Facile one-pot synthesis and antimycobacterial evaluation of pyrazolo[3,4-d]pyrimidines.
The present article describes a facile one-pot synthesis of a series of eight pyrazolo[3,4-d]pyrimidines 4a-h which were evaluated for their in-vitro antibacterial activity against Mycobacterium tuberculosis H37Rv using the Alamar-Blue susceptibility test and the activity expressed as the minimum inhibitory concentration (MIC) in mg/mL. The compounds 4b, 4c, 4d, and 4g exhibited the best results (1.2 microg/mL) when compared with first-line drugs such as isoniazid (INH) and rifampicin (RIP). Therefore, this class of compounds could be a good starting point to develop new lead compounds in the treatment of multidrug-resistant tuberculosis.
Chemical Research Laboratory, Department of Chemistry, Saurashtra University, Rajkot, India.
Amit
A
Trivedi
Dipti
D
Dodiya
Janak
J
Surani
Samir
S
Jarsania
Hitesh
H
Mathukiya
Naresh
N
Ravat
Viresh
V
Shah
D000995:Antitubercular Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D007538:Isoniazid / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D009169:Mycobacterium tuberculosis / Q000187:drug effects*; D010078:Oxazines; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000494:pharmacology; D012293:Rifampin / Q000494:pharmacology; D013329:Structure-Activity Relationship; D018088:Tuberculosis, Multidrug-Resistant / Q000188:drug therapy; D014966:Xanthenes
D000995:Antitubercular Agents; D010078:Oxazines; D011743:Pyrimidines; D014966:Xanthenes; C005843:resazurin; D007538:Isoniazid; D012293:Rifampin