Synthesis and antitubercular activity of substituted novel pyrazoline derivatives. 2007

Mohamed Ashraf Ali, and Mohammad Shahar Yar, and Mahesh Kumar, and Ganesan Suresh Pandian
Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Jamia Hamdard University, New Delhi-110062, India. asraf80med@rediffmail.com

A series of 2-2-methoxy-4-[5-(substituted phenyl)1-(4-pyridylcarbonyl)-4,5-dihydro-1H-3-pyrazolyl] phenoxyacetic acid were synthesized by the reaction between isoniazid (INH) and chalcones, and were tested for their antimycobacterial activity in vitro against Mycobacterium tuberculosis H37Rv and INH resistant M. tuberculosis using BACTEC-460 radiometric system and agar dilution method. Among the synthesized compounds, Compounds II 2-4-[5-(4-hydroxyphenyl)-1-(4-pyridylcarbonyl)-4,5-ihydro-1H-3-pyrazolyl]-2-methoxy phenoxy acetic acid was found to be most active agent against M. tuberculosis H37Rv (MTB) and INH resistant M. tuberculosis (INHR-MTB), with minimum inhibitory concentration of 0.12 microM, when compared to INH 5.6-fold more active against MTB and 78-fold more active against INHR-MTB, respectively.

UI MeSH Term Description Entries
D007538 Isoniazid Antibacterial agent used primarily as a tuberculostatic. It remains the treatment of choice for tuberculosis. Isonicotinic Acid Hydrazide,Ftivazide,Isonex,Isonicotinic Acid Vanillylidenehydrazide,Phthivazid,Phthivazide,Tubazide,Acid Vanillylidenehydrazide, Isonicotinic,Hydrazide, Isonicotinic Acid,Vanillylidenehydrazide, Isonicotinic Acid
D008826 Microbial Sensitivity Tests Any tests that demonstrate the relative efficacy of different chemotherapeutic agents against specific microorganisms (i.e., bacteria, fungi, viruses). Bacterial Sensitivity Tests,Drug Sensitivity Assay, Microbial,Minimum Inhibitory Concentration,Antibacterial Susceptibility Breakpoint Determination,Antibiogram,Antimicrobial Susceptibility Breakpoint Determination,Bacterial Sensitivity Test,Breakpoint Determination, Antibacterial Susceptibility,Breakpoint Determination, Antimicrobial Susceptibility,Fungal Drug Sensitivity Tests,Fungus Drug Sensitivity Tests,Sensitivity Test, Bacterial,Sensitivity Tests, Bacterial,Test, Bacterial Sensitivity,Tests, Bacterial Sensitivity,Viral Drug Sensitivity Tests,Virus Drug Sensitivity Tests,Antibiograms,Concentration, Minimum Inhibitory,Concentrations, Minimum Inhibitory,Inhibitory Concentration, Minimum,Inhibitory Concentrations, Minimum,Microbial Sensitivity Test,Minimum Inhibitory Concentrations,Sensitivity Test, Microbial,Sensitivity Tests, Microbial,Test, Microbial Sensitivity,Tests, Microbial Sensitivity
D009169 Mycobacterium tuberculosis A species of gram-positive, aerobic bacteria that produces TUBERCULOSIS in humans, other primates, CATTLE; DOGS; and some other animals which have contact with humans. Growth tends to be in serpentine, cordlike masses in which the bacilli show a parallel orientation. Mycobacterium tuberculosis H37Rv
D009682 Magnetic Resonance Spectroscopy Spectroscopic method of measuring the magnetic moment of elementary particles such as atomic nuclei, protons or electrons. It is employed in clinical applications such as NMR Tomography (MAGNETIC RESONANCE IMAGING). In Vivo NMR Spectroscopy,MR Spectroscopy,Magnetic Resonance,NMR Spectroscopy,NMR Spectroscopy, In Vivo,Nuclear Magnetic Resonance,Spectroscopy, Magnetic Resonance,Spectroscopy, NMR,Spectroscopy, Nuclear Magnetic Resonance,Magnetic Resonance Spectroscopies,Magnetic Resonance, Nuclear,NMR Spectroscopies,Resonance Spectroscopy, Magnetic,Resonance, Magnetic,Resonance, Nuclear Magnetic,Spectroscopies, NMR,Spectroscopy, MR
D011720 Pyrazoles Azoles of two nitrogens at the 1,2 positions, next to each other, in contrast with IMIDAZOLES in which they are at the 1,3 positions.
D000085 Acetates Derivatives of ACETIC ACID. Included under this heading are a broad variety of acid forms, salts, esters, and amides that contain the carboxymethane structure. Acetate,Acetic Acid Esters,Acetic Acids,Acids, Acetic,Esters, Acetic Acid
D000995 Antitubercular Agents Drugs used in the treatment of tuberculosis. They are divided into two main classes: "first-line" agents, those with the greatest efficacy and acceptable degrees of toxicity used successfully in the great majority of cases; and "second-line" drugs used in drug-resistant cases or those in which some other patient-related condition has compromised the effectiveness of primary therapy. Anti-Tuberculosis Agent,Anti-Tuberculosis Agents,Anti-Tuberculosis Drug,Anti-Tuberculosis Drugs,Antitubercular Agent,Antitubercular Drug,Tuberculostatic Agent,Tuberculostatic Agents,Antitubercular Drugs,Agent, Anti-Tuberculosis,Agent, Antitubercular,Agent, Tuberculostatic,Anti Tuberculosis Agent,Anti Tuberculosis Agents,Anti Tuberculosis Drug,Anti Tuberculosis Drugs,Drug, Anti-Tuberculosis,Drug, Antitubercular
D013055 Spectrophotometry, Infrared Spectrophotometry in the infrared region, usually for the purpose of chemical analysis through measurement of absorption spectra associated with rotational and vibrational energy levels of molecules. (McGraw-Hill Dictionary of Scientific and Technical Terms, 4th ed) IR Spectra,Infrared Spectrophotometry,IR Spectras,Spectra, IR
D047188 Chalcones Derivatives of CHALCONE that are important intermediates in the formation of FLAVONOIDS with anti-fungal, anti-bacterial, anti-inflammatory, and anti-tumor properties. 1,3-Diphenyl-propanediones,1,3-Diphenyl-propenones,1,3-Diphenylpropanediones,1,3-Diphenylpropenones,Chalconoids,1,3 Diphenyl propanediones,1,3 Diphenyl propenones,1,3 Diphenylpropanediones,1,3 Diphenylpropenones

