54344-92-2Relevant articles and documents
Design, synthesis, biological activities and DFT calculation of novel 1,2,4-triazole Schiff base derivatives
Jin, Ru-Yi,Zeng, Chu-Yue,Liang, Xu-Hua,Sun, Xiao-Hong,Liu, Yuan-Fa,Wang, Yan-Yan,Zhou, Sha
, p. 253 - 260 (2018/07/06)
Series of 1,2,4-triazole Schiff bases (2a-2d, 2f-2h and 3a-3h) have been designed and synthesized. The structure of title compounds was confirmed on the basis of their spectral data and elemental analysis. All the target compounds were screened for their in vitro antifungal activity and antibacterial activity. Two of the tested compounds (2a and 2b) exhibited significant antifungal activity against most fungi, especially compound 2a showed better antifungal activity than triadimefon. Meanwhile, the antibacterial activity assay also indicated compound 2a exhibited excellent antibacterial activities comparable to chloramphenicol. The SAR manifested no substitution at position 5 of the triazole ring caused an increase in activity, and 3-phenoxy phenyl group introduced in 1,2,4-triazole scaffold can enhance the antibacterial activity. The DFT calculation indicated triazole ring, S atom and benzene ring in both of the 2a and 3a make a major contribution to the activity.
One-pot synthesis of pyrimidinothiazolidinones and their anti-inflammatory and antimicrobial studies
Lingappa,Sujith,Adhikari, Adithya,Rai, N. Satheesha,Vijaynarayana,Kalluraya, Balakrishna
scheme or table, p. 501 - 508 (2010/06/12)
In the present investigation, we report a one-pot synthesis of the title compounds, 2-arylidene-5-(2,3,6-trimethyl-4-methoxyphenyl)-7-substituted-5H- pyrimidino-[2,3-b]thiazolidine-3-ones 6a-j and 2-(5-nitro-2-thienylidine)-5-(2, 3,6-trimethyl-4-methoxyphenyl)-7-substituted-5H- pyrimidino-[2,3-b]thiazolidine- 3-ones 7a-e. Thus, 6a-j and 7a-e were prepared in good yields by refluxing 4-(2,3,6-trimethyl-4-methoxyphenyl)-6-methyl/aryl-3,4-dihydropyrimidin-2-(1H) -thiones 5, monochloro acetic acid, and anhydrous sodium acetate with the appropriate aromatic aldehyde/5-nitro-2-thiophenediacetate in acetic acid/acetic anhydride medium. The structures of these new compounds were established on the basis of their analytical and spectral data. Some of the newly synthesized compounds were screened for their anti-inflammatory and antimicrobial activity. They show moderate anti-inflammatory activity, and some of them were found to be promising antibacterial and antifungal agents. Supplemental materials are available for this article. Go to the publisher's online edition of Phosphorus, Sulfur, and Silicon and the Related Elements to view the free supplemental file.
Evaluation of retinoid lactones as topical therapeutic agents in dermatology
Lewin,Black,Bos,Goehring,Nair,Whiting,Bouquin,Tetrault,Carroll
, p. 983 - 992 (2007/10/03)
Purpose. Optimization of the therapeutic ratio of analogs of the topically active 11-cis,13-cis-12-hydroxymethylretinoic acid, δ-lactone (I) relative to antihyperproliferation and antihyperkeratinization vs. toxicity. Methods. Nine analogs of 1, in which variations were made in the lipophilic cyclohexenyl moiety or in the lactone ring, were evaluated for topical activity against hyperkeratinization, inhibition of TPA-induced DNA synthesis and for skin irritation. Results. Although more potent lactones than the parent lactone 1 were identified, none possessed the favorable therapeutic ratio associated with 1. Conclusions. The δ-lactone 1 possesses unique molecular features responsible for its desirable therapeutic ratio as an anti-hyperproliferative and antihyperkeratotic agent. In view of its very low systemic retinoid toxicity and the absence of any systemic toxicity, this lactone may be a good candidate for use in the topical treatment of acne.
