De Rosa, Maria; Unge, Johan; Motwani, Hitesh V.; Rosenquist, Aasa; Vrang, Lotta; Wallberg, Hans; Larhed, Mats published the artcile< Synthesis of P1'-Functionalized Macrocyclic Transition-State Mimicking HIV-1 Protease Inhibitors Encompassing a Tertiary Alcohol>, Category: thiazole, the main research area is tertiary alc linear macrocyclic peptidomimetic preparation HIV1 protease inhibitor.
Seven novel tertiary alc.-containing linear HIV-1 protease inhibitors (PIs), decorated at the para position of the benzyl group in the P1′ side with (hetero)aromatic moieties, were synthesized and biol. evaluated. To study the inhibition and antiviral activity effect of P1-P3 macrocyclization, 14- and 15-membered macrocyclic PIs were prepared by ring-closing metathesis of the corresponding linear PIs. The macrocycles were more active than the linear precursors and compound 10f, with a 2-thiazolyl group in the P1′ position, was the most potent PI of this new series (Ki = 2.2 nM, EC50 0.2 μM). Co-crystallized complexes of both linear and macrocyclic PIs with the HIV-1 protease enzyme were prepared and analyzed.
Journal of Medicinal Chemistry published new progress about Anti-HIV agents. 198904-53-9 belongs to class thiazole, and the molecular formula is C10H7NOS, Category: thiazole.
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica