64778-46-7Relevant academic research and scientific papers
Exploring antimicrobial and antimycobacterial potential of novel quinazoline based thiazolidin-4-ones
Patel, Amit B.,Kumari, Premlata,Chikhalia, Kishor H.
, p. 260 - 271 (2015/03/04)
To affiliate multiple bioactivities in a compact heteronuclei, two series of N-phenyl acetamides and thiazolidin-4-ones based quinazolines have been synthesized. The in vitro antimicrobial efficacy of the synthesized analogs has been assessed against two Gram-positive bacteria, six Gram-negative bacteria and four fungi. Furthermore, the final analogs have also been screened against Mycobacterium tuberculosis H37Rv in order to explore the antituberculosis activity. Results of the antimicrobial screening has shown that a majority of compounds exhibit significant antibacterial and noticeable antifungal activities, with minimum inhibitory concentrations 3.12-50 μg/mL against several microorganisms. Some of the synthesized analogs have also elicited noticeable inhibitory action against M. tuberculosis H37Rv strain. The best results are observed amongst the thiazolidinone substituted analogs. The structures of the synthesized analogs are corroborated on the basis of IR, 1H and 13C NMR, mass spectrometric and elemental analysis.
Access to antimycobacterial and anticancer potential of some fused quinazolines
Patel, Amit B.,Chikhalia, Kishor H.,Kumari, Premlata
, p. 4439 - 4455 (2015/06/30)
Two series of some various N-phenyl/benzothiazolyl acetamide-fused quinazoline derivatives were synthesized and tested for their antimycobacterial activity against M. tuberculosis H37Rv. Moreover, the synthesized analogs were also screened against human P
Synthesis and biological evaluation of novel quinazoline derivatives obtained by Suzuki C-C coupling
Patel, Amit B.,Chikhalia, Kishor H.,Kumari, Premlata
, p. 2338 - 2346 (2014/05/06)
In the present investigation, two series of novel urea/thiourea-based quinazoline analogs (7a-g/8a-g) have been synthesized by introducing C-C Suzuki coupling between quinazoline and phenyl ring followed by condensation of various N-phenyl isocyanates/iso
Design, synthesis and computational studies of new benzothiazole substituted quinazolines as potential antimicrobial agents
Patel, Amit B.,Sahoo, Suban K.,Chikhalia, Kishor H.,Kumari, Premlata
, p. 957 - 966 (2013/12/04)
Some novel N-(benzo[d]thiazol-2-yl)-2-((4-(4-(m-tolyloxy)quinazolin-2yl) phenyl)amino)acetamides analogs (7a-j) have been synthesized. The synthetic approach exploits a consolidated protocol based on Suzuki coupling reaction on quinazoline ring. The analogs were tested for microbiological activity against eight bacteria (Staphylococcus aureus MTCC 96, Bacillus cereus MTCC 619, Escherichia coli MTCC 739, Pseudomonas aeruginosa MTCC 741, Klebsiella pneumoniae MTCC 109, Salmonella typhi MTCC 733, Proteus vulgaris MTCC 1771 and Shigella flexneri MTCC 1457) and four fungi (Aspergillus niger MTCC 282, Aspergillus fumigatus MTCC 343, Aspergillus clavatus MTCC 1323, and Candida albicans MTCC 183). Some of the synthesized analogs have demonstrated excellent antimicrobial activity (MICs: 3.12-25 μg/mL) as compared with the standards (MICs: 6.25-25 μg/mL). Density Functional Theory (DFT) calculations at the B3LYP/6-31G(d,p) level were performed to predict the molecular structure and electronic properties of the analogs. Further, the binding orientations of the potent analogs were validated by molecular docking studies. 2013 Bentham Science Publishers.
Hybrid diarylbenzopyrimidine non-nucleoside reverse transcriptase inhibitors as promising new leads for improved anti-HIV-1 chemotherapy
Zeng, Zhao-Sen,He, Qiu-Qin,Liang, Yong-Hong,Feng, Xiao-Qing,Chen, Fen-Er,Clercq, Erik De,Balzarini, Jan,Pannecouque, Christophe
experimental part, p. 5039 - 5047 (2010/09/05)
Molecular hybridization of the known anti-HIV-1 template DPC083 and etravirine based on docking model overlay has been generated a novel series of diarylbenzopyrimidine analogues (DABPs) (5a-z). These new hybrids were assessed for their activity against HIV in MT-4 cell cultures. Most of these compounds showed good activity against wild-type HIV-1 and mutant viruses. In particular, compound 5r showed the most potent activity against wild-type HIV-1 with an EC50 value of 1.8 nM, and with a selectivity index up to 111,954. It also proved more active against mutant L100I, K103N, Y188L, and K103N + Y181C RT HIV-1 strains than efavirenz.
Synthesis and evaluation on anticonvulsant and antidepressant activities of 5-alkoxy-tetrazolo[1,5-a]quinazolines
Wang, Huo-Jian,Wei, Cheng-Xi,Deng, Xian-Qing,Li, Fu-Lan,Quan, Zhe-Shan
experimental part, p. 671 - 675 (2010/07/06)
Several 5-alkoxy-tetrazolo[1,5-a]quinazoline derivatives have been synthesized by reacting 2,4-dichloroquinazoline with various phenols or aliphatic alcohol and then with sodium azide. The structures of these compounds have been confirmed by IR, MS,
