Synthesis and antimycobacterial evaluation of various 6-substituted pyrazolo[3,4-d]pyrimidine derivatives.
Various pyrazolo[3,4-d]pyrimidines carrying a variety of substituents in the 6-position have been synthesised and their ability to inhibit growth of Mycobacterium tuberculosis in vitro has been determined. Compounds 5a, 5b, 6c, 7a, 7b, 8d, 8e and 8f demonstrated a minimum inhibitory concentration (MIC) of <6.25 µg/mL and were found to be active against Mycobacterium tuberculosis strain H(37)RV. Compound 8d was found to be the most active compound in vitro with a MIC of <6.25 µg/mL and inhibitory concentration IC(90) of 1.53 µg/mL.
Department of Chemistry, Saurashtra University, Rajkot, India.
Amit
A
Trivedi
Shailesh
S
Vaghasiya
Bipin
B
Dholariya
Dipti
D
Dodiya
Viresh
V
Shah
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D015195:Drug Design; D020128:Inhibitory Concentration 50; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D009169:Mycobacterium tuberculosis / Q000187:drug effects*; D009574:Nitro Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014376:Tuberculosis / Q000188:drug therapy
C556604:6-(2,4-dinitrophenylthio)-4-(3-nitrophenyl)-3-methyl-1-phenyl-4,5-dihydro-1H-pyrazolo(3,4-d)pyrimidine; D000900:Anti-Bacterial Agents; D009574:Nitro Compounds; D011720:Pyrazoles; D011743:Pyrimidines