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Literature DB >> 1433181

Novel 1,2,4-oxadiazoles and 1,2,4-thiadiazoles as dual 5-lipoxygenase and cyclooxygenase inhibitors.

P C Unangst¹, G P Shrum, D T Connor, R D Dyer, D J Schrier.

Abstract

A series of 1,2,4-oxadiazoles and 1,2,4-thiadiazoles containing a 2,6-di-tert-butylphenol substituent were prepared and evaluated as dual inhibitors of 5-lipoxygenase and cyclooxygenase in rat basophilic leukemia (RBL-1) cells. Several of these compounds show oral efficacy in the rat carrageenan footpad edema (CFE) and mycobacterium footpad edema (MFE) antiinflammatory models, without concomitant gastric ulceration. Structure-activity relationships are discussed. The best compounds (ID40 values in MFE of 3-8 mg/kg po) contain guanidine-derived substituents on the heterocyclic ring.

Entities: Chemical Disease Gene Species

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Year: 1992 PMID： 1433181 DOI： 10.1021/jm00098a015

Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446

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Cited

10 in total

1. Molecular structure and vibrational and chemical shift assignments of 5-(2-Hydroxyphenyl)-4-(p-tolyl)-2,4-dihydro-1,2,4-triazole-3-thione by DFT and ab initio HF calculations.

Authors: Muharrem Dinçer; Davut Avci; Mehmet Sekerci; Yusuf Atalay
Journal: J Mol Model Date: 2008-06-26 Impact factor: 1.810

2. Quantum chemical investigation of the intra- and intermolecular proton transfer reactions and hydrogen bonding interactions in 4-amino-5-(2-hydroxyphenyl)-2H-1,2,4-triazole-3(4H)-thione.

Authors: Namık Özdemir
Journal: J Mol Model Date: 2012-09-01 Impact factor: 1.810

Review 3. Rationally designed multitarget agents against inflammation and pain.

Authors: S H Hwang; A T Wecksler; K Wagner; B D Hammock
Journal: Curr Med Chem Date: 2013 Impact factor: 4.530

4. Direct and solvent-assisted keto-enol tautomerism and hydrogen-bonding interactions in 4-(m-chlorobenzylamino)-3-phenyl-4,5-dihydro-1H-1,2,4-triazol-5-one: a quantum-chemical study.

Authors: N Burcu Arslan; Namık Özdemir
Journal: J Mol Model Date: 2015-01-25 Impact factor: 1.810

5. Design, Synthesis, and Biological Evaluation of 1,2,4-Thiadiazole-1,2,4-Triazole Derivatives Bearing Amide Functionality as Anticancer Agents.

Authors: Yazala Jyothsna Pragathi; Reddymasu Sreenivasulu; Deekala Veronica; Rudraraju Ramesh Raju
Journal: Arab J Sci Eng Date: 2020-05-22 Impact factor: 2.334

6. Synthesis, X-ray diffraction analysis, quantum chemical studies and α-amylase inhibition of probenecid derived S-alkylphthalimide-oxadiazole-benzenesulfonamide hybrids.

Authors: Bilal Ahmad Khan; Syeda Shamila Hamdani; Muhammad Naeem Ahmed; Shahid Hameed; Muhammad Ashfaq; Ahmed M Shawky; Mahmoud A A Ibrahim; Peter A Sidhom
Journal: J Enzyme Inhib Med Chem Date: 2022-12 Impact factor: 5.756

Novel 1,2,4-oxadiazoles and 1,2,4-thiadiazoles as dual 5-lipoxygenase and cyclooxygenase inhibitors.

1. Molecular structure and vibrational and chemical shift assignments of 5-(2-Hydroxyphenyl)-4-(p-tolyl)-2,4-dihydro-1,2,4-triazole-3-thione by DFT and ab initio HF calculations.

2. Quantum chemical investigation of the intra- and intermolecular proton transfer reactions and hydrogen bonding interactions in 4-amino-5-(2-hydroxyphenyl)-2H-1,2,4-triazole-3(4H)-thione.

Review 3. Rationally designed multitarget agents against inflammation and pain.

4. Direct and solvent-assisted keto-enol tautomerism and hydrogen-bonding interactions in 4-(m-chlorobenzylamino)-3-phenyl-4,5-dihydro-1H-1,2,4-triazol-5-one: a quantum-chemical study.

5. Design, Synthesis, and Biological Evaluation of 1,2,4-Thiadiazole-1,2,4-Triazole Derivatives Bearing Amide Functionality as Anticancer Agents.

6. Synthesis, X-ray diffraction analysis, quantum chemical studies and α-amylase inhibition of probenecid derived S-alkylphthalimide-oxadiazole-benzenesulfonamide hybrids.

7. Synthesis of some new 4,5-substituted-4H-1,2,4-triazole-3-thiol derivatives.

8. 3-Ethyl-6-[3-(4-fluoro-phen-yl)-1H-pyrazol-4-yl]-1,2,4-triazolo[3,4-b][1,3,4]thia-diazole.

9. Butylated hydroxytoluene analogs: synthesis and evaluation of their multipotent antioxidant activities.

10. Synthesis of oxadiazoles, thiadiazoles and triazoles derived from benzo[b]thiophene.