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.