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

Siddiqui, Arif B.; Trivedi, Anjali; Kataria, Vipul B.; Shah, V. H.

doi:10.1016/j.bmcl.2014.02.012

Cited by 38 publications

(6 citation statements)

References 31 publications

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“…Moreover, the nitroimidazopyran PA‐824 has potent in vitro activity against M. tuberculosis , a narrow spectrum of activity limited primarily to the M. tuberculosis complex, and no demonstrable cross‐resistance to a variety of antituberculosis drugs . Keeping this in view and in continuation of our previous work , it was envisaged that the design, synthesize, and investigation of in vitro antitubercular potency of new prototypes which include advantage of dual pharmacophore of 1,4‐dihyropyridine and imidazole in single molecular framework is worth the attempt.…”

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confidence: 92%

Design, Synthesis, and Biological Evaluation of 1,4‐dihydropyridine Derivatives as Potent Antitubercular Agents

et al. 2015

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A series of novel 1,4-dihydropyridine-3,5-dicarbamoyl derivatives bearing an imidazole nucleus at C-4 position were synthesized in excellent yields via multicomponent Hantzsch reaction. The newly synthesized compounds were characterized by IR, (1) H NMR, (13) C NMR, and mass spectroscopy. The synthesized compounds 3a-p were screened for antitubercular activity. Among all the screened compounds, compounds 3j and 3m showed most prominent activity against Mycobacterium tuberculosis with minimum inhibitory concentration of 0.02 μg/mL and SI > 500, making it more potent than first-line antitubercular drug isoniazid. In addition, these compounds displayed relatively low cytotoxicity.

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confidence: 92%

Design, Synthesis, and Biological Evaluation of 1,4‐dihydropyridine Derivatives as Potent Antitubercular Agents

et al. 2015

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“…As a result of ongoing research in the series of substituted pyrimidines, new compounds have been discovered that have antibacterial and antimicrobial [1][2][3][4], antifungal [5,6], antitumor [7][8][9], anti-inflammatory [10,11], anticonvulsant [12,13], antioxidant [14,15], antiviral [16,17], anti-HIV [18][19][20], anti-tuberculosis [21,22], antimalarial [23][24][25], cardiotonic [26,27] activity. Some pyrimidine derivatives were inhibitors of acetylcholinesterase [28,29].…”

Section: Introductionmentioning

confidence: 99%

Ultrasound-Assisted Green Syntheses of Novel Pyrimidine Derivatives and Their Comparison With Conventional Methods

Pivazyan¹,

Ghazaryan²,

Karapetyan³

et al. 2022

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Ultrasound-assisted green syntheses of novel potentially bioactive pyrimidine derivatives have been carried out. The same compounds were obtained by conventional methods of synthesis, and the reaction times and yields of final products obtained by these two methods were compared. It was found that the time of utrasound-promoted reactions was reduced by almost 6-96 times, and their yields were equal or turn out to be greater compared to the traditional approach. The synthesized compounds showed a pronounced stimulating effect on plant growth. The most active derivatives were selected for deeper biological studies and subsequent field trials.

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“…Recognizing these serious facts, we initiated a programme to synthesize and screen diverse heterocyclic entities like pyridines, phenothiazines and pyrimidines as potential anti-tubercular agents. Based on our previous results [9,10,11,14], we set upon a programme of making antitubercular agents, using the central dihydropyrimidine as the template and adding versatile substituents on the various positions of dihydropyrimidine ring and subjected them to antimycobacterial screening.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and biological evaluation of pyrimidinyl sulphonamide derivatives as promising class of antitubercular agents

Bhuva

Talpara

Singala

et al. 2017

Journal of Saudi Chemical Society

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A small library of compounds are synthesized and evaluated for their in vitro antitubercular activity against Mycobacterium tuberculosis H37RV. Two compounds, -[(2 0 ,4 0 -dinitrophenyl) sulphonyl]-4-(p-aminophenylsulphonylamino)-6-(2 0 -chlorophenyl)-pyrimidine-5-carboxamide F b and 2-hydrazino-4-(p-aminophenylsulphonylamino)-6-(2 0 -chlorophenyl)-pyrimidine-5-carboxamide D b were found to be the most active compounds in vitro with MIC of 0.02 lg/mL against MTB and were more potent compared to isoniazid (MIC: 0.03 lg/mL). ª 2015 The Authors. Production and hosting by Elsevier B.V. on behalf of King Saud University. This is an open access article under the CC BY-NC-ND license (http://creativecommons.org/licenses/by-nc-nd/4.0/).

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

Cited by 38 publications

References 31 publications

Design, Synthesis, and Biological Evaluation of 1,4‐dihydropyridine Derivatives as Potent Antitubercular Agents

Design, Synthesis, and Biological Evaluation of 1,4‐dihydropyridine Derivatives as Potent Antitubercular Agents

Ultrasound-Assisted Green Syntheses of Novel Pyrimidine Derivatives and Their Comparison With Conventional Methods

Synthesis and biological evaluation of pyrimidinyl sulphonamide derivatives as promising class of antitubercular agents

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