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

Bioorg Med Chem Lett. 2014 Mar 15;24(6):1493-5. doi: 10.1016/j.bmcl.2014.02.012.

Arif B Siddiqui ¹, Amit R Trivedi ², Vipul B Kataria ³, Viresh H Shah ³

Affiliations

1 Amneal Pharmaceuticals India Pvt Ltd, 882/1-871, Village Rajoda, Tal.: Bavla Dist.: Ahmedabad 382220, Gujarat, India. Electronic address: [email protected].
2 Division of Medicinal Chemistry, Department of Chemistry (DST-FIST Sponsored), Mahatma Gandhi Campus, Maharaja Krishnakumarsinhji Bhavnagar University, Bhavnagar 364002, Gujarat, India.
3 Department of Chemistry, Saurashtra University, Kalawad Road, Rajkot 360005, Gujarat, India.

PMID: 24582983 DOI: 10.1016/j.bmcl.2014.02.012

Abstract

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, (1)H NMR, (13)C 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 0.02μg/mL, making it more potent than first line antitubercular drug isoniazid.

Keywords

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

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