Kumar Ashok, Sharma Shalabh, Bajaj Kiran, Sharma Shipra, Panwar Hemant, Singh Tripti, Srivastava V K
Medicinal Chemistry Division, Department of Pharmacology, L.L.R.M Medical College, (U.P.)-250004, Meerut, India.
Bioorg Med Chem. 2003 Nov 17;11(23):5293-9. doi: 10.1016/s0968-0896(03)00501-7.
Various 2-(substitutedphenylmethyleneimino)aminoacetylmethylene-3-(2'-substitutedindol-3'-yl)-halosubstituted-4(3H)quinazolinones (5a-5i) and 2-(substituted phenylaminomethyleneacetyl-4'-oxo-1'-thiazolidinyl-3-(2"-substitutedindol-3"-yl) 4(3H)-quinazolinones (6a-6i) have been synthesized in the present studies. The structure of these compounds have been elucidated by elemental (C, H, N) and spectral (IR, 1H NMR and mass) analysis. Furthermore, above said compounds were evaluated for their anti-inflammatory, analgesic, ulcerogenic activities and acute toxicity study. Compound 6d was found to be most potent. Compound exihibiting less ulcerogenic liability and ALD(50) >2000mg/kg po.
在本研究中已合成了多种2 -（取代苯基亚甲基亚氨基）氨基乙酰亚甲基-3 -（2'-取代吲哚-3'-基）-卤代取代-4（3H）喹唑啉酮（5a - 5i）和2 -（取代苯氨基亚甲基乙酰基-4'-氧代-1'-噻唑烷基-3 -（2''-取代吲哚-3''-基）4（3H）-喹唑啉酮（6a - 6i）。这些化合物的结构已通过元素分析（C、H、N）和光谱分析（红外光谱、1H核磁共振谱和质谱）得以阐明。此外，对上述化合物进行了抗炎、镇痛、致溃疡活性和急性毒性研究。发现化合物6d最为有效。该化合物显示出较低的致溃疡倾向且经口半数致死剂量（ALD50）>2000mg/kg。
