- Alkylamino derivatives of pyrazinamide: Synthesis and antimycobacterial evaluation
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A series of pyrazinamide derivatives with alkylamino substitution was designed, synthesized and tested for their ability to inhibit the growth of selected mycobacterial, bacterial and fungal strains. The target structures were prepared from the corresponding 5-chloro (1) or 6-chloropyrazine-2-carboxamide (2) by nucleophilic substitution of chlorine by various non-aromatic amines (alkylamines). To determine the influence of alkyl substitution, corresponding amino derivatives (1a, 2a) and compounds with phenylalkylamino substitution were prepared. Some of the compounds exerted antimycobacterial activity against Mycobacterium tuberculosis H37Rv significantly better than standard pyrazinamide and corresponding starting compounds (1 and 2). Basic structure-activity relationships are presented. Only weak antibacterial and no antifungal activity was detected.
- Servusova, Barbora,Paterova, Pavla,Mandikova, Jana,Kubicek, Vladimir,Kucera, Radim,Kunes, Jiri,Dolezal, Martin,Zitko, Jan
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p. 450 - 453
(2014/01/23)
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- CARBAMOYL COMPOUNDS AS DGAT1 INHIBITORS 190
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DGAT-1 inhibitor compounds of formula (I), pharmaceutically-acceptable salts and pro- drugs thereof are described, together with pharmaceutical compositions, processes for making them and their use in treating, for example, obesity wherein, for example, Ring A is optionally substituted 2,6-pyrazindiyl; X is =O; Ring B is optionally substituted 1,4-phenylene; Y1 is a direct bond or -O-; Y2 is -(CH 2) r- wherein r is 2 or 3; n is 0 or n is 1 when Y1 is a direct bond between Ring B and Ring C and when Ring B is 1,4-phenylene and Ring C is (4-6C)cycloalkane; Ring C is optionally substituted (4-6C)cycloalkane, (7-10C)bicycloalkane, (8-12C)tricycloalkane, phenylene or pryidindiyl; L is a direct bond or -O-; p is 0, 1 or 2 and when p is 1 or 2 RA1 and RA2 are each independently hydrogen or (1-4C)alkyl; Z is carboxy or a mimic or bioisostere thereof.
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Page/Page column 77
(2009/07/25)
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- PYRROLIDONES WITH ANTI-HIV ACTIVITY
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The present invention relates to inhibition of viruses, e.g., HIV using pyrrolidones and compounds related to pyrrolidones. The invention further relates to methods for identifying and using agents, including small molecule chemical compositions that inhi
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- SYNTHESIS AND 1H AND 13C NMR SPECTRA OF SULFUR DERIVATIVES OF PYRAZINE DERIVED FROM AMIDATION PRODUCT OF 2-CHLOROPYRAZINE AND 6-CHLORO-2-PYRAZINECARBONITRILE. TUBERCULOSTATIC ACTIVITY
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Homolytic amidations of 2-chloropyrazine and 6-chloropyrazine-2-carbonitrile have been carried out to obtain products which have been used to prepare sulfur derivatives of pyrazine as potential tuberculostatic agents.The 1H and 13C NMR spectra of the products have been measured and interpreted, and the antituberculotic activity has been evaluated.
- Dlabal, Karel,Palat, Karel,Lycka, Antonin,Odlerova, Zelmira
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p. 2493 - 2501
(2007/10/02)
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