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Dive into the research topics where Ashwin U. Rao is active.

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Featured researches published by Ashwin U. Rao.


Bioorganic & Medicinal Chemistry Letters | 2012

Facile synthesis of tetracyclic azepine and oxazocine derivatives and their potential as MAPKAP-K2 (MK2) inhibitors.

Ashwin U. Rao; Dong Xiao; Xianhai Huang; Wei Zhou; James Fossetta; Dan Lundell; Fang Tian; Prashant Trivedi; Robert Aslanian; Anandan Palani

Facile synthesis of two new series of tetracyclic azepine and oxazocine analogs is described. These analogs were evaluated for their potential as MAPKAP-K2 (MK2) inhibitors and several were found to be potent at inhibiting MK2 with a non-ATP competitive binding mode.


Bioorganic & Medicinal Chemistry Letters | 2014

Discovery of a novel series of potent MK2 non-ATP competitive inhibitors using 1,2-substituted azoles as cis-amide isosteres.

Dong Xiao; Xiaohong Zhu; Michael Sofolarides; Sylvia Degrado; Ning Shao; Ashwin U. Rao; Xiao Chen; Robert Aslanian; James Fossetta; Fang Tian; Prashant Trivedi; Daniel Lundell; Anandan Palani

A unified strategy was conceived and implemented to deliver conformationally constrained anilides based on their preferred cis-amide conformers. The imidazole/triazole mimicing amide bonds were designed, building upon an earlier discovery of a novel series of tricyclic lactams MK2 kinase inhibitors. This approach enabled rapid, modular synthesis of structurally novel analogs. The efficient SAR development led to the discovery of low molecular weight and potent MK2 non-ATP competitive inhibitors with good ligand efficiency, which led to improved permeability and oral exposure in rats.


Bioorganic & Medicinal Chemistry Letters | 2014

Quality by design (QbD) of amide isosteres: 5,5-Disubstituted isoxazolines as potent CRTh2 antagonists with favorable pharmacokinetic and drug-like properties.

Dong Xiao; Xiaohong Zhu; Younong Yu; Ning Shao; Jie Wu; Kevin D. McCormick; Pawan Dhondi; Jun Qin; Robert Mazzola; Haiqun Tang; Ashwin U. Rao; Phieng Siliphaivanh; Hongchen Qiu; Xiaoxin Yang; Maria A. Rivelli; Charles G. Garlisi; Steve Eckel; Gitali Mukhopadhyay; Craig Correll; Diane Rindgen; Robert Aslanian; Anandan Palani

Isoxazoles are frequently used amide isosteres, as shown in the context of discovery of CRTh2 antagonists from amide 1 to isoxazole 2. However, persistent agonism and poor solubility in isoxazole series presented challenges to its further development. Based on the concept of quality by design (QbD), 5,5-disubstituted isoxazolines 3 were introduced. The chirality at 5 position of isoxazolines controlled the switch between two modes of actions, which led to a novel series of pure antagonists. This non-planar motif also conferred a change of shape of these molecules, which avoided flat structures and improved their physical properties.


Bioorganic & Medicinal Chemistry Letters | 2012

SAR studies of C2 ethers of 2H-pyrano[2,3-d]pyrimidine-2,4,7(1H,3H)-triones as nicotinic acid receptor (NAR) agonist

Xianhai Huang; Jing Su; Ashwin U. Rao; Haiqun Tang; Wei Zhou; Xiaohong Zhu; Xiao Chen; Zhidan Liu; Ying Huang; Sylvia Degrado; Dong Xiao; Jun Qin; Robert Aslanian; Brian A. McKittrick; Scott Greenfeder; Margaret van Heek; Madhu Chintala; Anandan Palani

Based on in house screening lead compound 1 for the NAR project, SAR studies have been focused on the modification of the C2 ethers of the pyrimidinedione core structure. In this effort, an unpredictable SAR trend was overcome in the alkyl ether and arylalkyl ether series to identify compound 24 with improved in vitro activity compared to nicotinic acid. More consistent and predictable SAR was achieved in the propargyl ether series. Lead compound 41 was identified with good in vitro and in vivo activity in rat, and much improved rat PK profile.


Archive | 2011

Quinazolinone-type compounds as crth2 antagonists

Robert Aslanian; Christopher W. Boyce; Robert Mazzola; Brian A. McKittrick; Kevin D. McCormick; Anandan Palani; Jun Qin; Haiqun Tang; Dong Xiao; Younong Yu; John P. Caldwell; Elizabeth Helen Kelley; Hongjun Zhang; Phieng Siliphaivanh; Rachel N. Maccoss; Joey L. Methot; Jolicia Polivina Gauuan; Qin Jiang; Andrew J. Leyhane; Purakkattle Biju; Li Dong; Xianhai Huang; Ning Shao; Wei Zhou; Pawan Dhondi; Ashwin U. Rao


Archive | 2009

BIARYL SPIROAMINOOXAZOLINE ANALOGUES AS ALPHA2C ADRENERGIC RECEPTOR MODULATORS

Kevin D. McCormick; Li Dong; Christopher W. Boyce; Lera Ruiz Manuel De; Salem Fevrier; Jie Wu; Junying Zheng; Younong Yu; Jianhua Chao; Walter Won; Ashwin U. Rao; Rongze Kuang; Pauline C. Ting; Xianhai Huang; Ning Shao; Anandan Palani; Michael Berlin; Robert Aslanian


Archive | 2012

IMIDAZOLE DERIVATIVES AND METHODS OF USE THEREOF

Ashwin U. Rao; Anandan Palani; Robert Aslanian


Archive | 2011

Substituted quinoxalines as inhibitors of fatty acid binding protein

Clifford Cheng; Gerald W. Shipps; Xiaohua Huang; Ying Huang; Ning Shao; Ashwin U. Rao; Anandan Palani; Peter Orth; Johannes Voigt; Robert Jason Herr; Lana M. Rossiter; Qi Zeng; Xianfeng Sun


Archive | 2009

Biaryl-spiroaminooxazoline analogues as alpha 2c adrenergic receptor modulators

Kevin D. McCormick; Li Dong; Christopher W. Boyce; Manuel de Lera Ruiz; Salem Fevrier; Jie Wu; Junying Zheng; Youngong Yu; Jianhua Chao; Walter Won; Ashwin U. Rao; Rongze Kuang; Pauline C. Ting; Xianhai Huang; Ning Shao; Anandan Palani; Michael Berlin; Robert Aslanian


Archive | 2006

ORTHO-CONDENSED 2-PYRIDINONE DERIVATIVES AS NICOTINIC ACID RECEPTOR AGONISTS FOR THE TREATMENT OF DYSLIPIDEMIA

Anandan Palani; Jing Su; Dong Xiao; Xianhai Huang; Ashwin U. Rao; Xiao Chen; Haiqun Tang; Jun Qin; Ying Huang; Robert Aslanian; Brian A. McKittrick

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