5159-59-1Relevant articles and documents
Synthesis, crystal structure and dynamic behavior of naphthalene-based calix[3]amide: Cyclic trimers of 2-alkylamino-6-naphthoic acid
Katagiri, Kosuke,Sawano, Kanako,Okada, Miho,Yoshiyasu, Shiho,Shiroyama, Reiko,Ikejima, Norio,Masu, Hyuma,Kato, Takako,Tominaga, Masahide,Azumaya, Isao
, p. 346 - 350 (2008)
Treatment of 6-amino-2-naphthoic acid with dichlorotriphenylphosphorane afforded a new naphthalene ring-based calix[3]amide in moderate yield. The macrocyclic calix[3]amide exists in an anti-form in the crystalline state and forms a channel structure along its b axis. In CDCl3 solution it exists in equilibrium between the syn- and anti-forms in solution (100:57). The energy barrier between the anti- to syn-forms was calculated to be 17.8 ± 0.2 kcal/mol.
Discovery of new photoactivatable diaryltetrazoles for photoclick chemistry via scaffold hopping
Yu, Zhipeng,Ho, Lok Yin,Wang, Zhiyong,Lin, Qing
supporting information; scheme or table, p. 5033 - 5036 (2011/10/09)
We report the discovery of two long-wavelength (365 nm) photoactivatable diaryltetrazoles through screening a small library of diaryltetrazoles that were designed using a 'scaffold hopping' strategy. A naphthalene-derived tetrazole showed excellent reacti
Modulation on C- and N-terminal moieties of a series of potent and selective linear tachykinin NK2 receptor antagonists
Gensini, Martina,Altamura, Maria,Dimoulas, Tula,Fedi, Valentina,Giannotti, Danilo,Giuliani, Sandro,Guidi, Antonio,Harmat, Nicholas J. S.,Meini, Stefania,Nannicini, Rossano,Pasqui, Franco,Tramontana, Manuela,Triolo, Antonio,Maggi, Carlo Alberto
scheme or table, p. 65 - 78 (2010/11/16)
Herein we describe the synthesis of a series of new potent tachykinin NK2 receptor antagonists by the modulation of the Cand N-terminal moieties of ibodutant (MEN 15596, 1). The Nterminal benzo[b]thiophene ring was replaced by different substituted naphthalenes and benzofurans, while further modifications were evaluated at the C-terminal tetrahydropyran moiety. Most compounds demonstrated a high affinity for the human NK2 receptor and high in vitro antagonist potency, indicating that a wide range of substituents at both termini can be incorporated in the molecule without detrimental effects on the interactions with the NK2 receptor. Selected compounds were tested in vivo confirming their activity as NK2 antagonists. In particular, after both iv and id administration to guinea pig, compound 61b was able to antagonize NK2-induced colonic contractions with a potency and duration-of-action fully comparable to the reference compound 1 (MEN 15596, ibodutant).
