Literature DB >> 3572984

Substituted 1,3,4-thiadiazoles with anticonvulsant activity. 3. Guanidines.

C B Chapleo, P L Myers, A C Smith, I F Tulloch, S Turner, D S Walter.   

Abstract

The synthesis and anticonvulsant activity of a number of 2-aryl-5-guanidino-1,3,4 thiadiazoles are described. The unsubstituted guanidine 2a was found to possess potent anticonvulsant properties; considerable reduction or loss of activity however was observed with the majority of the substituted guanidines. Incorporation of the guanidine group into an imidazoline ring also resulted in a loss of activity. Secondary pharmacological evaluation confirmed the anticonvulsant properties of 2a but also revealed that the compound exhibited a considerable degree of sedative activity.

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Year:  1987        PMID: 3572984     DOI: 10.1021/jm00388a038

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


  6 in total

1.  Discovery of Fused Triazolo-thiadiazoles as Inhibitors of TNF-alpha: Pharmacophore Hybridization for Treatment of Neuropathic Pain.

Authors:  Monika Sharma; Vanamala Deekshith; Arvind Semwal; Dharmarajan Sriram; Perumal Yogeeswari
Journal:  Pain Ther       Date:  2012-09-11

2.  2,2'-Bi-1,3,4-thia-diazole-5,5'-diamine tetra-hydrate.

Authors:  Chaveng Pakawatchai; Saowanit Saithong
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2010-08-04

3.  N-(5-Benzyl-sulfanyl-1,3,4-thia-diazol-2-yl)-2-(piperidin-1-yl)acetamide.

Authors:  D S Ismailova; R Ya Okmanov; A A Ziyaev; Kh M Shakhidoyatov; B Tashkhodjaev
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2014-02-05

4.  Synthesis, characterization, antimicrobial, and pharmacological evaluation of some 2, 5-disubstituted sulfonyl amino 1,3,4-oxadiazole and 2-amino-disubstituted 1,3,4-thiadiazole derivatives.

Authors:  Dilipkumar Pal; Rohit Tripathi; Desh Deepak Pandey; Preety Mishra
Journal:  J Adv Pharm Technol Res       Date:  2014-10

5.  Synthesis of new 1,3,4-thiadiazole and 1,2,3,4-oxathiadiazole derivatives from carbohydrate precursors and study of their effect on tyrosinase enzyme.

Authors:  Mohamed M El-Sadek; Seham Y Hassan; Huda E Abdelwahab; Galila A Yacout
Journal:  Molecules       Date:  2012-07-11       Impact factor: 4.411

6.  Synthesis and Antiviral Activity of Novel 1,4-Pentadien-3-one Derivatives Containing a 1,3,4-Thiadiazole Moiety.

Authors:  Lu Yu; Xiuhai Gan; Dagui Zhou; Fangcheng He; Song Zeng; Deyu Hu
Journal:  Molecules       Date:  2017-04-21       Impact factor: 4.411

  6 in total

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