136465-98-0Relevant articles and documents
Antiviral drug and drug composition thereof
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Paragraph 0108; 0111; 0112, (2019/01/08)
The invention relates to an antiviral drug and a drug composition thereof, specially relates to a drug against human immunodeficiency virus (HIV) and a drug composition thereof, and particularly relates to a drug capable of serving as a retrovirus proteas
Synthesis of new thienyl ring containing HIV-1 protease inhibitors: Promising preliminary pharmacological evaluation against recombinant HIV-1 proteases
Bonini, Carlo,Chiummiento, Lucia,De Bonis, Margherita,Blasio, Nadia Di,Funicello, Maria,Lupattelli, Paolo,Pandolfo, Rocco,Tramutola, Francesco,Berti, Federico
scheme or table, p. 1451 - 1457 (2010/07/05)
A series of new thienyl ring containing analogues of nelfinavir and saquinavir with different, substitution patterns were synthesized from suitable enantiopure diols. Their inhibitory activity against wild type recombinant HIV-1 protease was evaluated. In general thienyl groups spaced from the core by a methylene group gave products showing IC50 in the nanomolar range, irrespective of the type and the substitution pattern of the heterocycle. The range of activity of the two most, active compounds is substantially maintained or even increased against two commonly selected mutants, under drug pressure, such as V32I and V82A.
Synthesis of the HIV-proteinase inhibitor Saquinavir: A challenge for process research
Goehring, Wolfgang,Gokhale, Surendra,Hilpert, Hans,Roessler, Felix,Schlageter, Markus,Vogt, Peter
, p. 532 - 537 (2007/10/03)
The task of process research, namely developing efficient, economically and technically as well as ecologically feasible syntheses in time, is demonstrated on the HIV-proteinase inhibitor Saquinavir (1), a complex molecule comprising six stereo-centres. Based on the first 26-step research synthesis furnishing a 10% overall yield, process research established a new, short 11-step synthesis affording a 50% overall yield.