Search Results - "Sasmal, Pradip K."
-
1
Anti-angiogenic and antioxidant effects of axitinib in human retinal endothelial cells: implications in diabetic retinopathy
Published in Frontiers in pharmacology (17-06-2024)“…Diabetic retinopathy is a secondary microvascular complication of diabetes mellitus. This disease progresses from two stages, non-proliferative and…”
Get full text
Journal Article -
2
Melanin concentrating hormone receptor 1 (MCHR1) antagonists—Still a viable approach for obesity treatment?
Published in Bioorganic & medicinal chemistry letters (01-10-2012)“…Obesity is a global epidemic associated with multiple severe diseases. Several pharmacotherapies have been investigated including the melanin concentrating…”
Get full text
Journal Article -
3
Design and optimization of quinazoline derivatives as melanin concentrating hormone receptor 1 (MCHR1) antagonists
Published in Bioorganic & medicinal chemistry letters (01-05-2012)“…The receptor model-supported design, synthesis and multi-parameter optimization of novel quinazoline derivatives as MCHR1 antagonists are described. The in…”
Get full text
Journal Article -
4
Design and optimization of quinazoline derivatives as melanin concentrating hormone receptor 1 (MCHR1) antagonists: Part 2
Published in Bioorganic & medicinal chemistry letters (01-05-2012)“…The synthesis and design guided by SAR and SPR studies of novel quinazoline derivatives as MCHR1 antagonists are described. Compound 8 (DRL-21816) has emerged…”
Get full text
Journal Article -
5
A deep eutectic-based, self-emulsifying subcutaneous depot system for apomorphine therapy in Parkinson's disease
Published in Proceedings of the National Academy of Sciences - PNAS (01-03-2022)“…Apomorphine, a dopamine agonist, is a highly effective therapeutic to prevent intermittent off episodes in advanced Parkinson's disease. However, its short…”
Get full text
Journal Article -
6
Asymmetric Synthesis of Hexapropionate Synthons by Sequential Enantiotopic Group Selective Enolization of Meso Diketones
Published in Organic letters (08-06-2006)“…Meso 1,9-diketones (six to seven stereocenters) are readily obtained by stepwise or simultaneous two-directional aldol reactions of…”
Get full text
Journal Article -
7
Studies toward the Synthesis of Azadirachtin, Part 2: Construction of Fully Functionalized ABCD Ring Frameworks and Unusual Intramolecular Reactions Induced by Close-Proximity Effects
Published in Angewandte Chemie International Edition (30-05-2005)“…The remarkable antifeedant agent and insecticide, azadirachtin (1), has, to date, escaped a total synthesis. The preparation of an advanced precursor has…”
Get full text
Journal Article -
8
Total Synthesis of 1-O-Methyllateriflorone
Published in Angewandte Chemie International Edition (15-09-2003)“…The unique spiroxalactone framework of lateriflorone (1) consists of a prenylated dihydrobenzoquinone moiety and a trioxatetracyclotetradecane system. A tandem…”
Get full text
Journal Article -
9
Formation of Bicyclic Ethers from Lewis Acid Promoted Cyclizations of Cyclic Oxonium Ions
Published in Organic letters (18-04-2002)“…Oxacycles carrying a vinyl group and an acetal were extended with a cyclization terminator (vinyl silane or vinyl sulfide) by Suzuki coupling. Treatment with…”
Get full text
Journal Article -
10
First total synthesis of 3a-hydroxy-1,1-dimethyl-5-((N-methylsulfamoyl)methyl)-1,2,3,3a,8,8a-hexahydropyrrolo[2,3-b]indol-1-ium 2,2,2-trifluoroacetate by mimicking the oxidative degradation pathway of sumatriptan
Published in Results in Chemistry (01-01-2021)“…[Display omitted] •Forced degradation studies were performed on sumatriptan autoinjector product Zembrace under different stress conditions.•The primary…”
Get full text
Journal Article -
11
Thiopyran Route to Polypropionates: Aldol Diastereoselectivity of Linear and Two-Directional Iterative Homologations
Published in Organic letters (04-05-2000)“…Aldol reaction of tetrahydro-4H-thiopyran-4-one with racemic 1,4-dioxa-8-thiaspiro[4.5]decane-6-carboxaldehyde is easily controlled to give the…”
Get full text
Journal Article -
12
Novel pyrazole-3-carboxamide derivatives as cannabinoid-1 (CB1) antagonists: Journey from non-polar to polar amides
Published in Bioorganic & medicinal chemistry letters (01-01-2011)“…The synthesis and biological evaluation of novel pyrazole-3-carboxamide derivatives as CB1 antagonists are described. The in vivo proof of principle for weight…”
Get full text
Journal Article -
13
Optimisation of in silico derived 2-aminobenzimidazole hits as unprecedented selective kappa opioid receptor agonists
Published in Bioorganic & medicinal chemistry letters (15-02-2015)“…[Display omitted] Kappa opioid receptor (KOR) is an important mediator of pain signaling and it is targeted for the treatment of various pains. Pharmacophore…”
Get full text
Journal Article -
14
Biomimetically Inspired Total Synthesis and Structure Activity Relationships of 1-O-Methyllateriflorone. 6π Electrocyclizations in Organic Synthesis
Published in Journal of the American Chemical Society (05-05-2004)“…The total synthesis of 1-O-methyllateriflorone (2) is described. The construction of the cage-like domain of the molecule involved a biomimetic…”
Get full text
Journal Article -
15
Structure–activity relationship studies of novel pyrazole and imidazole carboxamides as cannabinoid-1 (CB1) antagonists
Published in Bioorganic & medicinal chemistry letters (15-08-2011)“…The synthesis and biological evaluation of novel pyrazole and imidazole carboxamides as CB1 antagonists are described. The in vivo proof of principle for…”
Get full text
Journal Article -
16
Design, Synthesis, and Biological Properties of Highly Potent Epothilone B Analogues
Published in Angewandte Chemie International Edition (04-08-2003)“…A number of rationally designed epoxide and cyclopropane epothilone B (1) analogues with substituted side chains were prepared and their biological activities…”
Get full text
Journal Article -
17
Discovery of novel, orally available benzimidazoles as melanin concentrating hormone receptor 1 (MCHR1) antagonists
Published in Bioorganic & medicinal chemistry letters (15-09-2010)“…The synthesis and biological evaluation of novel benzimidazole derivatives as MCHR1 antagonists are described. The in vivo proof of principle for weight loss…”
Get full text
Journal Article -
18
Studies toward the Synthesis of Azadirachtin, Part 1: Total Synthesis of a Fully Functionalized ABC Ring Framework and Coupling with a Norbornene Domain
Published in Angewandte Chemie International Edition (30-05-2005)“…The advanced decalin intermediate 1 was synthesized and elaborated into the potential azadirachtin precursor 2. The challenging synthesis involved several…”
Get full text
Journal Article -
19
Syn−Anti Isomerization of Aldols by Enolization
Published in Journal of organic chemistry (09-07-2004)“…A variety of aldol adducts are shown to undergo efficient syn−anti isomerization in the presence of imidazole by an enolization mechanism. Isomerizations are…”
Get full text
Journal Article -
20
Acetal−Vinyl Sulfide Cyclization on Sugar Substrates: Effect of Structure and Substituent
Published in Journal of organic chemistry (07-02-2003)“…A range of 2-deoxyfuranoside and -pyranoside derivatives were fashioned into derivatives that carry a vinyl or propenyl side chain. Extension of the alkene by…”
Get full text
Journal Article