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Literature DB >> 2970549

3-[1-(2-Benzoxazolyl)hydrazino]propanenitrile derivatives: inhibitors of immune complex induced inflammation.

F Haviv¹, J D Ratajczyk, R W DeNet, F A Kerdesky, R L Walters, S P Schmidt, J H Holms, P R Young, G W Carter.

Abstract

3-[1-(2-Benzoxazolyl)hydrazino]propanenitrile derivatives were evaluated in the dermal and pleural reverse passive Arthus reactions in the rat. In the pleural test these compounds were effective in reducing exudate volume and accumulation of white blood cells. This pattern of activity was similar to that of hydrocortisone and different from that of indomethacin. The structural requirements for inhibiting the Arthus reactions were studied by systematic chemical modification of 1. These structure-activity relationship studies revealed that nitrogen 1' of the hydrazino group is essential for activity and must be electron rich, whereas chemical modifications of other sites of 1 had only a modest effect on activity.

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Year: 1988 PMID： 2970549 DOI： 10.1021/jm00117a010

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

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Cited

9 in total

1. Evaluation of the thiazole Schiff bases as β-glucuronidase inhibitors and their in silico studies.

Authors: Khalid Mohammed Khan; Aneela Karim; Sumayya Saied; Nida Ambreen; Xayale Rustamova; Shagufta Naureen; Sajid Mansoor; Muhammad Ali; Shahnaz Perveen; M Iqbal Choudhary; Guillermo Antonio Morales
Journal: Mol Divers Date: 2014-02-18 Impact factor: 2.943

2. Synthesis of chiral polyaminothiazoles.

Authors: Sergey Arutyunyan; Adel Nefzi
Journal: J Comb Chem Date: 2010-05-10

3. 5-Bromo-4-(3,4-dimeth-oxy-phen-yl)thia-zol-2-amine.

Authors: Hazem A Ghabbour; Tze Shyang Chia; Hoong-Kun Fun
Journal: Acta Crystallogr Sect E Struct Rep Online Date: 2012-05-05

4. A Remarkably High-Speed Solution-Phase Combinatorial Synthesis of 2-Substituted-Amino-4-Aryl Thiazoles in Polar Solvents in the Absence of a Catalyst under Ambient Conditions and Study of Their Antimicrobial Activities.

Authors: Satish N Dighe; Pratip K Chaskar; Kishor S Jain; Manisha S Phoujdar; Kumar V Srinivasan
Journal: ISRN Org Chem Date: 2011-04-11

5. Synthesis of novel (E)-1-(2-(2-(4(dimethylamino) benzylidene) hydrazinyl)-4-methylthiazol-5-yl)ethanone derivatives as ecto-5'-nucleotidase inhibitors.

Authors: Sidra Hassan; Pervaiz Ali Channar; Fayaz Ali Larik; Aamer Saeed; Hamid Saeed Shah; Joanna Lecka; Jean Sévigny; Jamshed Iqbal
Journal: R Soc Open Sci Date: 2018-09-12 Impact factor: 2.963

3-[1-(2-Benzoxazolyl)hydrazino]propanenitrile derivatives: inhibitors of immune complex induced inflammation.

1. Evaluation of the thiazole Schiff bases as β-glucuronidase inhibitors and their in silico studies.

2. Synthesis of chiral polyaminothiazoles.

3. 5-Bromo-4-(3,4-dimeth-oxy-phen-yl)thia-zol-2-amine.

4. A Remarkably High-Speed Solution-Phase Combinatorial Synthesis of 2-Substituted-Amino-4-Aryl Thiazoles in Polar Solvents in the Absence of a Catalyst under Ambient Conditions and Study of Their Antimicrobial Activities.

5. Synthesis of novel (E)-1-(2-(2-(4(dimethylamino) benzylidene) hydrazinyl)-4-methylthiazol-5-yl)ethanone derivatives as ecto-5'-nucleotidase inhibitors.

6. A mild one-pot synthesis of 2-iminothiazolines from thioureas and 1-bromo-1-nitroalkenes.

7. Brønsted acid-promoted thiazole synthesis under metal-free conditions using sulfur powder as the sulfur source.

8. Iridium-catalyzed 1,3-hydrogen shift/chlorination of allylic alcohols.

9. Synthesis and Biological Evaluation of Bisthiazoles and Polythiazoles.