- Development of 2-(4-oxoquinazolin-3(4 H)-yl)acetamide derivatives as novel enoyl-acyl carrier protein reductase (InhA) inhibitors for the treatment of tuberculosis
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InhA, the enoyl acyl carrier protein reductase of Mycobacterium tuberculosis (MTB) is an attractive target for developing novel anti-tubercular agents. Twenty eight 2-(4-oxoquinazolin-3(4H)-yl)acetamide derivatives were synthesized and evaluated for their in vitro MTB InhA inhibition. Compounds were further evaluated for their in vitro activity against drug sensitive and resistant MTB strains and cytotoxicity against RAW 264.7 cell line. Compounds were docked at the active site of InhA to understand their binding mode and differential scanning fluorimetry was performed to ascertain their protein interaction and stability.
- Pedgaonkar, Ganesh S.,Sridevi, Jonnalagadda Padma,Jeankumar, Variam Ullas,Saxena, Shalini,Devi, Parthiban Brindha,Renuka, Janupally,Yogeeswari, Perumal,Sriram, Dharmarajan
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p. 613 - 627
(2015/01/09)
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- Synthesis, antimalarial and antibacterial activities of 3-amino acid- and aryl amine-substituted 2-methyl- 3H-quinalzolin-4-ones
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A new series of 2-methyl-3H-quinazolinones substituted at the third position with amino acids (2-5) and aryl amine (6, 7) was designed, synthesized, and analyzed by infrared, NMR, and mass spectral analysis. Further, the compounds were screened for their in vivo antimalarial activity using the rodent malaria parasite Plasmodium yoelii (N-67) with the Swiss mice model. The compounds were also tested for their antibacterial activity. Birkhaueser Boston 2009.
- Nainar Meyyanathan, Subramania,Ramu, Mamillapalli,Suresh, Bhojraj
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experimental part
p. 993 - 999
(2011/12/01)
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- Synthesis and Biological Activity of 3-(5-Aryl-1,3,4-oxadiazol-2-ylmethyl)-2-methyl-4(3H)-quinazolinones
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Fourteen 3-(5-aryl-1,3,4-oxadiazol-2-ylmethyl)-2-methyl-4(3H)-quinazolinones (IV) have been prepared by condensation of the respective 2-methyl-4-oxo-3-quinazolineacetic acid hydrazides with different aromatic carboxylic acids in the presence of phosphoro
- Rao, A. Devender,Shankar, Ch. Ravi,Rao, A. Bhaskar,Reddy, V. Malla
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p. 665 - 667
(2007/10/02)
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