13037-46-2Relevant articles and documents
Structural features of tetraazathiapentalenes fused with pyrimidine and/or pyridine rings. Experimental evaluation of the nature of hypervalent N-S-N bond by restricted internal rotation of the pyrimidine ring
Ohkata, Katsuo,Ohsugi, Minoru,Yamamoto, Kazuhiro,Ohsawa, Mika,Akiba, Kin-Ya
, p. 6355 - 6369 (1996)
A series of neutral (8-10), monomethylated (12-14), and dimethylated (17) 10-S-3 sulfuranes, derivatives of tetraazathiapentalenes fused with pyrimidine and/or pyridine ring, were prepared. These molecules are planar, and bond energies of the hypervalent
Antimicrobial activities of some synthesized 1-(3-(2-methylphenyl)-4-Oxo-3H-quinazolin-2-yl-4-(substituted)thiosemicarbazide derivatives
Alagarsamy,Anjana,Sulthana,Parthiban,Solomon, V. Raja
, p. 332 - 339 (2016/07/06)
The substituted thiosemicarbazide moiety was placed at the C-2 position and 2-methylphenyl group at N-3 position of quinazoline ring and obtained compounds were tested for their antitubercular activities and antibacterial activities against selected gram-positive and gram-negative bacteria. The target compounds 1-(3-(2-methylphenyl)-4-oxo-3H-quinazolin-2-yl)-4-(substituted) thiosemicarbazides were obtained by the reaction of 2-hydrazino-3-(2-methylphenyl) quinazolin-4(3H)-one with different dithiocarbamic acid methyl ester derivatives. All synthesized compounds were also screened for their antimicrobial activity against selective gram-positive and gram-negative bacteria by agar dilution method. Among the series, 1-[3-(2-methylphenyl)-4-oxo-3H-quinazolin-2-yl]-4-[4-chlorophenyl]-thiosemicarbazide exhibited the most potent activity against S. typhi, E. coli, and B. subtilis, while 1-[3-(2-methylphenyl)-4-oxo-3H-quinazolin-2-yl]-4-[4-nitrophenyl]-thiosemicarbazide was the most potent against E. coli, B. subtilis, P. aeruginosa, S. typhi, and S. flexneri. These two compounds exhibited the antitubercular activity at the minimum concentration (3 μg/mL) that offered potential for further optimization and development of new antitubercular agents. The obtained results demonstrated promising antimicrobial and antitubercular activities of the synthesized quinazoline compounds which could be used as new scaffolds for improving their antimicrobial activity.
Design, synthesis and biological evaluation of novel HSP70 inhibitors: N, N′-disubstituted thiourea derivatives
Zeng, Yan-Qun,Cao, Rui-Yuan,Yang, Jian-Ling,Li, Xing-Zhou,Li, Song,Zhong, Wu
, p. 83 - 95 (2016/05/24)
As novel heat shock protein 70 (HSP70) inhibitors, N, N′-disubstituted thiourea derivatives were designed and synthesized based on the X-ray structure of the ATPase domain (nucleotide binding domain, NBD). An ATPase activity inhibition assay revealed that these compounds effectively inhibited HSP70 ATPase activity. The results revealed that the compounds 370/371/374/379/380//392/394/397/404/405 and 407 can inhibit the HSP70 ATPase turnover with high percentages of inhibition: 50.42, 38.46, 50.45, 44.12, 47.13, 50.50, 40.95, 65.36, 46.23, 35.78, and 58.37 in 200 μM, respectively. Significant synergies with lapatinib were observed for compound 379 and compound 405 in the BT474 breast cancer cell line. A structure-function analysis revealed that most of the thiourea derivatives exhibited cooperative action with lapatinib in the BT474 cancer cell line and the BT/LapR1.0 lapatinib-resistant cell line. HSP70 inhibitors may be developed as synergetic drugs in drug-resistant cancer therapy.
Synthesis and pharmacological investigation of novel 1-alkyl-4-(4- substituted aryl/heteroaryl)-1,2,4-triazolo[4,3-a]quinazolin-5(4H)-ones as a new class of H1-antihistaminic agents
Alagarsamy, Veerachamy,Yadav, Mangae Ram,Giridhar, Rajani
, p. 834 - 841 (2008/02/08)
A series of novel 1-alkyl-4-(4-substituted aryl/heteroaryl)-1,2,4- triazolo[4,3-a] quinazolin-5(4H)-ones were synthesized by the cyclization of 2-hydrazino-3-(4-subst. aryl/heteroaryl) quinazolin-4(3H)-one with various carbon donors. The starting material
