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EnglishA series of N-aryl heteroarylisopropanolamines in which an indole or a 3-arylpyrrole moiety was linked to an aryl group through an isopropanolamine linker, were designed and synthesized as potential anti-HIV-1-PR agents. Series was tested for their ability in blocking PR activity. As a rule, indole derivatives of class I exhibited more potency than pyrrole analogues of class 2 while tert-butylamide substituents increased anti-PR potency. In fact, bis tert-butylamide le showed the highest activity with IC50 = 25 muM. Even if not very potent, a simple class of anti-PR agents, with a facile synthetic pathway was discovered. QSAR Studies on isopropanolamines I and 2 were performed in comparison with diarylbutanols, a new class of non peptidic anti-PR agents, recently discovered by Agouron Pharmaceuticals. QSAR and CoMFA models based on 30 diarylbutanols used as a training set were developed. The obtained models were used to investigate the binding mode of the newly synthesized derivatives I and 2. The results of this study suggest that N-aryl heteroarylisopropanolamines bind to the PR active site similarly to the diarylbutanols of Agouron. (C) 2002 Elsevier Science Ltd. All rights reserved.
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| Titolo: | Design, synthesis and QSAR studies on N-aryl heteroarylisopropanolamines, a new class of non-peptidic HIV-1 protease inhibitors | |
| Autori: | ||
| Data di pubblicazione: | 2002 | |
| Rivista: | ||
| Handle: | http://hdl.handle.net/11573/46051 | |
| Appartiene alla tipologia: | 01a Articolo in rivista |
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