Discovery of potent cyclic pseudopeptide human tachykinin NK-2 receptor antagonists.
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Animals↗
Biomedical subjects
D Giannotti
Publications and source records attributed to D Giannotti.
Gender-related differences in body dysmorphic disorder (dysmorphophobia).
Body Dysmorphic Disorder (BDD), which consists of pathological preoccupations with defects in different body parts, has been systematically studied only in the last decade. We hypothesized that gender would differentially influence the localization of the preoccupations as well as the extent and type of comorbidity with other psychiatric disorders. With the use of a specially constructed semistructured interview, we evaluated 58 consecutive outpatients with DSM-III-R BDD (women = 41.4%, men = 58.6%). Women had significantly more preoccupations with breast and legs, checking in the mirror and camouflaging, as well as lifetime comorbidity with panic, generalized anxiety, and bulimia. Men had significantly higher preoccupations with genitals, height, excessive body hair, as well as higher lifetime comorbidity with bipolar disorder. Although BDD is almost never found without comorbidity, it does appear to be an autonomous syndrome, and gender tends to influence the nature and extent of this comorbidity.
Adolescent↗
New arylpyrido-diazepine and -thiodiazepine derivatives are potent and highly selective HIV-1 inhibitors targeted at the reverse transcriptase.
A series of pyridobenzothiodiazepindioxides such as the 11-ethyl-6,8,9-trimethyl-6,11-dihydro-pyrido[2,3-f] [2,1,5]benzothiodiazepine-5,5-dioxide and arylpiridodiazepines such as the 6,7-dihydro-7-methyl-12-ethyl-pyrido[2,3-b] pyrido(2',3'-4,5]furo[2,3-f][1,4]diazepin-6(12H)-thio and the 6,7-dihydro-7-methyl-12-ethyl-pyrido[2,3-b]pyrido- [2,3-4,5]thieno[2,3-f][1,4] diazepin-6(12H)-thione were found to inhibit human immunodeficiency virus type 1 [HIV-1(IIIB)] replication at a concentration of 0.003-0.04 microM without being cytotoxic at a 3,000- to 15,000-fold higher concentration. These compounds proved effective against a variety of HIV-1 strains, including those that are resistant to 3'-azido-3' deoxythymidine (AZT), but not against HIV-2, simian immunodeficiency virus or herpes simplex virus. An HIV-1 strain containing the 188 Tyr-->His mutation in the reverse transcriptase displayed severely reduced sensitivity to the compounds. The specificity of these compounds is due to an interaction with the reverse transcription process. The 6,7-dihydro-7-methyl-12-ethyl-pyrido[2,3-b]pyrido [2,3-4,5]thieno[2,3-f][1,4]diazepin-6(12H)-thione (MEN 10979) enhanced the anti-HIV-1 activity of AZT and dideoxyinosine (ddI) in a synergistic manner. The new arylpyrido-diazepine and -thiodiazepine derivatives appear to be drug candidates for the treatment of HIV-1 infection.
Antiviral Agents↗
Fluvoxamine in the treatment of body dysmorphic disorder (dysmorphophobia).
Fifteen consecutive patients with a DSM-III-R diagnosis of body dysmorphic disorder (BDD) were included in a 10-week open clinical trial of fluvoxamine. Treatment began at 100 mg/day fluvoxamine and was increased to a maximum of 300 mg/day or until intolerable side effects developed or a complete or nearly complete resolution of symptoms occurred. At baseline and at weeks 2, 6 and 10, patients completed the Hopkins Symptoms Check-List (HSCL-90) and a specific rating scale for BDD symptoms (BDDSS), and clinicians completed a Clinical Global Improvement Scale. Twelve of the 15 patients completed the trial. Of the three patients who did not complete the study, one improved moderately during the placebo phase, one showed a marked worsening of the depressive symptoms during the wash-out phase and one showed adverse side effects, such as nausea and diarrhoea, after the first week of treatment and was unable to continue the trial. After 10 weeks, of the 12 remaining patients, 10 were considered to be markedly improved, one minimally improved and one unchanged. Several outcome measures showed a significant improvement from baseline to week 10. Our findings suggest that fluvoxamine may be effective in the treatment of BDD. Double-blind studies will be required to investigate these findings further.
