162927-72-2Relevant articles and documents
Long term storage inducer
-
Paragraph 0068-0070, (2021/02/25)
PROBLEM TO BE SOLVED: To provide a long-term memory inducing agent.SOLUTION: A long-term memory inducing agent comprises a compound represented by the formula I, pharmaceutically acceptable salt thereof, or solvate thereof.SELECTED DRAWING: None
Thiadiazoline- And pyrazoline-based carboxamides and carbothioamides: Synthesis and inhibition against nitric oxide synthase
Arias, Fabio,Encarnación Camacho,Dora Carrión,Chayah, Meriem,Romero, Miguel,Duarte, Juan,Gallo, Miguel A.
, (2019/07/12)
Two new families of pyrazoline and thiadiazoline heterocycles have been developed. Their inhibitory activities against two different isoforms of nitric oxide synthase (inducible and neuronal NOS) are reported. The novel derivatives were synthesized combining the arylthiadiazoline or arylpyrazoline skeleton and a carboxamide or carbothioamide moiety, used as starting material ethyl 2-nitrobenzoates or substituted nitrobenzaldehydes, respectively. The structure-activity relationships of final molecules are discussed in terms of the R1 radical effects in the aromatic ring, the Y atom in the heterocyclic system, the X heteroatom in the main chain, and the R2 substituent in the carboxamide or carbothioamide rest. In general, thiadiazolines (5a-e) inhibit preferentially the neuronal isoform; among them, 5a is the best nNOS inhibitor (74.11% at 1 mM, IC50 = 420 M). In contrast, pyrazolines (6a-r) behave better as iNOS than nNOS inhibitors, 6m being the best molecule of this series (76.86% at 1 mM of iNOS inhibition, IC50 = 130 M) and the most potent of all tested compounds.
Concise Total Syntheses of dl-Camptothecin and Related Anticancer Drugs
Shen, Wang,Coburn, Craig A.,Bornmann, William G.,Danishefsky, Samuel J.
, p. 611 - 617 (2007/10/02)
The readily available tricyclic ester 10 has been converted to dl-camptothecin (1) in 39percent yield.It was discovered that, with the C5 carbomethoxy group in place, the C6 benzylic position of 10 (pyridone numbering) is selectively
