- Synthesis and biological evaluation of 1,4-benzodiazepin-2-ones with antitrypanosomal activity
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A library of 1,4-benzodiazepines has been synthesized and evaluated against Trypanosoma brucei, a causative parasite of Human African trypanosomiasis. Benzodiazepines possessing a P2- transporter motif were found to have MIC values as low as 0.78 μM.
- Spencer, John,Rathnam, Rajendra P.,Harvey, Alan L.,Clements, Carol J.,Clark, Rachel L.,Barrett, Michael P.,Wong, Pui Ee,Male, Louise,Coles, Simon J.,MacKay, Simon P.
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experimental part
p. 1802 - 1815
(2011/04/17)
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- Method for inhibiting the proliferation of tumor cells
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A method of inhibiting the proliferation of tumor cells is disclosed which comprises the treatment of such tumor cells with a benzodiazepine having a selective affinity to bind peripheral binding sites on the tumor cell in order to induce non-proliferation of said tumor cells.
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- Synthesis and Resolution of 3-Amino-1,3-dihydro-5-phenyl-2H-1,4-benzodiazepin-2-ones
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Two efficient synthetic routes to the 3-amino-1,4-benzodiazepin-2-ones 2 and 3 were developed.The first sequence was carried out in 55-60percent overall yield and involves a novel mercuric ion assisted ammonia displacement of the (alkylthio)glycinamide 14 to produce the key intermediate α-aminoglycinamide 15.The second approach features a practical two-step amination of the parent 1,4-benzodiazepine ring system 24 to afford the title compound 3 in 49percent overall yield from 2-aminobenzophenone.The 3-amino-1,4-benzodiazepine 3 was resolved via the separation of the corresponding diastereomeric phenylalanyl amides.The desired (-)-3 enantiomer was then liberated by use of the Edman degradation.
- Bock, Mark G.,DiPardo, Robert M.,Evans, Ben E.,Rittle, Kenneth E.,Veber, Daniel F.,et al.
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p. 3232 - 3239
(2007/10/02)
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- Benzophenone glycinamide derivatives
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This invention is directed toward pharmacologically active compounds of the formula STR1 wherein A represents a nitrogen atom which may be substituted by a methyl, cyclopropylmethyl, di(C1-4 alkyl)aminoethyl, methoxymethyl or hydroxyethyl group and B represents a carbonyl group or A and B together represent a grouping of the formula STR2 in which Ra represents a hydrogen atom or a lower alkyl or hydroxymethyl group and X represents a nitrogen atom or C--Rb wherein Rb represents a hydrogen atom or a lower alkyl or hydroxymethyl group; R represents a halogen atom or a nitro or trifluoromethyl group; R1 represents a hydrogen atom or a lower alkyl group; R2 represents an acyl group derived from a naturally occurring amino acid (all such groups which contain an asymmetric carbon atom having the L- or D,L-configuration) and R3 represents a phenyl, halophenyl or 2-pyridyl group And acid addition salts thereof. Also provided are methods for their preparation and intermediates thereof. These compounds exhibit activity as anticonvulsants, muscle relaxants and sedatives.
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