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Items: 28

1.

Discovery of Novel, Potent, Brain-Permeable, and Orally Efficacious Positive Allosteric Modulator of α7 Nicotinic Acetylcholine Receptor [4-(5-(4-Chlorophenyl)-4-methyl-2-propionylthiophen-3-yl)benzenesulfonamide]: Structure-Activity Relationship and Preclinical Characterization.

Sinha N, Karche NP, Verma MK, Walunj SS, Nigade PB, Jana G, Kurhade SP, Hajare AK, Tilekar AR, Jadhav GR, Thube BR, Shaikh JS, Balgude S, Singh LB, Mahimane V, Adurkar SK, Hatnapure G, Raje F, Bhosale Y, Bhanage D, Sachchidanand S, Dixit R, Gupta R, Bokare AM, Dandekar M, Bharne A, Chatterjee M, Desai S, Koul S, Modi D, Mehta M, Patil V, Singh M, Gundu J, Goel RN, Shah C, Sharma S, Bakhle D, Kamboj RK, Palle VP.

J Med Chem. 2019 Dec 6. doi: 10.1021/acs.jmedchem.9b01569. [Epub ahead of print]

PMID:
31755711
2.

Discovery and Characterization of Potent Pan-Genotypic HCV NS5A Inhibitors Containing Novel Tricyclic Central Core Leading to Clinical Candidate.

Ramdas V, Talwar R, Banerjee M, Joshi AA, Das AK, Walke DS, Borhade P, Dhayagude U, Loriya R, Gote G, Bommakanti A, Sivaram A, Agarwal G, Goswami A, Nigade P, Mehta M, Patil V, Modi D, Kumar H, Mallurwar S, Dash A, Modi F, Kuldharan S, Srivastava P, Singh M, Narasimham L, Gundu J, Sharma S, Kamboj RK, Palle VP.

J Med Chem. 2019 Dec 12;62(23):10563-10582. doi: 10.1021/acs.jmedchem.9b01562. Epub 2019 Nov 22.

PMID:
31710479
3.

Modifications of flexible nonyl chain and nucleobase head group of (+)-erythro-9-(2's-hydroxy-3's-nonyl)adenine [(+)-EHNA] as adenosine deaminase inhibitors.

Kandalkar SR, Ramaiah PA, Joshi M, Wavhal A, Waman Y, Raje AA, Tambe A, Ansari S, De S, Palle VP, Mookhtiar KA, Deshpande AM, Barawkar DA.

Bioorg Med Chem. 2017 Oct 15;25(20):5799-5819. doi: 10.1016/j.bmc.2017.09.015. Epub 2017 Sep 14.

PMID:
28951094
4.

Discovery of Potent and Selective A2A Antagonists with Efficacy in Animal Models of Parkinson's Disease and Depression.

Basu S, Barawkar DA, Ramdas V, Naykodi M, Shejul YD, Patel M, Thorat S, Panmand A, Kashinath K, Bonagiri R, Prasad V, Bhat G, Quraishi A, Chaudhary S, Magdum A, Meru AV, Ghosh I, Bhamidipati RK, Raje AA, Madgula VLM, De S, Rouduri SR, Palle VP, Chugh A, Hariharan N, Mookhtiar KA.

ACS Med Chem Lett. 2017 Jul 5;8(8):835-840. doi: 10.1021/acsmedchemlett.7b00175. eCollection 2017 Aug 10.

5.

Design and synthesis of novel xanthine derivatives as potent and selective A2B adenosine receptor antagonists for the treatment of chronic inflammatory airway diseases.

Basu S, Barawkar DA, Ramdas V, Patel M, Waman Y, Panmand A, Kumar S, Thorat S, Naykodi M, Goswami A, Reddy BS, Prasad V, Chaturvedi S, Quraishi A, Menon S, Paliwal S, Kulkarni A, Karande V, Ghosh I, Mustafa S, De S, Jain V, Banerjee ER, Rouduri SR, Palle VP, Chugh A, Mookhtiar KA.

Eur J Med Chem. 2017 Jul 7;134:218-229. doi: 10.1016/j.ejmech.2017.04.014. Epub 2017 Apr 12.

PMID:
28415011
6.

Discovery of liver-directed glucokinase activator having anti-hyperglycemic effect without hypoglycemia.

Deshpande AM, Bhuniya D, De S, Dave B, Vyavahare VP, Kurhade SH, Kandalkar SR, Naik KP, Kobal BS, Kaduskar RD, Basu S, Jain V, Patil P, Chaturvedi Joshi S, Bhat G, Raje AA, Reddy S, Gundu J, Madgula V, Tambe S, Shitole P, Umrani D, Chugh A, Palle VP, Mookhtiar KA.

