ChemInform Abstract: NEUROTROPIC AND PSYCHOTROPIC AGENTS. CXLIX. SYNTHESIS OF ARYLTHIOACETAMIDOXIMES AS POTENTIAL ANTIDEPRESSANTS

Cervena, I.; Hrubantová, M.; Bartosova, M.; Protiva, M.

doi:10.1002/chin.198136186

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“…A series of arylthioacetamidoxime hydrochlorides 300 were tested in mice as potential antidepressants. Thus, those bearing a chloro, alkyloxy, alkylthio or 3,4-benzo substituent exhibited relatively low antireserpine activity in ptosis, while (3-methoxy-phenyl) and 2-(1-naphthyl)thio acetamidoximes were active in the test of reserpine hypothermia [279,280]. Heteroaryl acetamidoximes bearing an indolyl, isoindolyl or benzimidazolyl group, as well as heteroaryloxyacet-or propionamidoximes bearing a quinolyl, isoquinolyl, indolyl, carbazolyl or indanyl moiety and their naphthyl analogues acted as antidepressants [281,282].…”

Section: Iv11 Anxiolytics-antidepressantsmentioning

confidence: 94%

“…Thus, 4-chlorophenyl-thio-acetamidoxime decreased the blood pressure [279,280]. Furthermore, [2-(2-phenylthio)phenyl]acetamidoxime 291 (Scheme 47), acted as hypotensive [267].…”

Section: Iv12 Antihypertensive Activitymentioning

confidence: 98%

“…The Nmethylated amidoxime derivative 257 was allowed to react with an excess of acetic acid anhydride at 70°C forming the O-acetyl Nmethylamidoxime 277 in 35% yield. All further O-acylations of the hydroxyimino group were carried out with three equivalents of the corresponding alkyl or alkenyl chloroformates in dry pyridine at low temperature to give the O-acylated N-methylamidoxime derivatives (278)(279)(280)(281) [252] (Scheme 43).…”

Section: Iv5 Anthelminthicidesmentioning

confidence: 99%

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Recent Developments in the Chemistry and in the Biological Applications of Amidoximes

Fylaktakidou¹,

Hadjipavlou‐Litina

Litinas³

et al. 2008

CPD

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Amidoximes are compounds bearing both a hydroxyimino and an amino group at the same carbon atom which makes them versatile building blocks for the synthesis of various heterocycles. Their importance in chemistry along with their rich biology, make amidoximes an attractive target for medicinal chemists, biochemists and biologists. Amidoximes and simple O-substituted derivatives possess very important biological activities functioning as antituberculotic, antibacterial, bacteriostatic, insecticidal, elminthicidal, antiviral, herbicidal, fungicidal, antineoplastic, antiarrythmic, antihypertensive, antihistaminic, anxiolytic-antidepressant, anti-inflammatory/antioxidant, antiaggregatory (NO donors) or plant growth regulatory agents. A number of amidoximes has already been used as drugs, or currently being in clinical trials. Their numerous pharmaceutical applications have been recently enriched, due to the fact that some mechanistic pathways, concerning their conversion to amidines, as well as their ability to release NO were clarified, giving a new insight to their mode of action and allowing the design of new therapeutic agents. The main subject of the present review paper is to highlight aspects concerning chemical and biological questions on this interesting class of compounds. Some new synthetic methodologies as well as improvements of previously reported general reactions involving amidoximes, acylated amidoximes, and amidines are presented. The biological applications of amidoximes over the end of 2006 are also extensively reviewed.

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Section: Iv11 Anxiolytics-antidepressantsmentioning

confidence: 94%

“…Thus, 4-chlorophenyl-thio-acetamidoxime decreased the blood pressure [279,280]. Furthermore, [2-(2-phenylthio)phenyl]acetamidoxime 291 (Scheme 47), acted as hypotensive [267].…”

Section: Iv12 Antihypertensive Activitymentioning

confidence: 98%

Section: Iv5 Anthelminthicidesmentioning

confidence: 99%

See 1 more Smart Citation

Recent Developments in the Chemistry and in the Biological Applications of Amidoximes

Fylaktakidou¹,

Hadjipavlou‐Litina

Litinas³

et al. 2008

CPD

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ChemInform Abstract: NEUROTROPIC AND PSYCHOTROPIC AGENTS. CXLIX. SYNTHESIS OF ARYLTHIOACETAMIDOXIMES AS POTENTIAL ANTIDEPRESSANTS

Abstract: Die Thiophenole (I) reagieren mit dem Nitril (II) zu den Arylthjoacetonitrilen (III), die in die Titelverbindungen (IV) bzw. deren Hydro‐ Chloride übergeführt werden.

Cited by 1 publication

References 1 publication

Recent Developments in the Chemistry and in the Biological Applications of Amidoximes

Recent Developments in the Chemistry and in the Biological Applications of Amidoximes

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