The Experts below are selected from a list of 207 Experts worldwide ranked by ideXlab platform
Saeed Emami - One of the best experts on this subject based on the ideXlab platform.
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Synthesis, in vitro antifungal evaluation and in silico study of 3-azolyl-4-chromanone phenylhydrazones
DARU Journal of Pharmaceutical Sciences, 2012Co-Authors: Adile Ayati, Mehraban Falahati, Hamid Irannejad, Saeed EmamiAbstract:Background The currently available antifungal drugs suffer from toxicity, greatest potential drug interactions with other drugs, insufficient pharmacokinetics properties, and development of resistance. Thus, development of new antifungal agents with optimum pharmacokinetics and less toxicity is urgent task. In the search for new azole antifungals, we have been previously described azolylchromanone oxime ethers as rigid analogs of Oxiconazole. In continuation of our work, we incorporated phenylhydrazone moiety instead of oxime ether fragment in azolylchromanone derivatives. Methods The 3-azolyl-4-chromanone phenylhydrazones were synthesized via ring closure of 2-azolyl-2'-hydroxyacetophenones and subsequent reaction with phenylhydrazine. The biological activity of title compounds was evaluated against different pathogenic fungi including Candida albicans , Saccharomyces cerevisiae , Aspergillus niger , and Microsporum gypseum . Docking study, in silico toxicity risks and drug-likeness predictions were used to better define of title compounds as antifungal agents. Results The in vitro antifungal activity of compounds based on MIC values revealed that all compounds showed good antifungal activity against C. albicans , S. cerevisiae and M. gypseum at concentrations less than 16 μg/mL. Among the test compounds, 2-methyl-3-imidazolyl derivative 3b showed the highest values of drug-likeness and drug-score. Conclusion The 3-azolyl-4-chromanone phenylhydrazones considered as analogs of 3-azolyl-4-chromanone oxime ethers basically designed as antifungal agents. The antifungal activity of title compounds was comparable to that of standard drug fluconazole. The drug-likeness data of synthesized compounds make them promising leads for future development of antifungal agents.
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synthesis in vitro antifungal evaluation and in silico study of 3 azolyl 4 chromanone phenylhydrazones
DARU, 2012Co-Authors: Adile Ayati, Mehraban Falahati, Hamid Irannejad, Saeed EmamiAbstract:The currently available antifungal drugs suffer from toxicity, greatest potential drug interactions with other drugs, insufficient pharmacokinetics properties, and development of resistance. Thus, development of new antifungal agents with optimum pharmacokinetics and less toxicity is urgent task. In the search for new azole antifungals, we have been previously described azolylchromanone oxime ethers as rigid analogs of Oxiconazole. In continuation of our work, we incorporated phenylhydrazone moiety instead of oxime ether fragment in azolylchromanone derivatives. The 3-azolyl-4-chromanone phenylhydrazones were synthesized via ring closure of 2-azolyl-2'-hydroxyacetophenones and subsequent reaction with phenylhydrazine. The biological activity of title compounds was evaluated against different pathogenic fungi including Candida albicans, Saccharomyces cerevisiae, Aspergillus niger, and Microsporum gypseum. Docking study, in silico toxicity risks and drug-likeness predictions were used to better define of title compounds as antifungal agents. The in vitro antifungal activity of compounds based on MIC values revealed that all compounds showed good antifungal activity against C. albicans, S. cerevisiae and M. gypseum at concentrations less than 16 μg/mL. Among the test compounds, 2-methyl-3-imidazolyl derivative 3b showed the highest values of drug-likeness and drug-score. The 3-azolyl-4-chromanone phenylhydrazones considered as analogs of 3-azolyl-4-chromanone oxime ethers basically designed as antifungal agents. The antifungal activity of title compounds was comparable to that of standard drug fluconazole. The drug-likeness data of synthesized compounds make them promising leads for future development of antifungal agents.
Adile Ayati - One of the best experts on this subject based on the ideXlab platform.
