ?4, tricyclic compounds 7a, b were obtained in good yields. Condensation of 3-isothiocyanatobutanal with o-phenylenediamines 1h and 1j at pH ? 5 by refluxing in methanol for 8 h gave products 8 and 9. All these compounds were screened for anti-inflammatory activity. Compounds 3c, 4c and 7a exhibited anti-inflammatory activity comparable to standard drug ibuprofen. © Springer Science+Business Media, LLC 2010.
Citation: Medicinal Chemistry Research (2012), 21(1): 91-99
URI: https://doi.org/10.1007/s00044-010-9507-y
http://repository.iitr.ac.in/handle/123456789/1620
Issue Date: 2012
Keywords: Anti-inflammatory activity
Condensed pyrimidine
Heterocyclic compounds
Pyrimidine
ISSN: 10542523
Author Scopus IDs: 7006090710
55330178200
24173353300
7401482447
35509207200
Author Affiliations: Sondhi, S.M., Department of Chemistry, Indian Institute of Technology, Roorkee 247667, Uttarakhand, India
Singh, J., Department of Chemistry, Indian Institute of Technology, Roorkee 247667, Uttarakhand, India
Agrawal, S.K., Pharmacology Division, Indian Institute of Integrative Medicine, Jammu 180001, India
Saxena, A.K., Pharmacology Division, Indian Institute of Integrative Medicine, Jammu 180001, India
Roy, P., Department of Biotechnology, Indian Institute of Technology, Roorkee 247667, Uttarakhand, India
Funding Details: Acknowledgments We are thankful to technical staff of the Chemistry Department, I. I. T. Roorkee, for spectroscopic studies and elemental analysis. One of the authors Mr. Jaiveer Singh (SRF-NET) is thankful to CSIR, New Delhi, for financial assistance.
Corresponding Author: Sondhi, S.M.; Department of Chemistry, Indian Institute of Technology, Roorkee 247667, Uttarakhand, India; email: sondifcy@iitr.ernet.in
Appears in Collections:Journal Publications [BT]

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