title: 4,5-Dihydro-1H-pyrazolo[3,4-d]pyrimidine containing phenothiazines as antitubercular agents.
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.
authors.affiliation: Amneal Pharmaceuticals India Pvt Ltd, 882/1-871, Village Rajoda, Tal.: Bavla Dist.: Ahmedabad 382220, Gujarat, India. Electronic address: drarifsiddiqui2013@gmail.com.
authors.forename: Arif B
authors.initials: AB
authors.lastname: Siddiqui
authors.affiliation: Division of Medicinal Chemistry, Department of Chemistry (DST-FIST Sponsored), Mahatma Gandhi Campus, Maharaja Krishnakumarsinhji Bhavnagar University, Bhavnagar 364002, Gujarat, India.
authors.forename: Amit R
authors.initials: AR
authors.lastname: Trivedi
authors.affiliation: Department of Chemistry, Saurashtra University, Kalawad Road, Rajkot 360005, Gujarat, India.
authors.forename: Vipul B
authors.initials: VB
authors.lastname: Kataria
authors.affiliation: Department of Chemistry, Saurashtra University, Kalawad Road, Rajkot 360005, Gujarat, India.
authors.forename: Viresh H
authors.initials: VH
authors.lastname: Shah
mesh_terms: D000818:Animals; D000995:Antitubercular Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D002470:Cell Survival / Q000187:drug effects; D002522:Chlorocebus aethiops; D008826:Microbial Sensitivity Tests; D009169:Mycobacterium tuberculosis / Q000187:drug effects; D010640:Phenothiazines / Q000737:chemistry*; D011720:Pyrazoles / Q000737:chemistry* / Q000494:pharmacology*; D011725:Pyridines / Q000737:chemistry* / Q000494:pharmacology*; D014709:Vero Cells
chemical_list: D000995:Antitubercular Agents; D010640:Phenothiazines; D011720:Pyrazoles; D011725:Pyridines; C118531:pyrazolopyridine; C031637:phenothiazine
keywords: Antitubercular activity; Biginelli multicomponent reaction; Cytotoxicity; Dihydropyrazolo[3,4-d]pyrimidine; Phenothiazines