4,5-Dihydro-1H-pyrazolo[3,4-d] pyrimidine containing phenothiazines as antitubercular agents

作者：Siddiqui Arif B^*; Trivedi Amit R; Kataria Vipul B; Shah Viresh H

来源：Bioorganic & Medicinal Chemistry Letters, 2014, 24(6): 1493-1495.

DOI：10.1016/j.bmcl.2014.02.012

• Dihydropyrazolo[3,4-d]pyrimidine
• Phenothiazines
• Biginelli multicomponent reaction
• Cytotoxicity
• Antitubercular activity

A series of novel dihydropyrazolo[3,4-d]pyrimidine derivatives bearing a phenothiazine nucleus were synthesized in excellent yields via a modified Biginelli multicomponent reaction. The newly synthesized compounds were characterized by IR, H-1 NMR, C-13 NMR, Mass spectra and elemental analysis followed by antimycobacterial screening. Among all the screened compounds, compound 4g showed most pronounced activity against Mycobacterium tuberculosis (Mtb) with minimum inhibitory concentration (MIC) of 0.02 mu g/mL, making it more potent than first line antitubercular drug isoniazid.

• 出版日期2014-3-15