Search of Antimicrobial Activity in a Series of Substituted 4-Aryl-4-oxo-2-tienilaminobut-2-enoic Acids

被引：8

作者：

Shipilovskikh, Sergei A. ^{[1
,2
]}

Makhmudov, R. R. ^{[1
]}

Balandina, S. Yu ^{[1
]}

Rubtsov, Aleksandr E. ^{[1
]}

机构：

[1] Perm State Univ, Dept Chem, Bukireva 15, Perm 614990, Russia

[2] Ural Fed Univ, Inst Chem Technol, Mira 19, Ekaterinburg 620002, Russia

来源：

MODERN SYNTHETIC METHODOLOGIES FOR CREATING DRUGS AND FUNCTIONAL MATERIALS (MOSM2019) | 2020年 / 2280卷

基金：

俄罗斯基础研究基金会;

关键词：

ANALGESIC ACTIVITY; RIBONUCLEASE H; CHEMISTRY; INHIBITORS; ETHYL; PHARMACOPHORE; DECYCLIZATION;

D O I：

10.1063/5.0018494

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

Studied the antimicrobial activity against the test cultures of microorganisms St. aureus ATCC 906 and E. coli ATCC 1257 defined by two-fold serial dilutions in a liquid growth medium in a series of substituted 4-aryl-4-oxo-2-tienilaminobut-2-enoic acid. Found that several of the test substances have pronounced antimicrobial activity, and some are at the level of the reference drug dioxidine. Also analyzed acute toxicity (LD50, mg/ml) in white mice (females) weighing 16-18 g. after a single intraperitoneal injection for all the compounds obtained and found that they are practically non-toxic 5 class of drugs.

引用

页数：5

共 50 条

[1] Synthesis and Analgesic Activity of Substituted 4-(Het)aryl-4-oxo-2-thienylaminobut-2-enoic Acids
S. A. Shipilovskikh
R. R. Makhmudov
D. Yu. Lupach
P. T. Pavlov
E. V. Babushkina
A. E. Rubtsov
Pharmaceutical Chemistry Journal, 2013, 47 : 366 - 370
[2] SYNTHESIS AND ANALGESIC ACTIVITY OF SUBSTITUTED 4-(HET)ARYL-4-OXO-2-THIENYLAMINOBUT-2-ENOIC ACIDS
Shipilovskikh, S. A.
Makhmudov, R. R.
Lupach, D. Yu.
Pavlov, P. T.
Babushkina, E. V.
Rubtsov, A. E.
PHARMACEUTICAL CHEMISTRY JOURNAL, 2013, 47 (07) : 366 - 370
[3] Synthesis and Intramolecular Cyclization of Substituted 4-(Het)aryl-4-oxo-2-thienylaminobut-2-enoic Acids Containing Nitrile Group in the Thiophene Ring
Gorbunova, I. A.
Shipilovskikh, D. A.
Rubtsov, A. E.
Shipilovskikh, S. A.
RUSSIAN JOURNAL OF GENERAL CHEMISTRY, 2021, 91 (09) : 1623 - 1628
[4] Synthesis, Intramolecular Cyclization, and Antinociceptive Activity of Substituted 2-[2-(4-Nitrobenzoyl)hydrazinylidene]-4-oxobut-2-enoic Acids
Denisova, E., I
Lipin, D., V
Parkhoma, K. Yu
Devyatkin, I. O.
Shipilovskikh, D. A.
Chashchina, S., V
Makhmudov, R. R.
Igidov, N. M.
Shipilovskikh, S. A.
RUSSIAN JOURNAL OF ORGANIC CHEMISTRY, 2021, 57 (12) : 1955 - 1960
[5] Synthesis, antimicrobial and analgesic activity of N-substituted 2-amino-4-aryl-4-oxo-2-butaneoic acids
Koz'minykh E.N.
Belyaev A.O.
Koz'minykh V.O.
Makhmudov R.R.
Odegova T.F.
Pharmaceutical Chemistry Journal, 2002, 36 (11) : 604 - 607
[6] Synthesis and Antibacterial Activity of 4-Oxo-2-thienylaminobut-2-enoic Acids
Gorbunova, I. A.
Shadrin, V. M.
Pulina, N. A.
Novikova, V. V.
Dubrovina, S. S.
Shipilovskikh, D. A.
Shipilovskikh, S. A.
RUSSIAN JOURNAL OF GENERAL CHEMISTRY, 2023, 93 (01) : 8 - 15
[7] Synthesis and Antinociceptive Activity ofN-Substituted 4-Aryl-4-oxo-2-[(3-thiophen-2-yl)amino]but-2-enamides
Shipilovskikh, S. A.
Vaganov, V. Y.
Makhmudov, R. R.
Rubtsov, A. E.
RUSSIAN JOURNAL OF GENERAL CHEMISTRY, 2020, 90 (04) : 583 - 589
[8] Synthesis, antimicrobial, and analgesic activity of 4-aryl-2-tert- butylamino-4-oxo-2-butenoic acids
Koz'minykh V.O.
Belyaev A.O.
Koz'minykh E.N.
Odegova T.F.
Makhmudov R.R.
Pharmaceutical Chemistry Journal, 2004, 38 (11) : 602 - 604
[9] Synthesis, antimicrobial, and analgesic activity of 4-aryl-2-N-morpholino- 4-oxo-2-butenoic acids
Koz'minykh V.O.
Belyaev A.O.
Koz'minykh E.N.
Makhmudov R.R.
Odegova T.F.
Pharmaceutical Chemistry Journal, 2004, 38 (8) : 431 - 433
[10] Substituted amides and hydrazides of acylpyruvic acids. Part 10. Synthesis, antimicrobial and analgesic activity of 4-aryl-2-arylamino-4-oxo-2-butenoic acid arylamides
Belyaev A.O.
Koz'minykh E.N.
Makhmudov R.R.
Koz'minykh V.O.
Odegova T.F.
Pharmaceutical Chemistry Journal, 2004, 38 (7) : 364 - 367

← 1 2 3 4 5 →