摘要:

AbstractA series of steroidal 1,4‐diketone derivatives was synthesized by acid‐catalyzed condensation of 2‐acetylestradiol‐17β‐acetate with substituted phenylglyoxals. Conversion of the products into the corresponding pyridazine derivatives was achieved by reaction with hydrazine hydrate. The synthesized compounds were evaluated for their uterotrophic, antiuterotrophic, and antifertility activities in mature female albino rats. Among the compounds tested, the phenyl2,p‐bromophenyl3, andp‐methoxyphenyl5diketone derivatives displayed uterotrophic activity of 72%, 72%, and 91%, respectively. The gradation of antiestrogenic activity was assessedin vivoby the inhibition of the estrone‐stimulated uterine growth. Compounds2–5showed moderate antiestrogenic activity of 53–56%. None of the tested compounds elicited antifertility activity as assessed by the post‐coital antiimpl

ISSN:0365-6233    

DOI:10.1002/ardp.19963291002

出版商:WILEY‐VCH Verlag    

年代:1996

数据来源: WILEY

摘要:

AbstractA series of 4‐alkylthiopyridine‐2‐carbothioamides have been prepared and evaluatedin vitrofor antimicrobial activity. Chemical structures have been demonstrated by IR and1H NMR data and by elemental analysis. The antimycobacterial activity of these compounds againstMycobacterium tuberculosis, Mycobacterium kansasii, Mycobacterium avium, andMycobacterium fortuitum, and the antifungal activity againstCandida albicans, Candida tropicalis, Candida krusei, Candida glabrata, Trichosporon beigelii, Trichophyton mentagrophytes, Aspergillus fumigatus, andAbsidia corymbiferawere determined by the MIC values. Compounds3exhibit good antimycobacterial activity compared to isoniazide. A moderate antifungal activity was observed againstT. mentagrophytes.Activity is influenced by hydrophobicity of the alkyl

ISSN:0365-6233    

DOI:10.1002/ardp.19963291003

出版商:WILEY‐VCH Verlag    

年代:1996

数据来源: WILEY

摘要:

AbstractThe synthesis of new series of 1‐β‐methylcarbapenems having a 1,3‐diazabicyclo[3.3.0]octan‐4‐one moiety is described. Theirin vitroantibacterial activities against both Gram‐positive and Gram negative bacteria are reported and the effect of the substituent on the bicyclic ring was investigated and was in agreement with findings from our prev

ISSN:0365-6233    

DOI:10.1002/ardp.19963291004

出版商:WILEY‐VCH Verlag    

年代:1996

数据来源: WILEY

摘要:

AbstractThe ether extract of the aerial parts ofLeptospermum scopariumcultivars yielded a lactone with a 20,29,30‐ trinorlupane skeleton (1). Furthermore, 2α‐hydroxyursolic acid (2), platanic acid (3) and 3β,30‐dihydroxy‐lup‐20(29)‐en‐28‐oic acid

ISSN:0365-6233    

DOI:10.1002/ardp.19963291005

出版商:WILEY‐VCH Verlag    

年代:1996

数据来源: WILEY

摘要:

AbstractTwo series of new MP 3022 analogs, i.e. 1‐(o‐methoxyphenyl)‐4‐n‐propylpiperazines (3, 4a, 4b, 6–9, and12–13) and 2‐(n‐propyl)‐1,2,3,4‐tetrahydroisoquinolines (5a, 5b, 11a, and11b) containing a terminal heteroaromatic system with a different number of nitrogen atoms, were synthesized and their 5‐HT1A/5‐HT2Aand α1receptor affinity was assayed. The majority of investigated piperazines may be classified as non‐selective 5‐HT1A/5‐HT2A/α1receptor ligands. Compounds3, 4a, 4b, 7–9awith the highest affinity for 5‐HT1Areceptors (Ki= 4–54 nM) were testedin vivo.Their functional activity was differentiated; while3, 8, and9abehaved like weak antagonists of postsynaptic 5‐HT1Areceptors,4band7may be classified as potential partial 5‐HT1Areceptor agonists. Isomer4ahas characteristic features of a potenti

ISSN:0365-6233    

DOI:10.1002/ardp.19963291006

出版商:WILEY‐VCH Verlag    

年代:1996

数据来源: WILEY

摘要:

AbstractThe radical scavenging activity of tenoxicam against hydroxyl (HO⋅), superoxide (O2⋅−), and peroxyl (LOO⋅) radicals, all of them involved in the inflammatory reactions, has been tested in different cell‐free systems and by different techniques. Tenoxicam is a good scavenger of both HO⋅ radicals (IC50= 56.7 μM), as determined by Electron Spin Resonance (ESR) spectroscopy with the spin trapping (5,5‐dimethyl‐1‐pyrrolineN‐oxide, DMPO) technique, and O2⋅−radicals generated by the phenazine methosulfate/reduced β‐nicotinamide adenine dinucleotide (PMS/NADH) system. The high reactivity of the drug towards HO⋅ was confirmed by the rate constant of reaction with HO⋅ (k⋍ 1010M−1s−1), determined by competition kinetic studies withN,N‐dimethyl‐4‐nitrosoaniline. In addition at a μM level (1–5 μM) it dose‐dependently prevents the phycoerythrin peroxidation induced by the water‐soluble azoinitiator 2,2‐azobis(2‐amidinopropane) dihydrochloride (ABAP), indicating a quenching effect on aqueous peroxyl radicals. The HO⋅‐entrapping capacity was confirmed in models more close to thein vivosituation: tenoxicam inhibits the HO⋅‐induced depolymerization of hyaluronic acid already at 15 μM and the HO⋅‐driven lipid peroxidation in phosphatidylcholine liposomes (PCL) with an IC50of 10 μM. In this membrane model it delays at 1–10 μM level the decomposition of phosphatidylcholine hydroperoxides to short‐chain alkenals (markers: total carbonyl functions as 2,4‐dinitrophenylhydrazones and conjugated dienes). The high susceptibility of the drug of HO⋅ attack is also demonstrated by its extensive degradation (HPLC studies) when irradiated with HO⋅ radicals. The antioxidant component of tenoxicam evidenced in this study sheds some ligh

ISSN:0365-6233    

DOI:10.1002/ardp.19963291007

出版商:WILEY‐VCH Verlag    

年代:1996

数据来源: WILEY

摘要:

AbstractSpecific branched fatty acids are of great interest in the search of a new type of drug penetration enhancers across human skin for transdermal drug delivery and in gaining an understanding of structure‐activity relationships with skin lipids. A convenient synthesis has therefore been developed especially for ethyloctadecanoic acids. The successful syntheses of 6‐ and 9‐ethyloctadecanoic acids are reported

ISSN:0365-6233    

DOI:10.1002/ardp.19963291008

出版商:WILEY‐VCH Verlag    

年代:1996

数据来源: WILEY

摘要:

AbstractThe synthesis of eight novel 1,4‐benzodioxane derivatives is reported. The blocking activity of these compounds was determined on the pre‐ and postsynaptic α‐adrenoceptors of isolated rat vas deferens. Structure‐activity relationships are d

ISSN:0365-6233    

DOI:10.1002/ardp.19963291009

出版商:WILEY‐VCH Verlag    

年代:1996

数据来源: WILEY

ISSN:0365-6233    

DOI:10.1002/ardp.19963291010

出版商:WILEY‐VCH Verlag    

年代:1996

数据来源: WILEY

ISSN:0365-6233    

DOI:10.1002/ardp.19963291001

出版商:WILEY‐VCH Verlag    

年代:1996

数据来源: WILEY