Related Publications

Mohamed Ashraf Ali, and Mohammad Shahar Yar, and Mahesh Kumar, and Ganesan Suresh Pandian
June 1975, Journal of pharmaceutical sciences,
Mohamed Ashraf Ali, and Mohammad Shahar Yar, and Mahesh Kumar, and Ganesan Suresh Pandian
October 2010, Journal of enzyme inhibition and medicinal chemistry,
Mohamed Ashraf Ali, and Mohammad Shahar Yar, and Mahesh Kumar, and Ganesan Suresh Pandian
February 2009, European journal of medicinal chemistry,
Mohamed Ashraf Ali, and Mohammad Shahar Yar, and Mahesh Kumar, and Ganesan Suresh Pandian
February 2012, Chemical biology & drug design,
Mohamed Ashraf Ali, and Mohammad Shahar Yar, and Mahesh Kumar, and Ganesan Suresh Pandian
May 2010, European journal of medicinal chemistry,
Mohamed Ashraf Ali, and Mohammad Shahar Yar, and Mahesh Kumar, and Ganesan Suresh Pandian
February 2007, European journal of medicinal chemistry,
Mohamed Ashraf Ali, and Mohammad Shahar Yar, and Mahesh Kumar, and Ganesan Suresh Pandian
July 2013, Chemistry Central journal,
Mohamed Ashraf Ali, and Mohammad Shahar Yar, and Mahesh Kumar, and Ganesan Suresh Pandian
July 2012, Archiv der Pharmazie,
Mohamed Ashraf Ali, and Mohammad Shahar Yar, and Mahesh Kumar, and Ganesan Suresh Pandian
June 2019, Bioorganic chemistry,
Mohamed Ashraf Ali, and Mohammad Shahar Yar, and Mahesh Kumar, and Ganesan Suresh Pandian
July 2004, Archives of pharmacal research,
Copied contents to your clipboard!