Page last updated: 2024-10-20

pyrazinoic acid and Koch's Disease

pyrazinoic acid has been researched along with Koch's Disease in 19 studies

pyrazinoic acid: active metabolite of pyrazinamide; structure
pyrazine-2-carboxylic acid : The parent compound of the class of pyrazinecarboxylic acids, that is pyrazine bearing a single carboxy substituent. The active metabolite of the antitubercular drug pyrazinamide.

Research Excerpts

ExcerptRelevanceReference
"Pyrazinamide has been a mainstay in the multidrug regimens used to treat tuberculosis."7.96The molecular basis of pyrazinamide activity on Mycobacterium tuberculosis PanD. ( Li, X; Perez, LM; Sacchettini, JC; Shi, W; Sun, Q; Zhang, Y, 2020)
"Pyrazinamide (PZA) is an important component of first-line drugs because of its distinctive capability to kill subpopulations of persistent Mycobacterium tuberculosis (MTB)."7.91Pyrazinamide resistance and mutations in pncA among isolates of Mycobacterium tuberculosis from Khyber Pakhtunkhwa, Pakistan. ( Afzal, MT; Ali, S; Khan, AS; Khan, MT; Malik, SI; Masood, N; Nadeem, T, 2019)
"Through mutant selection on agar containing pyrazinoic acid (POA), the bioactive form of the prodrug pyrazinamide (PZA), we recently showed that missense mutations in the aspartate decarboxylase PanD and the unfoldase ClpC1, and loss-of-function mutation of polyketide synthases Mas and PpsA-E involved in phthiocerol dimycocerosate synthesis, cause resistance to POA and PZA in Mycobacterium tuberculosis."7.85In Vivo-Selected Pyrazinoic Acid-Resistant Mycobacterium tuberculosis Strains Harbor Missense Mutations in the Aspartate Decarboxylase PanD and the Unfoldase ClpC1. ( Dartois, V; Dick, T; Gopal, P; Lanoix, JP; Li, L; Nuermberger, E; Rasic, G; Sarathy, J; Tasneen, R; Yee, M, 2017)
"Pyrazinamide (PZA) is an important front-line anti-tuberculosis drug that is active only at acid pH."7.71Conditions that may affect the results of susceptibility testing of Mycobacterium tuberculosis to pyrazinamide. ( Permar, S; Sun, Z; Zhang, Y, 2002)
"Pyrazinamide (PZA) is a prodrug requiring conversion to pyrazinoic acid (POA) by an amidase encoded by pncA for in vitro activity."5.43High Systemic Exposure of Pyrazinoic Acid Has Limited Antituberculosis Activity in Murine and Rabbit Models of Tuberculosis. ( Alland, D; Dartois, V; Lanoix, JP; Nuermberger, E; O'Brien, P; Pinn, M; Safi, H; Sarathy, J; Tasneen, R, 2016)
"46 μm, as measured by inertial impaction, for POA-leu and POA-NH4, respectively) and with properties (stoichiometric 1:1 ratio of salt to drug, melting points at ∼180 °C, with water content of <1%) that would support further development as an inhaled dosage form."5.42Spray Dried Aerosol Particles of Pyrazinoic Acid Salts for Tuberculosis Therapy. [Corrected]. ( Dhillon, J; Durham, PG; Fourie, PB; German, N; Hickey, AJ; Mitchison, DA; Mortensen, N; Zhang, Y, 2015)
"Pyrazinamide has been a mainstay in the multidrug regimens used to treat tuberculosis."3.96The molecular basis of pyrazinamide activity on Mycobacterium tuberculosis PanD. ( Li, X; Perez, LM; Sacchettini, JC; Shi, W; Sun, Q; Zhang, Y, 2020)
"Pyrazinamide is a sterilizing first-line tuberculosis drug."3.96Pyrazinamide triggers degradation of its target aspartate decarboxylase. ( Akopian, T; Bhushan, S; Dick, T; Gengenbacher, M; Gopal, P; Grüber, G; Kandror, O; Lim, TK; Lin, Q; Ragunathan, P; Rubin, EJ; Sarathy, JP; Shin, J; Yee, M; Zhu, J, 2020)
