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CNS effects of a series of 1,2,4-triazolyl heterocarboxylic derivatives.
A series of 1,2,4-triazolyl heterocarboxylic derivatives were tested for acute toxicity and CNS effects in mice and some of the screened derivatives showed interesting anxiolytic properties. Expand
Novel 1,1,3-trioxo-2H,4H-thieno[3,4-e][1,2,4]thiadiazine derivatives as non-nucleoside reverse transcriptase inhibitors that inhibit human immunodeficiency virus type 1 replication.
Compounds bearing at the N-4 position a cyanomethyl, propargyl, or benzyl substituent were found to be the most potent of the series. Expand
Synthesis and Anti‐inflammatory Evaluation of New Sulfamoylheterocarboxylic Derivatives
A series of new sulfamoylthiophene and sulfamoylpyrazole carboxylic acid derivatives was synthesized. Some of these compounds show interesting analgesic properties and significant nonsteroidalExpand
Synthesis of 3-substituted-4-phenyl-2-thioxo-1,2,3,4,5,6,7,8-octahydrobenzo[4,5]thieno[2,3-á]pyrimidines †
The reactions between 3-benzoyl-2-isothiocyanato-4,5,6,7-tetrahydrobenzo[b]thiophene and hydrazine or primary amines have been studied. The products obtained were identified as derivatives ofExpand
Synthesis and anti-HIV activity of 1,1,3-trioxo-2H,4H-thieno[3,4-e][1,2,4]thiadiazines (TTDs): a new family of HIV-1 specific non-nucleoside reverse transcriptase inhibitors.
Several 4-substituted-2-benzyl-derivatives were found to selectively inhibit human immunodeficiency virus type 1 [HIV-1 (IIIB)] replication in MT-4 and CEM cells and represent a new chemical class of non-nucleoside HIV-1 reverse transcriptase inhibitors (NNRTIs). Expand
Synthesis and Antidepressant Evaluation of New Hetero[2,1]benzothiazepine Derivatives
A series of new hetero[2,1]benzothiazepine derivatives was synthesized that antagonized the ptosis and motor depression induced by tetrabenazine and were also active in the Porsolt forced swimming test. Expand
1,1,3-Trioxo-2H,4H-Thieno[3,4-e][1,2,4]Thiadiazine (TTD) Derivatives: a New Class of Nonnucleoside Human Immunodeficiency Virus Type 1 (HIV-1) Reverse Transcriptase Inhibitors with Anti-HIV-1 Activity
Modelling studies suggest that in contrast to most other NNRTIs, but akin to nevirapine, QM96521 does not act as a hydrogen bond donor in the RT-drug complex, and enhanced the anti-HIV-1 activity of AZT and didanosine in a subsynergistic manner. Expand
NSAI Activity Study of 4‐Phenyl‐2‐thioxo‐benzo[4,5]thieno [2,3‐d]pyrimidine Derivatives
The studied compounds possess a remarkable analgesic activity, devoid of central effects, and show an interesting anti‐inflammatory profile evidenced by their effectiveness in different experimental models of inflammation. Expand
Synthesis of thieno[3,4-c] and thieno[3,2-c][2,1]benzothiazepines
Starting from [4,3-c] and [3,2-c] methyl chlorosulfonylthiophene- carboxylates the synthesis of ketones thieno[2,1]benzothiazepinones (7 and 8) is described. These compounds are the first twoExpand
Thiophene isosteres: synthesis and biological evaluation of 3-substituted derivatives of 4-phenyl-2-thioxo-benzo[4,5] thieno[2,3-d]pyrimidine
Abstract As an extension of a previous work, in which a series of 4-phenyl-2-thioxo-benzo[4,5]thieno[2,3-d]pyrimidines were synthesized, a new series of 3-amino derivatives of this ring system hasExpand