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Journal №5 for 2014 г.
Article in number:
Synthesis, properties and biological activity isopropylamides 2-arylaminoquinoline-4-carboxylic acid
Keywords:
isopropylamide 2-chloroquinoline-4-carboxylic acid
isopropylamides 2-arylaminoquinoline-4-carboxylic acid
antiinflammatory
analgesic
antimicrobial activity
Authors:
A.N. Dubrovin - Post-graduate Student, Department Biological Chemistry, Perm State Pharmaceutical Academy (PGFA), Russia. E-mail: andovin@yandex.ru
A.I. Mikhalev - Dr. Sc. (Pharm.), Professor, Biological Chemistry, Russia, Perm State Pharmaceutical Academy (PGFA), Russia. E-mail: biolhim@pfa.ru
S.V. Ukhov - Ph.D. (Pharm.), Pharmaceutical Chemistry, Perm State Pharmaceutical Academy (PGFA), Russia
T.M. Konshina - Ph.D. (Med.), Department Pharmacology, Perm State Pharmaceutical Academy (PGFA), Russia
A.G. Goldstein - Ph.D. (Pharm.), Department Pharmacology, Perm State Pharmaceutical Academy (PGFA), Russia
V.V. Novikova - Ph.D. (Pharm.), Department Microbiology, Perm State Pharmaceutical Academy (PGFA), Russia
R.R. Makhmudov - Ph.D. (Pharm.), Institute of Natural Sciences, Perm State National Research University, Russia
A.I. Mikhalev - Dr. Sc. (Pharm.), Professor, Biological Chemistry, Russia, Perm State Pharmaceutical Academy (PGFA), Russia. E-mail: biolhim@pfa.ru
S.V. Ukhov - Ph.D. (Pharm.), Pharmaceutical Chemistry, Perm State Pharmaceutical Academy (PGFA), Russia
T.M. Konshina - Ph.D. (Med.), Department Pharmacology, Perm State Pharmaceutical Academy (PGFA), Russia
A.G. Goldstein - Ph.D. (Pharm.), Department Pharmacology, Perm State Pharmaceutical Academy (PGFA), Russia
V.V. Novikova - Ph.D. (Pharm.), Department Microbiology, Perm State Pharmaceutical Academy (PGFA), Russia
R.R. Makhmudov - Ph.D. (Pharm.), Institute of Natural Sciences, Perm State National Research University, Russia
Abstract:
The synthesis of 11 previously unknown isopropylamides 2-arylaminoquinoline-4-carboxylic acid by reaction 2-chloroquinoline-4-carboxylic acid with the arylamines in DMFA is reported. The purity of synthesized compounds has been confirmed on the basic TLC data. The structures of synthesized compounds have been confirmed on the basic IR and NMR 1H spectral data. Synthesized compounds were screened for the antiinflammatory, analgesic and antimicrobial activity. Isopropylamides 2-arylaminoquinoline-4-carboxylic acid have been screened on animals for their acute toxicity, antiinflammatory, analgesic and antimicrobial activity as compared to the reference substances: diclofenac sodium, acetylsalicylic acid, metamizol sodium, dioxydinum. Synthesis technique isopropylamides 2-arylaminoquinoline-4-carboxylic acid can be used in preparative organic chemistry for synthesis of potentially biologically active compounds in the series of quinoline.
Pages: 14-18
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