"Pyrazinamide (PZA) is an important component of first-line drugs because of its distinctive capability to kill subpopulations of persistent Mycobacterium tuberculosis (MTB)."3.91Pyrazinamide resistance and mutations in pncA among isolates of Mycobacterium tuberculosis from Khyber Pakhtunkhwa, Pakistan. ( Afzal, MT; Ali, S; Khan, AS; Khan, MT; Malik, SI; Masood, N; Nadeem, T, 2019)
"Through mutant selection on agar containing pyrazinoic acid (POA), the bioactive form of the prodrug pyrazinamide (PZA), we recently showed that missense mutations in the aspartate decarboxylase PanD and the unfoldase ClpC1, and loss-of-function mutation of polyketide synthases Mas and PpsA-E involved in phthiocerol dimycocerosate synthesis, cause resistance to POA and PZA in Mycobacterium tuberculosis."3.85In Vivo-Selected Pyrazinoic Acid-Resistant Mycobacterium tuberculosis Strains Harbor Missense Mutations in the Aspartate Decarboxylase PanD and the Unfoldase ClpC1. ( Dartois, V; Dick, T; Gopal, P; Lanoix, JP; Li, L; Nuermberger, E; Rasic, G; Sarathy, J; Tasneen, R; Yee, M, 2017)
"The activity of different analogs of pyrazinamide on Mycobacterium tuberculosis fatty acid synthase type I (FASI) in replicating bacilli was studied."3.74Pyrazinoic acid and its n-propyl ester inhibit fatty acid synthase type I in replicating tubercle bacilli. ( Arai, M; Jacobs, WR; Vilchèze, C; Welch, JT; Zimhony, O, 2007)
"Pyrazinamide (PZA) is an important front-line anti-tuberculosis drug that is active only at acid pH."3.71Conditions that may affect the results of susceptibility testing of Mycobacterium tuberculosis to pyrazinamide. ( Permar, S; Sun, Z; Zhang, Y, 2002)
"Substituted pyrazinoic acid esters have previously been reported to have in vitro activity against Mycobacterium avium and Mycobacterium kansasii as well as Mycobacterium tuberculosis."3.69Quantitative structure-activity relationships for the in vitro antimycobacterial activity of pyrazinoic acid esters. ( Bergmann, KE; Cynamon, MH; Welch, JT, 1996)
"Pyrazinamide (PZA) is a critical component of the first-line TB treatment regimen because of its sterilizing activity against non-replicating Mycobacterium tuberculosis (Mtb), but its mechanism of action has remained enigmatic."1.72Structure activity relationship of pyrazinoic acid analogs as potential antimycobacterial agents. ( Aldrich, CC; Aragaw, WW; Cole, MS; Dick, T; Grüber, G; Harikishore, A; Hegde, PV; Jachak, G; Ragunathan, P; Sharma, S, 2022)
"Pyrazinoic acid (1: ) was esterified first (2: ) followed by amination to produce hydrazide (3: ) which was refluxed with POCl3 to obtain 2-chloromethyl-5pyrazino-1, 3, 4-oxadiazole (4: )."1.62Evaluation and Docking Study of Pyrazine Containing 1, 3, 4-Oxadiazoles Clubbed with Substituted Azetidin-2-one: A New Class of Potential Antimicrobial and Antitubercular. ( Das, R; Mehta, DK, 2021)
"Pyrazinamide (PZA) is a prodrug requiring conversion to pyrazinoic acid (POA) by an amidase encoded by pncA for in vitro activity."1.43High Systemic Exposure of Pyrazinoic Acid Has Limited Antituberculosis Activity in Murine and Rabbit Models of Tuberculosis. ( Alland, D; Dartois, V; Lanoix, JP; Nuermberger, E; O'Brien, P; Pinn, M; Safi, H; Sarathy, J; Tasneen, R, 2016)
"46 μm, as measured by inertial impaction, for POA-leu and POA-NH4, respectively) and with properties (stoichiometric 1:1 ratio of salt to drug, melting points at ∼180 °C, with water content of <1%) that would support further development as an inhaled dosage form."1.42Spray Dried Aerosol Particles of Pyrazinoic Acid Salts for Tuberculosis Therapy. [Corrected]. ( Dhillon, J; Durham, PG; Fourie, PB; German, N; Hickey, AJ; Mitchison, DA; Mortensen, N; Zhang, Y, 2015)

