Synthesis, lipophilicity and biological evaluation of indole-containing derivatives of 1,3,4-thiadiazole and 1,2,4-triazole

dc.contributor.author	Σιάτρα - Παπασταϊκούδη, Θεοδώρα	el
dc.contributor.author	Τσοτίνης, Ανδρέας	el
dc.contributor.author	Βαρβαρέσου, Αθανασία	el
dc.contributor.author	Τσαντίλη - Κακουλίδου, Άννα	el
dc.contributor.author	Βαμβακίδη, Αλεξάνδρα	el
dc.date.accessioned	2015-04-30T13:01:10Z
dc.date.available	2015-04-30T13:01:10Z
dc.date.issued	2015-04-30
dc.identifier.uri	http://hdl.handle.net/11400/9319
dc.rights	Αναφορά Δημιουργού-Μη Εμπορική Χρήση-Όχι Παράγωγα Έργα 3.0 Ηνωμένες Πολιτείες	*
dc.rights.uri	http://creativecommons.org/licenses/by-nc-nd/3.0/us/	*
dc.source	http://www.sciencedirect.com	en
dc.source	http://www.sciencedirect.com/science/article/pii/S0014827X9800024X	en
dc.subject	Καλλυντικά
dc.subject	Χημικά παρασκευάσματα
dc.subject	Λιποφιλικότητα
dc.subject	Αντικαταθλιπτική δράση
dc.subject	Cosmetics
dc.subject	Chemical preparations
dc.subject	Antidepressant activity
dc.title	Synthesis, lipophilicity and biological evaluation of indole-containing derivatives of 1,3,4-thiadiazole and 1,2,4-triazole	en
heal.type	journalArticle
heal.classification	Aesthetics
heal.classification	Chemistry
heal.classification	Αισθητική
heal.classification	Χημεία
heal.classificationURI	http://id.loc.gov/authorities/subjects/sh85001441
heal.classificationURI	http://id.loc.gov/authorities/subjects/sh85022986
heal.classificationURI	N/A-Αισθητική
heal.classificationURI	N/A-Χημεία
heal.identifier.secondary	10.1016/S0014-827X(98)00024-X
heal.language	en
heal.access	campus
heal.recordProvider	Τεχνολογικό Εκπαιδευτικό Ίδρυμα Αθηνών. Σχολή Επαγγελμάτων Υγείας και Πρόνοιας. Τμήμα Αισθητικής και Κοσμητολογίας	el
heal.publicationDate	1999-03-05
heal.bibliographicCitation	Varvaresou, A., Siatra-Papastaikoudi, T., Tsotinis, A., Tsantili-Kakoulidou, A., and Vamvakides, A. (1999) Synthesis, lipophilicity and biological evaluation of indole-containing derivatives of 1,3,4-thiadiazole and 1,2,4-triazole. "Farmaco" 53 (5), p.320-326	en
heal.abstract	3-[(2-Methyl-1H-3-indolyl)methyl]-4-aryl-4,5-dihydro-1H-1,2,4-triazole-5-thiones 6a-c and their respective N-{5-[(2-methyl-1H-3-indolyl) methyl]-1,3,4-thiadiazol-2-yl}-N-arylamines 7a,b have been prepared. The antidepressant profile of 6a,c and 7a was studied on mice with respect to that of the analogous 3-(1H-1-indolylmethyl)-4-aryl-4,5-dihydro-1H-1,2,4-triazole-5-thiones 1a-c and the respective N-15{(2-methyl-1H-3-indolyl)methyl]-1,3,4-thiadiazol-2-yl}-N-arylamines 2a-c, the synthesis and antimicrobial potency of which we have recently reported. Behavioral effects, induced by the members of both series, in conjunction with their activity in some specific tests (forced swim, pentetrazole convulsions) on mice, show that these derivatives cross the blood-brain barrier and could develop an antidepressant activity comparable to that of imipramine. Blood-brain barrier penetration is also supported by the lipophilicity data obtained for all analogs.	en
heal.publisher	Elsevier	en
heal.journalName	Farmaco	en
heal.journalType	peer-reviewed
heal.fullTextAvailability	false