Antitubercular Diazine Carboxamides

Rogers, Edward F.; Leanza, W. J.; Becker, Hans Joachim; Matzuk, A. R.; O'Neill, Richard; Basso, Antonella; Stein, Gustav A.; Solotorovsky, Morris; Gregory, Francis J.; Pfister, Karl

doi:10.1126/science.116.3010.253

Cited by 22 publications

(2 citation statements)

References 10 publications

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“…The relative activities of the pyrazinyl and pyridinyl amides, thioamides, and functional amide derivatives (hydroxamic acids, hydrazides) are given. These have been, in part, previously reported by us (4, 5), by our colleagues in these laboratories, (9,14,15), or by others (1,3,16,17). For comparison the activity of the corresponding related thiosemicarbazones is given.…”

supporting

confidence: 59%

THE SYNTHESIS OF COMPOUNDS FOR THE CHEMOTHERAPY OF TUBERCULOSIS. IV. THE AMIDE FUNCTION¹

Gardner¹,

Wenis²,

Lee³

1954

J. Org. Chem.

112

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The discovery by Chorine (1) of the in vivo activity of nicotinamide against tuberculosis in the mouse and the rediscovery of this activity by Kushner, et al. EXPERIMENTALGeneral procedure for the preparation of thioamides. The procedure of Karrer (8) for thionicotinamide and thiopicolinamide was used. One part by weight of the pure nitrile was added to five parts by weight of 30% ammonical methanol. The resulting solution was then saturated with dry hydrogen sulfide at 25°, and permitted to stand 1-2 days. The thioamide was separated by filtration. In the majority of cases, the recovered thioamide was recrystal -1 Presented before the Division of Medicinal Chemistry at the 124th meeting of the

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supporting

confidence: 59%

THE SYNTHESIS OF COMPOUNDS FOR THE CHEMOTHERAPY OF TUBERCULOSIS. IV. THE AMIDE FUNCTION¹

Gardner¹,

Wenis²,

Lee³

1954

J. Org. Chem.

112

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“…The method has been used to study the relationship between the half-wave potential and the antitubercular behavior for nicotinamide and a variety of heterocyclic compounds (275) and to help in the identification of nicotinamide isolated from squamous-cell carcinomas (49,50).…”

Section: Nitrogen Heterocyclic Compoundsmentioning

confidence: 99%

Organic Polarography

Wawzonek¹

1954

Anal. Chem.

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Antibacterial Agents, Overview

Macielag

Bush

Weidner‐Wells

2003

Kirk-Othmer Encyclopedia of Chemical Technology

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Antibacterial agents are synthetic compounds that kill or prevent the growth of bacteria. They exhibit selective toxicity to bacterial cells either because they inhibit a biochemical target present solely in bacteria or because they exhibit greater affinity for the bacterial target than the mammalian counterpart. Antibacterial agents are used in the treatment and/or prevention of infections due to pathogenic bacteria in humans and animals. The search for synthetic antiinfective agents began in the early 1900s with Paul Ehrlich's pioneering research on organoarsenicals. Currently, five classes of synthetic antibacterial agents are marketed for therapeutic use: the antitubercular agents, nitrofurans, oxazolidinones, quinolones, and the sulfonamides and combinations. Taken as a whole, drugs from these classes are used to treat a broad range of bacterial diseases, including tuberculosis, urinary tract infections, respiratory tract infections, and infections due to multidrug‐resistant bacteria. Emergence of resistance has limited the usefulness of the antitubercular agents and sulfonamides as sole therapy. The nitrofurans and the oxazolidinones have found their own niches, principally in the treatment of urinary tract infections and serious gram‐positive infections, respectively. The quinolones, by virtue of their broad spectrum of antimicrobial activity, oral bioavailability, good tissue distribution, and well‐understood safety profile, retain a prominent position in the armamentarium of antibacterial drugs.

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Antitubercular Diazine Carboxamides

Cited by 22 publications

References 10 publications

THE SYNTHESIS OF COMPOUNDS FOR THE CHEMOTHERAPY OF TUBERCULOSIS. IV. THE AMIDE FUNCTION¹

THE SYNTHESIS OF COMPOUNDS FOR THE CHEMOTHERAPY OF TUBERCULOSIS. IV. THE AMIDE FUNCTION¹

Organic Polarography

Antibacterial Agents, Overview

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Antitubercular Diazine Carboxamides

Cited by 22 publications

References 10 publications

THE SYNTHESIS OF COMPOUNDS FOR THE CHEMOTHERAPY OF TUBERCULOSIS. IV. THE AMIDE FUNCTION1

THE SYNTHESIS OF COMPOUNDS FOR THE CHEMOTHERAPY OF TUBERCULOSIS. IV. THE AMIDE FUNCTION1

Organic Polarography

Antibacterial Agents, Overview

Contact Info

Product

Resources

About

THE SYNTHESIS OF COMPOUNDS FOR THE CHEMOTHERAPY OF TUBERCULOSIS. IV. THE AMIDE FUNCTION¹

THE SYNTHESIS OF COMPOUNDS FOR THE CHEMOTHERAPY OF TUBERCULOSIS. IV. THE AMIDE FUNCTION¹