Research

Studies (19)

TimeframeStudies, this research(%)All Research%
pre-19904 (21.05)18.7374
1990's2 (10.53)18.2507
2000's2 (10.53)29.6817
2010's6 (31.58)24.3611
2020's5 (26.32)2.80

Authors

AuthorsStudies
Zimhony, O1
Vilchèze, C1
Arai, M1
Welch, JT3
Jacobs, WR1
Hegde, PV1
Aragaw, WW1
Cole, MS2
Jachak, G1
Ragunathan, P2
Sharma, S2
Harikishore, A1
Grüber, G2
Dick, T3
Aldrich, CC2
Howe, MD1
Buonomo, JA1
Lamont, EA1
Brody, SI1
Mishra, NK1
Minato, Y1
Thiede, JM1
Baughn, AD1
Sun, Q1
Li, X1
Perez, LM1
Shi, W1
Zhang, Y3
Sacchettini, JC1
Gopal, P2
Sarathy, JP1
Yee, M2
Shin, J1
Bhushan, S1
Zhu, J1
Akopian, T1
Kandror, O1
Lim, TK1
Gengenbacher, M1
Lin, Q1
Rubin, EJ1
Das, R1
Mehta, DK1
Khan, MT1
Malik, SI1
Ali, S1
Masood, N1
Nadeem, T1
Khan, AS1
Afzal, MT1
Durham, PG2
German, N1
Mortensen, N1
Dhillon, J1
Mitchison, DA2
Fourie, PB1
Hickey, AJ2
Corrêa, MF1
Fernandes, JP1
Lanoix, JP2
Tasneen, R2
O'Brien, P1
Sarathy, J2
Safi, H1
Pinn, M1
Alland, D1
Dartois, V2
Nuermberger, E2
Young, EF1
Perkowski, E1
Malik, S1
Hayden, JD1
Zhong, L1
Braunstein, MS1
Rasic, G1
Li, L1
FERRARI, S2
MORELLINI, M2
BONATI, F1
BERTONI, L1
CASALONE, G1
GANZETTI, G1
MANGIAROTTI, S1
SOLOTOROVSKY, M1
GREGORY, FJ1
IRONSON, EJ1
BUGIE, EJ1
O'NEILL, RC1
PFISTER, R1
Bergmann, KE1
Cynamon, MH1
Permar, S1
Sun, Z1

Reviews

1 review available for pyrazinoic acid and Koch's Disease

ArticleYear
Pyrazinamide and Pyrazinoic Acid Derivatives Directed to Mycobacterial Enzymes Against Tuberculosis.
    Current protein & peptide science, 2016, Volume: 17, Issue:3

    Topics: Animals; Anti-Bacterial Agents; Humans; Mycobacterium tuberculosis; Prodrugs; Pyrazinamide; Tubercul

2016

Other Studies

18 other studies available for pyrazinoic acid and Koch's Disease

ArticleYear
Pyrazinoic acid and its n-propyl ester inhibit fatty acid synthase type I in replicating tubercle bacilli.
    Antimicrobial agents and chemotherapy, 2007, Volume: 51, Issue:2

    Topics: Bacterial Proteins; Fatty Acid Synthases; Microbial Sensitivity Tests; Mycobacterium tuberculosis; P

2007
Structure activity relationship of pyrazinoic acid analogs as potential antimycobacterial agents.
    Bioorganic & medicinal chemistry, 2022, 11-15, Volume: 74

    Topics: Amidohydrolases; Antitubercular Agents; Carboxylic Acids; Drug Resistance, Bacterial; Humans; Microb

2022
Cephem-Pyrazinoic Acid Conjugates: Circumventing Resistance in Mycobacterium tuberculosis.
    Chemistry (Weinheim an der Bergstrasse, Germany), 2022, Sep-12, Volume: 28, Issue:51

    Topics: Antitubercular Agents; beta-Lactams; Humans; Microbial Sensitivity Tests; Mycobacterium tuberculosis

2022
The molecular basis of pyrazinamide activity on Mycobacterium tuberculosis PanD.
    Nature communications, 2020, 01-17, Volume: 11, Issue:1

    Topics: Amidohydrolases; Antitubercular Agents; Bacterial Proteins; Carboxy-Lyases; Crystallography, X-Ray;

2020
Pyrazinamide triggers degradation of its target aspartate decarboxylase.
    Nature communications, 2020, 04-03, Volume: 11, Issue:1

    Topics: Antitubercular Agents; Bacterial Proteins; Carboxy-Lyases; Drug Resistance, Bacterial; Endopeptidase

2020
Evaluation and Docking Study of Pyrazine Containing 1, 3, 4-Oxadiazoles Clubbed with Substituted Azetidin-2-one: A New Class of Potential Antimicrobial and Antitubercular.
    Drug research, 2021, Volume: 71, Issue:1

    Topics: Antifungal Agents; Antitubercular Agents; Aspergillus niger; Azetidines; Candida albicans; Drug Eval

2021
Pyrazinamide resistance and mutations in pncA among isolates of Mycobacterium tuberculosis from Khyber Pakhtunkhwa, Pakistan.
    BMC infectious diseases, 2019, Feb-06, Volume: 19, Issue:1

    Topics: Adolescent; Adult; Aged; Amidohydrolases; Antitubercular Agents; Child; Drug Resistance, Bacterial;

2019
Spray Dried Aerosol Particles of Pyrazinoic Acid Salts for Tuberculosis Therapy. [Corrected].
    Molecular pharmaceutics, 2015, Aug-03, Volume: 12, Issue:8

