Design and Synthesis of Novel Hydrazides, Thiosemicarbazides, Oxadiazoles, and Triazoles ofN,N‘-Bis(1-carboxy-15-hydroxy-n- pentadec-8-yl)alkyl or -aryl Diamides: An Approach for Their Biological Evaluation and Possible Industrial Utilization

2004 ◽  
Vol 43 (17) ◽  
pp. 4979-4999 ◽  
Author(s):  
Kallappa M. Hosamani ◽  
Raviraj S. Pattanashettar
Keyword(s):  
Biological Evaluation ◽  
Design And Synthesis ◽  
Industrial Utilization

Design and synthesis, biological evaluation of bis-(1,2,3- and 1,2,4)-triazole derivatives as potential antimicrobial and antifungal agents

2021 ◽  
Vol 41 ◽  
pp. 128004
Author(s):  
Sampath Bitla ◽  
Akkiraju Anjini Gayatri ◽  
Muralidhar Reddy Puchakayala ◽  
Vijaya Kumar Bhukya ◽  
Jagadeshwar Vannada ◽  
...  
Keyword(s):  
Antifungal Agents ◽  
Biological Evaluation ◽  
Triazole Derivatives ◽  
Design And Synthesis

Design and synthesis of herboxidiene derivatives that potently inhibit in vitro splicing

2021 ◽  
Vol 19 (6) ◽  
pp. 1365-1377
Author(s):  
Arun K. Ghosh ◽  
Srinivasa Rao Allu ◽  
Guddeti Chandrashekar Reddy ◽  
Adriana Gamboa Lopez ◽  
Patricia Mendez ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Design And Synthesis ◽  
In Vitro Splicing ◽  
Enantioselective Syntheses ◽  
Derivatives Of

Enantioselective syntheses of C-6 modified derivatives of herboxidiene and their biological evaluation in splicing inhibitory assay.

scholarly journals The design and synthesis of an antibacterial phenothiazine–siderophore conjugate

2018 ◽  
Vol 14 ◽  
pp. 2646-2650 ◽  
Author(s):  
Abed Tarapdar ◽  
James K S Norris ◽  
Oliver Sampson ◽  
Galina Mukamolova ◽  
James T Hodgkinson
Keyword(s):  
Small Molecules ◽  
Antibacterial Agents ◽  
Multidrug Resistant ◽  
Biological Evaluation ◽  
Amide Bond ◽  
Design And Synthesis ◽  
Resistant Tuberculosis ◽  
Multidrug Resistant Tuberculosis ◽  
Latent Tb ◽  
Covalently Linked

Siderophore–antibiotic conjugates consist of an antibiotic covalently linked by a tether to a siderophore. Such conjugates can demonstrate enhanced uptake and internalisation to the bacterial cell resulting in significantly reduced MIC values and extended spectrum of activity. Phenothiazines are a class of small molecules that have been identified as a potential treatment for multidrug resistant tuberculosis and latent TB. Herein we report the design and synthesis of the first phenothiazine–siderophore conjugate. A convergent synthetic route was developed whereby the functionalised phenothiazine component was prepared in four steps and the siderophore component also prepared in four steps. In M. smegmatis the functionalised phenothiazine demonstrated an equipotent MIC value in direct comparison to the parent phenothiazine from which it was derived. The final conjugate was synthesised by amide bond formation between the two components and global deprotection of the PMB protecting groups to unmask the catechol iron chelating groups of the siderophore. The synthesis is readily amenable to the preparation of analogues whereby the siderophore component of the conjugate can be modified. The route will be used to prepare a library of siderophore–phenothiazine conjugates for full biological evaluation of much needed new antibacterial agents.

scholarly journals Design, Synthesis and Biological Evaluation of N4-Sulfonamido-Succinamic, Phthalamic, Acrylic and Benzoyl Acetic Acid Derivatives as Potential DPP IV Inhibitors

2013 ◽  
Vol 7 (1) ◽  
pp. 39-48 ◽  
Author(s):  
Reema Abu Khalaf ◽  
Ghassan Abu Sheikha ◽  
Mahmoud Al-Sha'er ◽  
Mutasem Taha
Keyword(s):  
Acetic Acid ◽  
Type Ii Diabetes Mellitus ◽  
Biological Evaluation ◽  
Diabetic Patients ◽  
Type Ii ◽  
Design Synthesis ◽  
Multifunctional Protein ◽  
Design And Synthesis ◽  
Dpp Iv

As incidence rate of type II diabetes mellitus continues to rise, there is a growing need to identify novel therapeutic agents with improved efficacy and reduced side effects. Dipeptidyl peptidase IV (DPP IV) is a multifunctional protein involved in many physiological processes. It deactivates the natural hypoglycemic incretin hormone effect. Inhibition of this enzyme increases endogenous incretin level, incretin activity and should restore glucose homeostasis in type II diabetic patients making it an attractive target for the development of new antidiabetic drugs. One of the interesting reported anti- DPP IV hits is Gemifloxacin which is used as a lead compound for the development of new DPP IV inhibitors. In the current work, design and synthesis of a series of N4-sulfonamido-succinamic, phthalamic, acrylic and benzoyl acetic acid derivatives was carried out. The synthesized compounds were evaluated for their in vitro anti-DPP IV activity. Some of them have shown reasonable bioactivity, where the most active one 17 was found to have an IC50 of 33.5 μM.

scholarly journals Design and synthesis of some novel 2-(3-methyl-2-oxoquinoxalin-1(2H)-yl)-N-(4-(substituted)phenyl)acetamide derivatives for biological evaluation as anticonvulsant agents

2013 ◽  
Vol 51 (1) ◽  
pp. 101-111 ◽  
Author(s):  
Mohamed-Kamal Ibrahim ◽  
Ashraf A. Abd-Elrahman ◽  
Rezk R.A. Ayyad ◽  
Khaled El-Adl ◽  
Ahmed M. Mansour ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Anticonvulsant Agents ◽  
Design And Synthesis

Design and synthesis of a phenyl C-glycoside derivative of Spliceostatin A and its biological evaluation toward prostate cancer treatment

2019 ◽  
Vol 60 (51) ◽  
pp. 151313 ◽  
Author(s):  
Yusuke Yoshikawa ◽  
Airi Ishibashi ◽  
Kenichi Murai ◽  
Yasufumi Kaneda ◽  
Keisuke Nimura ◽  
...  
Keyword(s):  
Prostate Cancer ◽  
Cancer Treatment ◽  
Biological Evaluation ◽  
Prostate Cancer Treatment ◽  
Design And Synthesis ◽  
Spliceostatin A

Design and synthesis of novel, potent and selective hypoxanthine analogs as adenosine A 1 receptor antagonists and their biological evaluation

2017 ◽  
Vol 25 (6) ◽  
pp. 1963-1975 ◽  
Author(s):  
Summon Koul ◽  
Vidya Ramdas ◽  
Dinesh A. Barawkar ◽  
Yogesh B. Waman ◽  
Neela Prasad ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Receptor Antagonists ◽  
Design And Synthesis
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