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Bioorg Med Chem Lett. 2014 Mar 15;24(6):1493-5. doi: 10.1016/j.bmcl.2014.02.012. Epub 2014 Feb 14.

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

Author information

1
Amneal Pharmaceuticals India Pvt Ltd, 882/1-871, Village Rajoda, Tal.: Bavla Dist.: Ahmedabad 382220, Gujarat, India. Electronic address: drarifsiddiqui2013@gmail.com.
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.

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

PMID:
24582983
DOI:
10.1016/j.bmcl.2014.02.012
[Indexed for MEDLINE]
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