SYNTHESIS AND ANTI-HIV ACTIVITY OF OPYRROLO[1,2-B][1,2,5]BENZOTHIADIAZEPINE-11-ACETIC ACID 5,5-DIOXIDE DERIVATIVES AND RELATED-COMPOUNDS

The synthesis and the in vitro anti-HIV-l activity of novel pyrrolo an nulated benzothiadiazepine acetic acids and some related derivatives a re reported. The new compounds share chemical features with pyrrolo[1, 2-d][1,4]benzodiazepin-6-one 1 and Ro 5-3335 pyrrylbenzodiazepinone 4, two inhibitors of HIV-replication at the level of reverse transcripta se (RT) and transcriptional transactivation by Tat, respectively. Two derivatives, namely methyl 2-b][1,2,5]benzothidiazapine-11-acetic-5,5- dioxide (5a) and 2,1-d]pyrrolo[1,2-b][1,2,5]benzothiadiazepin-2-one 8, 8-dioxide (7a), were found to exhibit a significant, although not very potent, activity against human immunodeficiency virus Type 1 (HIV-1).