… -based inhibitors of HIV protease. Structure-activity studies of acylated 2, 4-diamino-1, 5-diphenyl-3-hydroxypentane and 2, 5-diamino-1, 6-diphenylhexane-3, 4-diol
…, L Codacovi, XC Wang, WE Kohlbrenner…
Index: Kempf, Dale J.; Codacovi, Lynnmarie; Wang, Xiu Chun; Kohlbrenner, William E.; Wideburg, Norman E.; et al. Journal of Medicinal Chemistry, 1993 , vol. 36, # 3 p. 320 - 330
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Citation Number: 142
Abstract
The structure-activity relationships in two series of novel, symmetry-based inhibitors of HIV protease, the enzyme responsible for maturation of the human immunodeficiency virus, are described. Beginning with lead compounds 3-6, the effect of adding polar, heterocyclic end groups to one or both ends of the symmetric or pseudosymmetric inhibitors was probed. Aqueous solubility was enhanced> 1000-fold while maintaining potent inhibition of ...
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