1619-56-3Relevant academic research and scientific papers
Synthesis of variously 9,9-dialkylated octahydropyrimido [3,4-a]-s-triazines with potential antifungal activity
Ghaib, Amar,Menager, Sabine,Verite, Philippe,Lafont, Olivier
, p. 109 - 116 (2002)
9,9-Dialkyloctahydropyrimido[3,4-a]-s-triazines were synthesized by iminodimethylation reaction between a 5,5-dialkyl-6-aminopyrimidine-2,4(3H,5H)-dione, a substituted aniline and two moles of formaldehyde. The synthesis of 5,5-dialkyl-6-aminopyrimidinedione consisted of the condensation of urea with ethyl 2,2-dialkylcyanoacetates. 18 Octahydropyrimido[3,4-a]-s-triazines were synthesized and compounds resulting from a supplementary aminomethylation were also obtained. Most of these compounds were tested for antifungal activity in vitro. Only 9,9-dibutyl-6,8-dioxo-3(2-chlorophenyl)2,3,4,5,6,7,8,9-octahydropyrimido[3, 4-a]-s-triazine showed some activity against Microsporum canis.
Au-catalyzed synthesis of 5,6-dihydro-8H-indolizin-7-ones from N-(pent-2-en-4-ynyl)-β-lactams
Peng, Yu,Yu, Meng,Zhang, Liming
supporting information; experimental part, p. 5187 - 5190 (2009/06/06)
(Chemical Equation Presented) Au-catalyzed synthesis of 5,6-dihydro-8H-indolizin-7-ones from readily available N-(pent-2-en-4-ynyl)- β-lactams is developed. In this reaction, a 5-exo-dig cyclization of the β-lactam nitrogen to the Au-activated C-C triple bond is followed by heterolytic fragmentation of the amide bond, forming a highly nucleophilic acyl cation. An expedient formal synthesis of indolizidine 167B was easily achieved using this new method.
The design and synthesis of potent cyclic peptide VCAM-VLA-4 antagonists incorporating an achiral Asp-Pro mimetic
Fotouhi, Nader,Joshi, Pramod,Fry, David,Cook, Charles,Tilley, Jefferson W.,Kaplan, Gerry,Hanglow, Angela,Rowan, Karen,Schwinge, Virginia,Wolitzky, Barry
, p. 1171 - 1173 (2007/10/03)
The Asp-Pro sequence of the cyclic peptide Ac-HN-Tyr-Cys*-Asp-Pro-Cys*-OH (1) could be replaced with the achiral dipeptide mimetic 1-(2-aminoethyl)cyclpentylcarboxylic acid with retention of potent inhibition of the VCAM-VLA-4 interaction. (C) Elsevier Science Ltd. All rights reserved.
Synthesis and biological evaluation of cryptophycin analogs with substitution at C-6 (fragment C region)
Varie, David L.,Shih, Chuan,Hay, David A,Andis, Sherri L.,Corbett, Tom H.,Gossett, Lynn S.,Janisse, Samantha K.,Martinelli, Michael J.,Moher, Eric D.,Schultz, Richard M.,Toth, John E.
, p. 369 - 374 (2007/10/03)
Analogs of the antitumor agents cryptophycins 1 and 8 with dialkyl substitution at C-6 (fragment C) were synthesized and evaluated for in vitro cytotoxicity against human leukemia cells (CCRF-CEM). The activity of these analogs decreased as the size of the substituents at C-6 increased. The C-6 spirocylopropyl compound (2g) was highly potent in vitro and showed excellent antitumor activity in animal models.
