1998
DOI: 10.1016/s0040-4039(98)01075-2
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Epsilon-lactam analogs of the anthelmintic cyclodepsipeptide PF1022A

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Cited by 17 publications
(7 citation statements)
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“…Backbone rigidization, e.g. synthesis of conformationally restricted analogues of 1 by fusing fivemembered (Scherkenbeck et al 1999(Scherkenbeck et al , 2002 to sevenmembered lactam rings (Dutton and Lee 1998;Lee et al 2002;Dutton et al 2003) or b-turn mimics (Dyker et al 2004) within the 24-membered macrocycle.…”
Section: Introductionmentioning
confidence: 99%
“…Backbone rigidization, e.g. synthesis of conformationally restricted analogues of 1 by fusing fivemembered (Scherkenbeck et al 1999(Scherkenbeck et al , 2002 to sevenmembered lactam rings (Dutton and Lee 1998;Lee et al 2002;Dutton et al 2003) or b-turn mimics (Dyker et al 2004) within the 24-membered macrocycle.…”
Section: Introductionmentioning
confidence: 99%
“…Studies of structure‐activity relationships in compounds related to 1 have mainly been concerned with variations of the α‐amino acids or their N ‐alkyl substituents6 and of side‐chains of the α‐hydroxycarboxylic acids 7. 8 Recently, conformationally restricted analogues of 1 were prepared by fusing a seven‐membered lactam ring onto the macrocycle9 and the chemical synthesis of a mono ‐proline PF1022A analogue10 has also been reported. Because of the lack of suitable functional groups in the cyclic octadepsipeptides (general structure I , Fig 2) we have now focussed our attention on the thioamidation of the backbone depsipeptide bond.…”
Section: Introductionmentioning
confidence: 99%
“…Neste sentido, o desenvolvimento de moléculas ativas requer características estruturais que as tornem metabolicamente estáveis com a manutenção de suas atividades biológicas. Os avanços dos estudos das interações de ligantes ou substratos peptídicos de receptores ou enzimas se dão pela obtenção de peptideomiméticos, análogos não-peptídicos, ou ainda pela utilização de novos métodos de obtenção de fármacos, como por exemplo a química combinatória 71 . Esta estratégia leva à produção de coleções de moléculas diferentes preparadas por síntese ou biossíntese e testadas quanto suas atividades biológicas, acelerando o processo de obtenção de um novo fármaco 72 .…”
Section: Perspectivasunclassified