937-39-3Relevant articles and documents
Design, synthesis, and in vitro antimicrobial activity of hydrazide–hydrazones of 2-substituted acetic acid
Popio?ek, ?ukasz,Biernasiuk, Anna
, p. 873 - 883 (2016)
In this study, 30 hydrazide–hydrazones of phenylacetic (3–10) and hydroxyacetic acid (11–32) were synthesized by the condensation reaction of appropriate 2-substituted acetic acid hydrazide with different aromatic aldehydes. The obtained compounds were characterized by spectral data and evaluated in vitro for their potential antimicrobial activities against a panel of reference strains of micro-organisms, including Gram-positive bacteria, Gram-negative bacteria, and fungi belonging to the Candida spp. The results from our antimicrobial assays indicated that among synthesized compounds 3–32, especially compounds 6, 14, and 26 showed high bactericidal activity (MIC?=?0.488–7.81?μg/ml) against reference Gram-positive bacteria, and in some cases, their activity was even better than that of commonly used antibiotics, such as cefuroxime or ampicillin.
Design, modification of phyllanthone derivatives as anti-diabetic and cytotoxic agents
Nguyen, Ngoc-Hong,Vo, Van-Giau,Phan, Hoang-Vinh-Truong,Ngo, Thanh-The,Sichaem, Jirapast,Nguyen, Thi-Phuong,Nguyen, Huu-Hung,Pham, Duc-Dung,Nguyen, Tien-Cong,Nguyen, Van-Kieu,Duong, Thuc-Huy
, p. 371 - 378 (2020/07/13)
Twelve benzylidene derivatives, one Baeyer-Villiger oxidative, six imine derivatives were successfully designed and synthesised from phyllanthone. In the search for potential new anti-diabetic agents, phyllanthone along with its benzylidene and oxidation analogues were evaluated for enzyme inhibition against α-glucosidase. In the benzylidene series, most analogues displayed stronger activity than the mother compound. Compound 1c revealed the strongest activity, outperforming the acarbose positive control with an IC50 value of 19.59 μM. Phyllanthone and its derivatives were then tested for cytotoxic activity against the K562 cell line. The imine analogues displayed the most powerful cytotoxic activity with 3cand 3d having IC50 values of 57.55 and 68.02 μM, respectively.
SUBSTITUTED AMINO TRIAZOLOPYRIMIDINE AND AMINO TRIAZOLOPYRAZINE ADENOSINE RECEPTOR ANTAGONISTS, PHARMACEUTICAL COMPOSITIONS AND THEIR USE
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Page/Page column 58; 66, (2020/06/10)
In its many embodiments, the present invention provides certain substituted amino triazolopyrimidine and amino triazolopyrazine compounds of Formula (IA) and Formula (IB): and, and pharmaceutically acceptable salts thereof, wherein, R1, n, R2, and R3 are as defined herein, pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other therapeutically active agents), and methods for their preparation and use, alone and in combination with other therapeutic agents, as antagonists of A2a and/or A2b receptors, and their use in the treatment of a variety of diseases, conditions, or disorders that are mediated, at least in part, by the adenosine A2a receptor and/or the adenosine A2b receptor.