Adolescent↗
Psychotic symptom patterns and the diagnosis of schizophrenia.
In comparing 101 psychotic patients subtyped by DSM-III criteria into paranoia, schizophrenia, schizoaffective, and affective disorders, we failed to distinguish them on the basis of delusional and hallucinatory experiences. These 'productive', 'positive' or 'irritative' symptoms--which the literature tends to link with temporolimbic dysfunction--did not appear specifically linked to schizophrenia. By contrast, 'negative' or 'deficit' symptoms--which the literature tends to relate to frontal lobe dysfunction--appeared more specific--especially for the disorganized subtype of schizophrenia. Although these data tend to support Bleulerian over Schneiderian conceptualization of schizophrenia, the heterogeneity of neuropsychological deficits implied in the negative symptom complexes limits the nosologic utility of the rubric of schizophrenia so defined.
Adolescent↗
New dibenzothiadiazepine derivatives with antidepressant activities.
A new series of 11-[(aminoalkyl)carbonyl] derivatives of 6,11-dihydrodibenzo[c,f][1,2,5]thiadiazepine 5,5-dioxide (10-39) were synthesized and evaluated for potential antidepressant activity in the apomorphine-induced hypothermia (Apo 16) test. Effects on reserpine-induced hypothermia and toxicity for the most potent antagonists of Apo 16 hypothermia were also studied. Structure-activity relationships are reported. Anticholinergic effects were evaluated for compound 12, identified as the most potent and least toxic in this series, by assessing physostigmine lethality. Compound 12 was also subjected to X-ray analysis.
Animals↗
New benzofuran-imidazoles as antimycotic agents. I. Synthesis and characterization.
With the aim of obtaining new drugs having antimycotic activity together with antibacterial and fewer side effects, we synthesized ten new benzofuran-2-yl-imidazoles.
Antifungal Agents↗
New benzofuran-imidazoles as antimycotic agents. II. In vitro studies.
Ten new imidazole derivatives, benzofuran-imidazoles, were studied in vitro to establish their antimycotic activity against 70 fungal strains, in comparison with three known imidazoles and, for the dermatophytes only, griseofulvin. A very high inhibitory activity against dermatophytes was shown by five of the new substances. The other filamentous fungi and yeasts showed a more marked variation in their susceptibility. However a good sensitivity of some isolates of Candida albicans and other yeasts was seen.
Antifungal Agents↗
[Relation between specific weight and water content of meats from immature animals or those treated with thyrostatic drugs].
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Age Factors↗
[Arturo Magliano].
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History of Medicine↗
2,6-Diketopiperazines from amino acids, from solution-phase to solid-phase organic synthesis.
A method to prepare 1,3-disubstituted 2,6-diketopiperazines (2,6-DKP) as useful heterocyclic library scaffolds in the search of new leads for drug discovery is described. The method can be used in solution-phase and solid-phase conditions. In the key step of the synthesis, the imido portion of the new molecule is formed in solution through intramolecular cyclization, under basic conditions, of a secondary amide nitrogen on a benzyl ester. A Wang resin carboxylic ester is used as the acylating agent under solid-phase conditions, allowing the cyclization to take place with simultaneous cleavage of the product from the resin ("cyclocleavage"). The synthetic method worked well with several couples of amino acids, independently from their configuration, and was used for the parallel synthesis of a series of fully characterized compounds. The use of iterative conditions in the solid phase (repeated addition of fresh solvent and potassium carbonate to the resin after filtering out the product-containing solution) allowed us to keep diastereoisomer content below the detection limit by HPLC and (1)H NMR (200 MHz).
Amino Acids↗