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Synthesis, in vitro antifungal evaluation and in silico study of 3-azolyl-4-chromanone phenylhydrazones
DARU Journal of Pharmaceutical Sciences, 2012Co-Authors: Adile Ayati, Mehraban Falahati, Hamid Irannejad, Saeed EmamiAbstract:Background The currently available antifungal drugs suffer from toxicity, greatest potential drug interactions with other drugs, insufficient pharmacokinetics properties, and development of resistance. Thus, development of new antifungal agents with optimum pharmacokinetics and less toxicity is urgent task. In the search for new azole antifungals, we have been previously described azolylchromanone oxime ethers as rigid analogs of Oxiconazole. In continuation of our work, we incorporated phenylhydrazone moiety instead of oxime ether fragment in azolylchromanone derivatives. Methods The 3-azolyl-4-chromanone phenylhydrazones were synthesized via ring closure of 2-azolyl-2'-hydroxyacetophenones and subsequent reaction with phenylhydrazine. The biological activity of title compounds was evaluated against different pathogenic fungi including Candida albicans , Saccharomyces cerevisiae , Aspergillus niger , and Microsporum gypseum . Docking study, in silico toxicity risks and drug-likeness predictions were used to better define of title compounds as antifungal agents. Results The in vitro antifungal activity of compounds based on MIC values revealed that all compounds showed good antifungal activity against C. albicans , S. cerevisiae and M. gypseum at concentrations less than 16 μg/mL. Among the test compounds, 2-methyl-3-imidazolyl derivative 3b showed the highest values of drug-likeness and drug-score. Conclusion The 3-azolyl-4-chromanone phenylhydrazones considered as analogs of 3-azolyl-4-chromanone oxime ethers basically designed as antifungal agents. The antifungal activity of title compounds was comparable to that of standard drug fluconazole. The drug-likeness data of synthesized compounds make them promising leads for future development of antifungal agents.
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synthesis in vitro antifungal evaluation and in silico study of 3 azolyl 4 chromanone phenylhydrazones
DARU, 2012Co-Authors: Adile Ayati, Mehraban Falahati, Hamid Irannejad, Saeed EmamiAbstract:The currently available antifungal drugs suffer from toxicity, greatest potential drug interactions with other drugs, insufficient pharmacokinetics properties, and development of resistance. Thus, development of new antifungal agents with optimum pharmacokinetics and less toxicity is urgent task. In the search for new azole antifungals, we have been previously described azolylchromanone oxime ethers as rigid analogs of Oxiconazole. In continuation of our work, we incorporated phenylhydrazone moiety instead of oxime ether fragment in azolylchromanone derivatives. The 3-azolyl-4-chromanone phenylhydrazones were synthesized via ring closure of 2-azolyl-2'-hydroxyacetophenones and subsequent reaction with phenylhydrazine. The biological activity of title compounds was evaluated against different pathogenic fungi including Candida albicans, Saccharomyces cerevisiae, Aspergillus niger, and Microsporum gypseum. Docking study, in silico toxicity risks and drug-likeness predictions were used to better define of title compounds as antifungal agents. The in vitro antifungal activity of compounds based on MIC values revealed that all compounds showed good antifungal activity against C. albicans, S. cerevisiae and M. gypseum at concentrations less than 16 μg/mL. Among the test compounds, 2-methyl-3-imidazolyl derivative 3b showed the highest values of drug-likeness and drug-score. The 3-azolyl-4-chromanone phenylhydrazones considered as analogs of 3-azolyl-4-chromanone oxime ethers basically designed as antifungal agents. The antifungal activity of title compounds was comparable to that of standard drug fluconazole. The drug-likeness data of synthesized compounds make them promising leads for future development of antifungal agents.
W Wagner - One of the best experts on this subject based on the ideXlab platform.
