19250-02-3Relevant articles and documents
Creating an antibacterial with in vivo efficacy: Synthesis and characterization of potent inhibitors of the bacterial cell division protein FTSZ with improved pharmaceutical properties
Haydon, David J.,Bennett, James M.,Brown, David,Collins, Ian,Galbraith, Greta,Lancett, Paul,MacDonald, Rebecca,Stokes, Neil R.,Chauhan, Pramod K.,Sutariya, Jignesh K.,Nayal, Narendra,Srivastava, Anil,Beanland, Joy,Hall, Robin,Henstock, Vincent,Noula, Caterina,Rockley, Chris,Czaplewski, Lloyd
supporting information; experimental part, p. 3927 - 3936 (2010/09/04)
3-Methoxybenzamide (1) is a weak inhibitor of the essential bacterial cell division protein FtsZ. Alkyl derivatives of 1 are potent antistaphylococcal compounds with suboptimal drug-like properties. Exploration of the structure-activity relationships of analogues of these inhibitors led to the identification of potent antistaphylococcal compounds with improved pharmaceutical properties.
Biphenyl-substituted guanidine derivatives useful as hypoglycaemic agents
-
, (2008/06/13)
Compounds of formula I STR1 and their salts in which R1 is optionally substituted phenyl, R2 is alkyl, cycloalkyl or optionally substituted amino, or R2 and R3 together with the nitrogen and carbon atoms to which they are attached form an optionally substituted heterocyclic ring or R3 and R4 together with the nitrogen atom to which they are attached form an optionally substituted heterocyclic ring and R5 is H, halo, alkyl, alkoxy, trifluoromethyl or a group of formula S(O)m R8 in which m is 0, 1 or 2 and R8 is alkyl have utility in the treatment of diabetes particularly in the treatment of hyperglycaemia.
Substituted 2-benzothiazolamines as sodium flux inhibitors: Quantitative structure-activity relationships and anticonvulsant activity
Hays,Rice,Ortwine,Johnson,Schwarz,Boyd,Copeland,Vartanian,Boxer
, p. 1425 - 1432 (2007/10/02)
Thirty-two aryl-substituted 2-benzothiazolamines have been tested for their ability to modulate sodium flux in rat cortical slices. A QSAR analysis, applied to these derivatives, showed a trend toward increasing potency as sodium flux inhibitors with increasing lipophilicity, decreasing size, and increasing electron withdrawal of the benzo ring substitutents. Additionally, 4- or 5-substitution of the benzo ring was found to decrease potency. The combination of increased lipophilicity, small size, and electron withdrawal severely limited which groups were tolerated on the benzo ring, thus suggesting that the optimal substitution patterns have been prepared within this series. Nine of these compounds were potent inhibitors of veratridine-induced sodium flux (NaFl). These nine compounds also proved to be anticonvulsant in the maximal electroshock (MES) assay. Fourteen additional 2-benzothiazolamines demonstrated activity in the MES screen, yet exhibited no activity in the NaFl assay. These derivatives may be interacting at the sodium channel in a manner not discernible by the flux paradigm, or they may be acting by an alternative mechanism in vivo.
New 2-aryliminoimidazolidines. II. Synthesis and antihypertensive activity of 2-(biphenylimino)-imidazolidines
Taniguchi,Katsura,Ueda,Matsuo
, p. 240 - 244 (2007/10/02)
For improvement of the duration of action of FR35447 (I), 2-(biphenylimino)imidazolidines (III) were synthesized and their hypotensive activity was tested against conscious normotensive rats. 2-(4'-Fluoro-[1,1'-biphenyl]-2ylimino)imidazolidine (III l) exh
Thermal Decomposition of Aromatic Thioureas
Parkanyi, Cyril,Al-Salamah, Mohammed A.
, p. 101 - 104 (2007/10/02)
Thermal decomposition of aromatic and heteroaromatic thioureas in boiling chlorobenzene is a first-order reaction.The reaction involves intramolecular hydrogen transfer followed by a cleavage of the C - N bond which is the rate-limiting step.The rate constants of decomposition have been determined and correlated with quantum-chemical reactivity indices. - Key words: Thioureas, Isothiocyanates, Thermal Decomposition, Side-Chain Elimination, Kinetics
Synthesis & Pharmacological Evaluation of Ethyl 3-Substituted-phenyl-2-methylmercapto/ phenyl/ methyl-4(3H)-pyrimidone-5-carboxylates
Gupta, K. A.,Saxena, Anil K.,Jain, Padam C.
, p. 228 - 233 (2007/10/02)
A number of ethyl 3-substituted-phenyl-2-methylmercapto/ phenyl/ methyl-4(3H)-pyrimidone-5-carboxylates (V) have been prepared by the reaction of amidines (III) with diethyl ethoxymethylenemalonate.In order to confirm the structure (V), ethyl 3-(2'-methylphenyl)-2-methylmercapto-4(3H)pyrimidone-5-carboxylate (103) has been transformed into the earlier synthesised 3-(2'-methylphenyl)-2-methylmercapto-4(3H)-pyrimidone (115) by decarboxylation of 3-(2'-methylphenyl)-2-methylmercapto-4(3H)-pyrimidone-5-carboxylic acid (114), obtained by the alkaline hydrolysis of 103.Someof these compounds have shown antiinflammatory, diuretic and antipassive cutaneous anaphylaxis activities.