Literature DB >> 14604693

Some new 2,3,6-trisubstituted quinazolinones as potent anti-inflammatory, analgesic and COX-II inhibitors.

Ashok Kumar1, Shalabh Sharma, Kiran Bajaj, Shipra Sharma, Hemant Panwar, Tripti Singh, V K Srivastava.   

Abstract

Various 2-(substitutedphenylmethyleneimino)aminoacetylmethylene-3-(2'-substitutedindol-3'-yl)-halosubstituted-4(3H)quinazolinones (5a-5i) and 2-(substituted phenylaminomethyleneacetyl-4'-oxo-1'-thiazolidinyl-3-(2"-substitutedindol-3"-yl) 4(3H)-quinazolinones (6a-6i) have been synthesized in the present studies. The structure of these compounds have been elucidated by elemental (C, H, N) and spectral (IR, 1H NMR and mass) analysis. Furthermore, above said compounds were evaluated for their anti-inflammatory, analgesic, ulcerogenic activities and acute toxicity study. Compound 6d was found to be most potent. Compound exihibiting less ulcerogenic liability and ALD(50) >2000mg/kg po.

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Year:  2003        PMID: 14604693     DOI: 10.1016/s0968-0896(03)00501-7

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN: 0968-0896            Impact factor:   3.641


  16 in total

1.  Site-Selective Copper-Catalyzed Amination and Azidation of Arenes and Heteroarenes via Deprotonative Zincation.

Authors:  Charles E Hendrick; Katie J Bitting; Seoyoung Cho; Qiu Wang
Journal:  J Am Chem Soc       Date:  2017-08-14       Impact factor: 15.419

2.  Direct and Selective 3-Amidation of Indoles Using Electrophilic N-[(Benzenesulfonyl)oxy]amides.

Authors:  Gerardo X Ortiz; Brett N Hemric; Qiu Wang
Journal:  Org Lett       Date:  2017-03-10       Impact factor: 6.005

Review 3.  An insight into the therapeutic potential of quinazoline derivatives as anticancer agents.

Authors:  Irshad Ahmad
Journal:  Medchemcomm       Date:  2017-04-07       Impact factor: 3.597

4.  Organocatalysis in heterocyclic synthesis: DABCO as a mild and efficient catalytic system for the synthesis of a novel class of quinazoline, thiazolo [3,2-a]quinazoline and thiazolo[2,3-b] quinazoline derivatives.

Authors:  Haider Behbehani; Hamada Mohamed Ibrahim
Journal:  Chem Cent J       Date:  2013-05-07       Impact factor: 4.215

5.  Synthesis and Antimicrobial Activity of 2-[2-(2,6-dichloro phenyl)amino]benzyl-3-(5-substituted phenyl-4,5-dihydro-1H-pyrazol-3-yl-amino)-6,8-dibromoquinazolin-4(3H)ones.

Authors:  Nb Patel; Jc Patel; Gg Barat
Journal:  J Young Pharm       Date:  2010-04

Review 6.  Chemical characteristics, synthetic methods, and biological potential of quinazoline and quinazolinone derivatives.

Authors:  Mohammad Asif
Journal:  Int J Med Chem       Date:  2014-11-12

7.  An Efficient and Facile Synthesis of 1,2,4-Aryl Triazoles and 4-Thiazolidinones Bearing 6-Fluorochroman Nucleus.

Authors:  Piyush B Vekariya; Jalpa R Pandya; Hitendra S Joshi
Journal:  Int Sch Res Notices       Date:  2014-10-29

8.  Synthesis, Characterization, and Anti-Inflammatory Activity of Newer Quinazolinone Analogs.

Authors:  Chatrasal Singh Rajput; Shiwani Singhal
Journal:  J Pharm (Cairo)       Date:  2013-01-17

9.  Synthesis and biological evaluation of 2-aminobenzamide derivatives as antimicrobial agents: opening/closing pharmacophore site.

Authors:  Yahia N Mabkhot; Abdullah M Al-Majid; Assem Barakat; Salim S Al-Showiman; Munirah S Al-Har; Smaail Radi; Muhammad Moazzam Naseer; Taibi B Hadda
Journal:  Int J Mol Sci       Date:  2014-03-21       Impact factor: 5.923

10.  Synthesis and antihypertensive screening of new derivatives of quinazolines linked with isoxazole.

Authors:  Mujeeb Ur Rahman; Ankita Rathore; Anees A Siddiqui; Gazala Parveen; M Shahar Yar
Journal:  Biomed Res Int       Date:  2014-06-12       Impact factor: 3.411

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