    Topics: Administration, Inhalation; Antitubercular Agents; Desiccation; Dry Powder Inhalers; Humans; Nanopar

2015
High Systemic Exposure of Pyrazinoic Acid Has Limited Antituberculosis Activity in Murine and Rabbit Models of Tuberculosis.
    Antimicrobial agents and chemotherapy, 2016, Volume: 60, Issue:7

    Topics: Animals; Antitubercular Agents; Female; Mice; Mice, Inbred BALB C; Microbial Sensitivity Tests; Myco

2016
Inhaled Pyrazinoic Acid Esters for the Treatment of Tuberculosis.
    Pharmaceutical research, 2016, Volume: 33, Issue:10

    Topics: Administration, Inhalation; Aerosols; Animals; Antitubercular Agents; Esters; Guinea Pigs; Male; Mic

2016
In Vivo-Selected Pyrazinoic Acid-Resistant Mycobacterium tuberculosis Strains Harbor Missense Mutations in the Aspartate Decarboxylase PanD and the Unfoldase ClpC1.
    ACS infectious diseases, 2017, 07-14, Volume: 3, Issue:7

    Topics: Animals; Antitubercular Agents; Bacterial Proteins; Carboxy-Lyases; Culture Media; Disease Models, A

2017
[Activity of pyrazinamide (pyrazine-2-carboxylic acid amide) in experimental tuberculosis of the cavy].
    Annali dell'Istituto "Carlo Forlanini", 1956, Volume: 16, Issue:2

    Topics: Amides; Guinea Pigs; Niacin; Nicotinic Acids; Pyrazinamide; Tuberculosis

1956
[Activity of pyrazinamide (pyrazine-2-carboxylic acid amide) in experimental tuberculosis of the cavy].
    Annali dell'Istituto "Carlo Forlanini", 1956, Volume: 16, Issue:2

    Topics: Amides; Guinea Pigs; Niacin; Nicotinic Acids; Pyrazinamide; Tuberculosis

1956
[Activity of pyrazinamide (pyrazine-2-carboxylic acid amide) in experimental tuberculosis of the cavy].
    Annali dell'Istituto "Carlo Forlanini", 1956, Volume: 16, Issue:2

    Topics: Amides; Guinea Pigs; Niacin; Nicotinic Acids; Pyrazinamide; Tuberculosis

1956
[Activity of pyrazinamide (pyrazine-2-carboxylic acid amide) in experimental tuberculosis of the cavy].
    Annali dell'Istituto "Carlo Forlanini", 1956, Volume: 16, Issue:2

    Topics: Amides; Guinea Pigs; Niacin; Nicotinic Acids; Pyrazinamide; Tuberculosis

1956
[Basic derivatives of pyrazine-2-carboxylic acid with antimycobacterial action. Microbiological and pharmacological study].
    Minerva medica, 1962, Jun-02, Volume: 53

    Topics: Anti-Bacterial Agents; Humans; Pyrazinamide; Tuberculosis

1962
[Experimental and clinical research on the antitubercular activity of the N-(4-morpholinomethyl)-amide of pyrazinecarboxylic acid].
    Minerva medica, 1962, Jun-02, Volume: 53

    Topics: Amides; Antitubercular Agents; Humans; Pyrazinamide; Tuberculosis

1962
Pyrazinoic acid amide; an agent active against experimental murine tuberculosis.
    Proceedings of the Society for Experimental Biology and Medicine. Society for Experimental Biology and Medicine (New York, N.Y.), 1952, Volume: 79, Issue:4

    Topics: Amides; Animals; Humans; Mice; Niacin; Nicotinic Acids; Pyrazinamide; Tuberculosis

1952
Pyrazinamide--on the antituberculosis drug frontline.
    Nature medicine, 1996, Volume: 2, Issue:6

    Topics: Amidohydrolases; Animals; Antitubercular Agents; Dose-Response Relationship, Drug; Drug Resistance,

1996
Quantitative structure-activity relationships for the in vitro antimycobacterial activity of pyrazinoic acid esters.
    Journal of medicinal chemistry, 1996, Aug-16, Volume: 39, Issue:17

    Topics: AIDS-Related Opportunistic Infections; Anti-Bacterial Agents; Esters; Humans; Microbial Sensitivity

1996
Conditions that may affect the results of susceptibility testing of Mycobacterium tuberculosis to pyrazinamide.
    Journal of medical microbiology, 2002, Volume: 51, Issue:1

    Topics: Antitubercular Agents; Cell Survival; Colony Count, Microbial; Culture Media; Drug Interactions; Dru

2002