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vergleich der klinischen wirksamkeit und vertraglichkeit von oxiconazol nach 1 x taglicher applikation mit der nach 2 x taglicher applikation comparison of clinical efficacy and tolerability of Oxiconazole one dose versus two doses daily
Mycoses, 2009Co-Authors: W WagnerAbstract:Zusammenfassung: An insgesamt 144 Patienten, die an Dermatomykosen bzw. Pityriasis versicolor litten, wurden Oxiconazol*-Creme bzw. -Losung bezuglich Wirksamkeit und Vertraglichkeit untersucht. Die Anwendung erfolgte bei 73 Patienten nur 1 x taglich, bei 71 Patienten 2 x taglich. Die Therapiedauer betrug in beiden Kollektiven im Durchschnitt 3 bis 4 Wochen. Weder hinsichtlich Wirksamkeit noch hinsichtlich Vertraglichkeit konnte ein Unterschied zwischen beiden Patientengruppen ermittelt werden. Somit wird mit der einmal taglichen Applikation von Oceral Roche der gleiche Therapieerfolg erzielt wie mit der zweimal taglichen Applikation. Summary: Oxiconazole cream or solution was tested for efficacy and tolerability in a total of 144 patients suffering from dermatomycosis or tinea versicolor. 73 patients received the treatment only once daily and 71 twice daily. In both groups the treatment lasted on an average 3–4 weeks. No difference was found between the two populations with respect to efficacy or tolerability. We may conclude that a single daily application of Oceral Roche provides the same therapeutic success as the twice daily application.
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oxiconazol bei dermatomykosen ein doppelblinder randomisierter therapievergleich mit bifonazol oxiconazol in dermatomycosis a double blind randomized comparison with bifonazol
Mycoses, 2009Co-Authors: W Wagner, Renate ReckersczaschkaAbstract:Summary: In a total of 204 patients with dermatomycosis and erythrasma, Oxiconazole (Oceral Roche, producer Hoffmann—La Roche AG, Grenzach-Wyhlen, (n = 105) and bifonazole (n = 99) were tested in a double—blind, randomized multicenter study. Both preparations were compared in regard to efficacy and tolerance. The period of treatment in both groups was 25 days on average. Mycological sanitation and clinical healing was seen in 81 % and 86 % of these cases respectively. Tolerance has been judged as excellent in 70 % and 71 % of all patients respectively. Local intolerances were noticed in 1 % and 4 % of all patients respectively. Both preparations can be regarded as equally effective and tolerable. Zusammenfassung: An insgesamt 204 Patienten mit Dermatomykosen und Erythrasma wurden Oxiconazol* (n = 105) und Bifonazol (n = 99) im Rahmen einer doppelblinden, randomisierten, multizentrischen Prufung untersucht. Beide Pra parate wurden hinsichtlich Wirksamkeit und Vertraglichkeit verglichen. Die Therapiedauer betrug in den zwei Kollektiven im Mittel 25 Tage. Die mykologische Sanierung und klinische Heilung wurde in 81% bzw. 86 % der Falle erreicht. Die Vertraglichkeit wurde bei 70% aller Patienten als ausgezeichnet beurteilt. Lokale Unvertraglichkeiten traten bei 1% bzw. 4% der Patienten auf. Beide Praparate konnen als gleich gut wirksam und vertraglich bezeichnet werden.
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Oxiconazole in dermatomycosis a double blind randomized therapy compared with bifonazole
Mycoses, 2009Co-Authors: W Wagner, Renate ReckersczaschkaAbstract:Summary: In a total of 204 patients with dermatomycosis and erythrasma, Oxiconazole (Oceral Roche, producer Hoffmann—La Roche AG, Grenzach-Wyhlen, (n = 105) and bifonazole (n = 99) were tested in a double—blind, randomized multicenter study. Both preparations were compared in regard to efficacy and tolerance. The period of treatment in both groups was 25 days on average. Mycological sanitation and clinical healing was seen in 81 % and 86 % of these cases respectively. Tolerance has been judged as excellent in 70 % and 71 % of all patients respectively. Local intolerances were noticed in 1 % and 4 % of all patients respectively. Both preparations can be regarded as equally effective and tolerable. Zusammenfassung: An insgesamt 204 Patienten mit Dermatomykosen und Erythrasma wurden Oxiconazol* (n = 105) und Bifonazol (n = 99) im Rahmen einer doppelblinden, randomisierten, multizentrischen Prufung untersucht. Beide Pra parate wurden hinsichtlich Wirksamkeit und Vertraglichkeit verglichen. Die Therapiedauer betrug in den zwei Kollektiven im Mittel 25 Tage. Die mykologische Sanierung und klinische Heilung wurde in 81% bzw. 86 % der Falle erreicht. Die Vertraglichkeit wurde bei 70% aller Patienten als ausgezeichnet beurteilt. Lokale Unvertraglichkeiten traten bei 1% bzw. 4% der Patienten auf. Beide Praparate konnen als gleich gut wirksam und vertraglich bezeichnet werden.
