Bandurco V T, Wong E M, Levine S D, Hajos Z G
J Med Chem. 1981 Dec;24(12):1455-60. doi: 10.1021/jm00144a017.
The synthesis of a variety of pyrrolo[1,2-c]quinazolines and pyrrolo[1,2-c]quinazolinones is described. Several of these compounds have exhibited antihypertensive properties in the spontaneously hypertensive rat (SHR). Structure-activity comparisons have indicated that optimal activity is obtained in both the 2-carbethoxydihydroquinazoline series (C) and 2-carbethoxyquinazolinone series (D) when there is either a carbethoxy or cyanoethyl group at position 6 and no substitution in the benzene ring, while optimal activity is obtained in the 2-methyl-quinazolinone series (D) when both position 6 and the benzene ring are unsubstituted.
本文描述了多种吡咯并[1,2 - c]喹唑啉和吡咯并[1,2 - c]喹唑啉酮的合成。其中几种化合物在自发性高血压大鼠（SHR）中表现出抗高血压特性。构效关系比较表明，在2 - 乙氧羰基二氢喹唑啉系列（C）和2 - 乙氧羰基喹唑啉酮系列（D）中，当6位有乙氧羰基或氰乙基且苯环无取代时可获得最佳活性，而在2 - 甲基喹唑啉酮系列（D）中，当6位和苯环均无取代时可获得最佳活性。
