更新于：2024-11-04
Orchid Pharma Ltd.
更新于：2024-11-04
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A Randomized, Double-blind, Placebo-controlled, Stepwise Study of the Pharmacokinetics (PK), Pharmacodynamics (PD), PK/PD Characteristics and Safety of Multiple Once-daily Oral Dosing of DPOC-4088 in Healthy Young Male Subjects
A Phase 1 Dose-Escalation Study of the Safety andPharmacokinetics of Daily OCID 4681-S-01 Administered Orally to Subjects with Advanced Solid Tumors
A Randomized, Open-label, 4-period Crossover Study to Evaluate the Pharmacokinetics (PK), Pharmacodynamics (PD) and the PK/PD Relationship of DPOC-4088 After Single Oral Dosing of 100 and 200 mg in 2 Prolonged Release Formulations (16 and 20 hr) in 12 Healthy Young Male Subjects
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2020-04-28MINI-REVIEWS IN ORGANIC CHEMISTRY
Benzofuran: A Key Heterocycle - Ring Closure And Beyond
作者: Narasimhan, Kilambi ; Padmini, Vediappen ; Lavanya, Andiappan
::
The benzofuranyl motif present in compounds exhibits various medicinal properties and
non-drug applications. These derivatives are naturally occurring compounds or synthetic materials,
which cover a broad spectrum of pharmacological activities like anti-inflammatory, anti-diabetic, anti-
depressant, anti-HIV, anti-microbial, anti-proliferative, anti-convulsant, cytotoxic, analgesic, etc.
Few of the commercially interesting compounds from this class are, ailanthoidol (anti-inflammatory),
amiodarone, dronedarone, celivarone (anti-arrhythmic), bufuralol (muscular airways relaxant), morphine,
5-(2-aminopropyl)benzofuran; 5-APB, 6-(2-aminopropyl)benzofuran; 6-APB (CNS), rifampicin
(antibiotic), etc., whereas, some of the non-drug applications are in perfumery industry (bergapten)
and as tannin activators in sunscreen preparations (psoralen, 8-methoxypsoralen, and angelicin).
Considering these interesting biological activities and commercial utilities, a review on the synthetic
aspects of this privileged scaffold was attempted. For the benefit of natural product-based drug discovery,
available sources of these derivatives, extraction process and reported biological activities
have also been outlined in this review.
2018-03-09LETTERS IN ORGANIC CHEMISTRY
Divergent Synthesis of Novel Dienylbenzothiazoles and Arylidenedibenzoxazepines and Evaluation of Their Antiproliferative and Cytotoxic Properties
作者: Dhatchanamoorthy, N. ; Shanmuganathan, T. ; Kathiravan, P.R. ; Muthukumaran, S. ; Venugopal, M.
Dibenzo-oxazepine and Benzothiazole derivatives are used as antipsychotics, anticancer, antibacterial and anti-inflammatory agents.Arylidene derivatives of 1,2,3,4-Tetrahydro-Dibenzo[b,f][1,4]Oxazepine and 2-[2-Chloro- Cyclohex-1-enyl]- Benzothiazoles were synthesized by reacting benzylidene derivative of chloroaldehyde with 2-aminophenol and 2-aminothiophenol resp.Benzylidene derivative of chloroaldehyde was prepared by Vilsmeier reaction of 2-benzylidenecyclohexanone derivatives, which were obtained from the condensation of various aromatic aldehydes with cyclohexanone.Benzylidene derivatives of 1,2,3,4-Tetrahydro-Dibenzo[b,f][1,4]Oxazepine I [X = H, F, Cl, etc.] exhibited promising antiproliferative activity with GI50 values in the micromolar range.The compounds containing halo, alkyl and alkoxyl groups as substituents on the benzylidine ring have been found to be very effective cytotoxic agents.This study identified dibenzo-oxazepine as a prospective pharmacophore which set the stage for thorough exploration of this compound class as cytotoxic agents.
2017-01-01Journal of natural science, biology, and medicine
Novel hydroxamates potentiated in vitro activity of fluconazole against Candida albicans
Article
作者: Hariharan, Periasamy ; Franklyne, Jonathan S ; Bharani, Thirunavukkarasu ; Rajagopal, Sridharan ; Paul-Satyaseela, Maneesh ; Narayanan, Shridhar ; Kumar, Chenniappan Vinoth ; Balasubramanian, Gopalan ; Selvakumar, Thangapazham ; Kachhadia, Virendra ; Bharathimohan, Kuppusamy
A set of 12 novel hydroxamate compounds (NHCs), structurally designed as inhibitors of histone deacetylase (HDAC) enzyme, were synthesized at our facility. These were adamantane derivatives with N-hydroxyacetamide as pharmacophore, and each of these compounds was tested for potentiating activity on fluconazole. The concentration of fluconazole which completely inhibited (concentration of complete inhibition [CCI]) the growth of Candida albicans ATCC 90028 and C. albicans ATCC 64550 was determined by micro-dilution method in the absence and presence of NHCs. The CCI of fluconazole without the NHC combination was 64 μg/ml and 1024 μg/ml against C. albicans ATCC 90028 and C. albicans ATCC 64550, respectively. The majority of the NHCs potentiated the fluconazole activity markedly as CCI of fluconazole against C. albicans ATCC 90028 reduced to 0.25 μg/ml. Similarly, CCI of fluconazole against C. albicans ATCC 64550 reduced to 4-8 μg/ml in combination with majority of NHCs while the best activity was displayed by the compound 1 with a reduction of CCI to 0.5 μg/ml. The study results revealed the potential usage of hydroxamate derivatives, structurally designed as HDAC inhibitors to enhance the activity of fluconazole against C. albicans.
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