Hamid Irannejad - One of the best experts on this subject based on the ideXlab platform.
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Synthesis, in vitro antifungal evaluation and in silico study of 3-azolyl-4-chromanone phenylhydrazones
DARU Journal of Pharmaceutical Sciences, 2012Co-Authors: Adile Ayati, Mehraban Falahati, Hamid Irannejad, Saeed EmamiAbstract:Background The currently available antifungal drugs suffer from toxicity, greatest potential drug interactions with other drugs, insufficient pharmacokinetics properties, and development of resistance. Thus, development of new antifungal agents with optimum pharmacokinetics and less toxicity is urgent task. In the search for new azole antifungals, we have been previously described azolylchromanone oxime ethers as rigid analogs of Oxiconazole. In continuation of our work, we incorporated phenylhydrazone moiety instead of oxime ether fragment in azolylchromanone derivatives. Methods The 3-azolyl-4-chromanone phenylhydrazones were synthesized via ring closure of 2-azolyl-2'-hydroxyacetophenones and subsequent reaction with phenylhydrazine. The biological activity of title compounds was evaluated against different pathogenic fungi including Candida albicans , Saccharomyces cerevisiae , Aspergillus niger , and Microsporum gypseum . Docking study, in silico toxicity risks and drug-likeness predictions were used to better define of title compounds as antifungal agents. Results The in vitro antifungal activity of compounds based on MIC values revealed that all compounds showed good antifungal activity against C. albicans , S. cerevisiae and M. gypseum at concentrations less than 16 μg/mL. Among the test compounds, 2-methyl-3-imidazolyl derivative 3b showed the highest values of drug-likeness and drug-score. Conclusion The 3-azolyl-4-chromanone phenylhydrazones considered as analogs of 3-azolyl-4-chromanone oxime ethers basically designed as antifungal agents. The antifungal activity of title compounds was comparable to that of standard drug fluconazole. The drug-likeness data of synthesized compounds make them promising leads for future development of antifungal agents.
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synthesis in vitro antifungal evaluation and in silico study of 3 azolyl 4 chromanone phenylhydrazones
DARU, 2012Co-Authors: Adile Ayati, Mehraban Falahati, Hamid Irannejad, Saeed EmamiAbstract:The currently available antifungal drugs suffer from toxicity, greatest potential drug interactions with other drugs, insufficient pharmacokinetics properties, and development of resistance. Thus, development of new antifungal agents with optimum pharmacokinetics and less toxicity is urgent task. In the search for new azole antifungals, we have been previously described azolylchromanone oxime ethers as rigid analogs of Oxiconazole. In continuation of our work, we incorporated phenylhydrazone moiety instead of oxime ether fragment in azolylchromanone derivatives. The 3-azolyl-4-chromanone phenylhydrazones were synthesized via ring closure of 2-azolyl-2'-hydroxyacetophenones and subsequent reaction with phenylhydrazine. The biological activity of title compounds was evaluated against different pathogenic fungi including Candida albicans, Saccharomyces cerevisiae, Aspergillus niger, and Microsporum gypseum. Docking study, in silico toxicity risks and drug-likeness predictions were used to better define of title compounds as antifungal agents. The in vitro antifungal activity of compounds based on MIC values revealed that all compounds showed good antifungal activity against C. albicans, S. cerevisiae and M. gypseum at concentrations less than 16 μg/mL. Among the test compounds, 2-methyl-3-imidazolyl derivative 3b showed the highest values of drug-likeness and drug-score. The 3-azolyl-4-chromanone phenylhydrazones considered as analogs of 3-azolyl-4-chromanone oxime ethers basically designed as antifungal agents. The antifungal activity of title compounds was comparable to that of standard drug fluconazole. The drug-likeness data of synthesized compounds make them promising leads for future development of antifungal agents.
