Die tuberkulostätischen Eigenschaften einiger primärer Amine

Wagner, W. H.; Vonderbank, Hermann

doi:10.1007/bf02056043

Cited by 6 publications

(3 citation statements)

References 26 publications

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“…Many thiourea derivatives have been tested for anti tubercular activity. Some show*ed no activity at all (97, 119, 240), while others did look promising in in vitro studies (30,33,110,219,239). How*ever, excluding the sulfonylthioureas, very little success w*as found in the treatment of tuberculosis with this class of compounds until very recently.…”

mentioning

confidence: 99%

Thioureas

Schroeder¹

1955

Chem. Rev.

196

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mentioning

confidence: 99%

Thioureas

Schroeder¹

1955

Chem. Rev.

196

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“…Benzoxazole skeleton has been studied as antitubercular agent since 1949 . However, this structure has attracted the considerable attention mostly during the last two decades.…”

Section: Benzoxazoles As Anti‐tb Agentsmentioning

confidence: 99%

“…Benzoxazole skeleton has been studied as antitubercular agent since 1949. [34] However, this structure has attracted the considerable attention mostly during the last two decades. Different substituents can be incorporated onto the benzene ring to improve the biological activity; especially the substitution at the position 2 and 5 is influential.…”

Section: Benzoxazoles As Anti-tb Agentsmentioning

confidence: 99%

Benzoxazole Derivatives as Promising Antitubercular Agents

Šlachtová

Brulíková

2018

ChemistrySelect

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Tuberculosis (TB) is an infectious disease caused predominantly by bacillus Mycobacterium tuberculosis (MTB). The increasing prevalence of multidrug‐resistant MTB necessitates the discovery and development of alternative drugs against tuberculosis with a new mechanism of action. Over the past years, several benzoxazole derivatives have been synthesized and screened for their biological activity. Interestingly, some of them had promising antitubercular activity. Despite that, none of the benzoxazole derivatives has entered the phase of the preclinical hit‐to‐lead optimization step in anti‐TB research. In this review, we are summarizing recently published articles that evaluate the potency of benzoxazole heterocycle in the development of novel anti‐TB agents and outlined the future aspects of this promising heterocycle.

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Synthesis and some reactions of naphth[1,2‐d]oxazole‐5‐sulfonic acids

Osman

Youssef

Atta

1982

Journal of Heterocyclic Chem

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Naphth[1,2‐d]oxazole‐5‐sulfonic acid (1) has been prepared by the fusion of 4‐amino‐3‐hydroxynaphthalene‐1‐sulfonic acid with formamide. Interaction of 1 with a number of arenesulfonyl chlorides, aryloxyacetyl chlorides, 1‐naphthyloxyacetyl chloride, and chloroacetyl chloride gave 2‐(arylsulfonyl)‐, 2‐(aryloxyacetyl)‐, 2‐(1‐naphthyloxyacetyl)‐ and 2‐(chloroacetyl)naphth[1,2‐d]oxaxole‐5‐sulfonic acids (2, 3, 4 and 5), respectively. The corresponding sulfonyl chloride of 2 was condensed with amines giving the expected 2‐(arylsulfonyl)‐naphth[1,2‐d]oxazole‐5‐sulfonamides (6). Interaction of 5 with hydrazine gave 2‐hydrazinoacetyl and disubstituted hydrazine derivatives 7 and 8. Condensation of 7 with aromatic aldehydes yielded substituted hydrazonoacetyl derivatives 9. Two moles of 5 react with one mole of hydroquinone in dry acetone in the presence of anhydrous potassium carbonate and potassium iodide gave 1,4‐bis[5‐sulfonaphth[1,2‐d]oxazol‐2‐ylcarbonyl‐methoxy]benzene (10).

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Die tuberkulostätischen Eigenschaften einiger primärer Amine

Cited by 6 publications

References 26 publications

Thioureas

Thioureas

Benzoxazole Derivatives as Promising Antitubercular Agents

Synthesis and some reactions of naphth[1,2‐d]oxazole‐5‐sulfonic acids

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