Antimycotic imidazoles. Part 4. Synthesis and antifungal activity of ketoconazole, a new potent orally active broad-spectrum antifungal agent

Heeres, Jan; Backx, L. J. J.; Mostmans, J. H.; Cutsem, J. Van

doi:10.1021/jm00194a023

Cited by 329 publications

(131 citation statements)

References 2 publications

Supporting

Mentioning

123

Contrasting

Unclassified

Order By: Relevance

“…Ketoconazole is an orally active, antifungal imidazole derivative synthesized and developed by Janssen Pharmaceutica in 1977 (127,302). It is considered to be the "gold standard" among the azole derivative antifungal drugs.…”

Section: Ketoconazolementioning

confidence: 99%

Overview of medically important antifungal azole derivatives

1988

View full text Add to dashboard Cite

Fungal infections are a major burden to the health and welfare of modern humans. They range from simply cosmetic, non-life-threatening skin infections to severe, systemic infections that may lead to significant debilitation or death. The selection of chemotherapeutic agents useful for the treatment of fungal infections is small. In this overview, a major chemical group with antifungal activity, the azole derivatives, is examined. Included are historical and state of the art information on the in vitro activity, experimental in vivo activity, mode of action, pharmacokinetics, clinical studies, and uses and adverse reactions of imidazoles currently marketed (clotrimazole, miconazole, econazole, ketoconazole, bifonazole, butoconazole, croconazole, fenticonazole, isoconazole, oxiconazole, sulconazole, and tioconazole) and under development (aliconazole and omoconazole), as well as triazoles currently marketed (terconazole) and under development (fluconazole, itraconazole, vibunazole, alteconazole, and ICI 195,739).

show abstract

Section: Ketoconazolementioning

confidence: 99%

Overview of medically important antifungal azole derivatives

1988

View full text Add to dashboard Cite

show abstract

“…6,7 In other studies, ketoconazole showed a wide spectrum of antimycotic activity against dermatophytes, Malassezia species and Candida species in vitro. 10 Topical ketoconazole 2% cream was used in this study for the treatment of Pityriasis versicolor, which had previously given 80%-90% of cure rate in the treatment of Pityriasis versicolor in other studies.…”

Section: Time Periodmentioning

confidence: 99%

A Study of Comparative Assessment of the Therapeutic Efficacy of Topical Luliconazole Versus Topical Ketoconazole in the Treatment of Pityriasis Versicolor

Kumar¹

2018

jebmh

View full text Add to dashboard Cite

BACKGROUNDPityriasis versicolor is one of the most common and recurring superficial fungal infections of the skin occurring in the patients attending the Dermatology Outpatient Department. Malassezia species are the causative organisms for the Pityriasis versicolor. Many different modalities of treatment are available to treat Pityriasis versicolor.The aim of the present study is to evaluate the drug, which is more therapeutically efficacious among topical luliconazole 1% cream versus topical ketoconazole 2% cream in the treatment of Pityriasis versicolor.

show abstract

“…Each of the reconstituted extract was added into 100 ml of respective medium in a conical flask, stirred and let to stand at 40-50 o C for 30 min. The positive control consisted of ketoconazole (Keto) incorporated at 10µg/ml of media (Heeres et al, 1979).The medium in each flask was poured in four petri dishes (replicates).…”

Section: Extractionmentioning

confidence: 99%

IN VITRO ANTIFUNGAL ACTIVITY OF METHANOLIC EXTRACTS OF DIFFERENT Senna didymobotrya (FRESEN.) H.S. IRWIN & BARNEBY PLANT PARTS

Jeruto¹,

Arama²,

Anyango³

et al. 2016

Afr J Tradit Complement Altern Med

View full text Add to dashboard Cite

Background: Herbal medicines have been in use for many years and remain widespread in developing countries; whereas, the use of complementary alternative medicine is on the increase in developed countries. Senna didymobotrya is important for its medicinal benefits among most communities in treating a wide range of ailments. Materials and methods: Plants were collected from a cluster in Siaya, Nandi and Nakuru counties (Kenya). Stem bark, root bark, leaves, flowers and immature pods were obtained; air-dried and ground into fine powder. Methanol was used to extract the plant extracts. The extracts were reconstituted in water and incorporated into growth media to obtain 0%, 2.5%, 5%, 7.5% and 10%. Bioassays were carried out on T. tonsurans (ATCC 28942) and C. albicans (14053). The growth of cultures on the plates was measured over a period of sixteen days. The area under disease progress stairs was determined and subjected to ANOVA and comparison of means using LSD. Results: Results indicated that the growth of C. albicans was not significantly affected by the plant extracts. Growth of T. tonsurans was completely inhibited by immature pods extract at 10%, the leaves and flowers extracts inhibited the growth at 7.5%. The stem and root bark extracts inhibited growth at low dosages of 2.5-5 %. Conclusion: There is need to carry out research on root and stem barks to identify the active phytochemicals that contribute to their high efficacies. On species conservation, harvesting of roots may lead to depletion of S. didymobotrya.

show abstract

Antimycotic imidazoles. Part 4. Synthesis and antifungal activity of ketoconazole, a new potent orally active broad-spectrum antifungal agent

Cited by 329 publications

References 2 publications

Overview of medically important antifungal azole derivatives

Overview of medically important antifungal azole derivatives

A Study of Comparative Assessment of the Therapeutic Efficacy of Topical Luliconazole Versus Topical Ketoconazole in the Treatment of Pityriasis Versicolor

IN VITRO ANTIFUNGAL ACTIVITY OF METHANOLIC EXTRACTS OF DIFFERENT Senna didymobotrya (FRESEN.) H.S. IRWIN & BARNEBY PLANT PARTS

Contact Info

Product

Resources

About