Mehraban Falahati - One of the best experts on this subject based on the ideXlab platform.
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Synthesis, in vitro antifungal evaluation and in silico study of 3-azolyl-4-chromanone phenylhydrazones
DARU Journal of Pharmaceutical Sciences, 2012Co-Authors: Adile Ayati, Mehraban Falahati, Hamid Irannejad, Saeed EmamiAbstract:Background The currently available antifungal drugs suffer from toxicity, greatest potential drug interactions with other drugs, insufficient pharmacokinetics properties, and development of resistance. Thus, development of new antifungal agents with optimum pharmacokinetics and less toxicity is urgent task. In the search for new azole antifungals, we have been previously described azolylchromanone oxime ethers as rigid analogs of Oxiconazole. In continuation of our work, we incorporated phenylhydrazone moiety instead of oxime ether fragment in azolylchromanone derivatives. Methods The 3-azolyl-4-chromanone phenylhydrazones were synthesized via ring closure of 2-azolyl-2'-hydroxyacetophenones and subsequent reaction with phenylhydrazine. The biological activity of title compounds was evaluated against different pathogenic fungi including Candida albicans , Saccharomyces cerevisiae , Aspergillus niger , and Microsporum gypseum . Docking study, in silico toxicity risks and drug-likeness predictions were used to better define of title compounds as antifungal agents. Results The in vitro antifungal activity of compounds based on MIC values revealed that all compounds showed good antifungal activity against C. albicans , S. cerevisiae and M. gypseum at concentrations less than 16 μg/mL. Among the test compounds, 2-methyl-3-imidazolyl derivative 3b showed the highest values of drug-likeness and drug-score. Conclusion The 3-azolyl-4-chromanone phenylhydrazones considered as analogs of 3-azolyl-4-chromanone oxime ethers basically designed as antifungal agents. The antifungal activity of title compounds was comparable to that of standard drug fluconazole. The drug-likeness data of synthesized compounds make them promising leads for future development of antifungal agents.
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synthesis in vitro antifungal evaluation and in silico study of 3 azolyl 4 chromanone phenylhydrazones
DARU, 2012Co-Authors: Adile Ayati, Mehraban Falahati, Hamid Irannejad, Saeed EmamiAbstract:The currently available antifungal drugs suffer from toxicity, greatest potential drug interactions with other drugs, insufficient pharmacokinetics properties, and development of resistance. Thus, development of new antifungal agents with optimum pharmacokinetics and less toxicity is urgent task. In the search for new azole antifungals, we have been previously described azolylchromanone oxime ethers as rigid analogs of Oxiconazole. In continuation of our work, we incorporated phenylhydrazone moiety instead of oxime ether fragment in azolylchromanone derivatives. The 3-azolyl-4-chromanone phenylhydrazones were synthesized via ring closure of 2-azolyl-2'-hydroxyacetophenones and subsequent reaction with phenylhydrazine. The biological activity of title compounds was evaluated against different pathogenic fungi including Candida albicans, Saccharomyces cerevisiae, Aspergillus niger, and Microsporum gypseum. Docking study, in silico toxicity risks and drug-likeness predictions were used to better define of title compounds as antifungal agents. The in vitro antifungal activity of compounds based on MIC values revealed that all compounds showed good antifungal activity against C. albicans, S. cerevisiae and M. gypseum at concentrations less than 16 μg/mL. Among the test compounds, 2-methyl-3-imidazolyl derivative 3b showed the highest values of drug-likeness and drug-score. The 3-azolyl-4-chromanone phenylhydrazones considered as analogs of 3-azolyl-4-chromanone oxime ethers basically designed as antifungal agents. The antifungal activity of title compounds was comparable to that of standard drug fluconazole. The drug-likeness data of synthesized compounds make them promising leads for future development of antifungal agents.