Eur J Med Chem. 2017 Jun 16;133:268-286. doi: 10.1016/j.ejmech.2017.03.042. Epub 2017 Mar 24.

PMID:
28390958
7.

Design and synthesis of novel, potent and selective hypoxanthine analogs as adenosine A1 receptor antagonists and their biological evaluation.

Koul S, Ramdas V, Barawkar DA, Waman YB, Prasad N, Madadi SK, Shejul YD, Bonagiri R, Basu S, Menon S, Reddy SB, Chaturvedi S, Chennamaneni SR, Bedse G, Thakare R, Gundu J, Chaudhary S, De S, Meru AV, Palle V, Chugh A, Mookhtiar KA.

Bioorg Med Chem. 2017 Mar 15;25(6):1963-1975. doi: 10.1016/j.bmc.2017.02.029. Epub 2017 Feb 16.

PMID:
28238512
8.

Design, Synthesis of Novel, Potent, Selective, Orally Bioavailable Adenosine A2A Receptor Antagonists and Their Biological Evaluation.

Basu S, Barawkar DA, Thorat S, Shejul YD, Patel M, Naykodi M, Jain V, Salve Y, Prasad V, Chaudhary S, Ghosh I, Bhat G, Quraishi A, Patil H, Ansari S, Menon S, Unadkat V, Thakare R, Seervi MS, Meru AV, De S, Bhamidipati RK, Rouduri SR, Palle VP, Chug A, Mookhtiar KA.

J Med Chem. 2017 Jan 26;60(2):681-694. doi: 10.1021/acs.jmedchem.6b01584. Epub 2017 Jan 17.

PMID:
28055204
9.

A2B adenosine receptor antagonists: Design, synthesis and biological evaluation of novel xanthine derivatives.

Basu S, Barawkar DA, Ramdas V, Waman Y, Patel M, Panmand A, Kumar S, Thorat S, Bonagiri R, Jadhav D, Mukhopadhyay P, Prasad V, Reddy BS, Goswami A, Chaturvedi S, Menon S, Quraishi A, Ghosh I, Dusange S, Paliwal S, Kulkarni A, Karande V, Thakre R, Bedse G, Rouduri S, Gundu J, Palle VP, Chugh A, Mookhtiar KA.

Eur J Med Chem. 2017 Feb 15;127:986-996. doi: 10.1016/j.ejmech.2016.11.007. Epub 2016 Nov 8.

PMID:
27842891
10.

Synthesis and evaluation of 4,5-dihydro-5-methylisoxazolin-5-carboxamide derivatives as VLA-4 antagonists.

Soni A, Rehman A, Naik K, Dastidar S, Alam MS, Ray A, Chaira T, Shah V, Palle VP, Cliffe IA, Sattigeri VJ.

Bioorg Med Chem Lett. 2013 Mar 1;23(5):1482-5. doi: 10.1016/j.bmcl.2012.12.043. Epub 2012 Dec 21.

PMID:
23312947
11.

Discovery of pyrazole carboxylic acids as potent inhibitors of rat long chain L-2-hydroxy acid oxidase.

Barawkar DA, Bandyopadhyay A, Deshpande A, Koul S, Kandalkar S, Patil P, Khose G, Vyas S, Mone M, Bhosale S, Singh U, De S, Meru A, Gundu J, Chugh A, Palle VP, Mookhtiar KA, Vacca JP, Chakravarty PK, Nargund RP, Wright SD, Roy S, Graziano MP, Cully D, Cai TQ, Singh SB.

Bioorg Med Chem Lett. 2012 Jul 1;22(13):4341-7. doi: 10.1016/j.bmcl.2012.05.020. Epub 2012 May 11.

PMID:
22658862
12.

Discovery of novel and potent heterocyclic carboxylic acid derivatives as protein tyrosine phosphatase 1B inhibitors.

Basu S, Prasad UV, Barawkar DA, De S, Palle VP, Menon S, Patel M, Thorat S, Singh UP, Das Sarma K, Waman Y, Niranjan S, Pathade V, Gaur A, Reddy S, Ansari S.

Bioorg Med Chem Lett. 2012 Apr 15;22(8):2843-9. doi: 10.1016/j.bmcl.2012.02.070. Epub 2012 Mar 1.

PMID:
22424978
13.

Potent and Selective Inhibitors of Long Chain l-2-Hydroxy Acid Oxidase Reduced Blood Pressure in DOCA Salt-Treated Rats.

Barawkar DA, Meru A, Bandyopadhyay A, Banerjee A, Deshpande AM, Athare C, Koduru C, Khose G, Gundu J, Mahajan K, Patil P, Kandalkar SR, Niranjan S, Bhosale S, De S, Mukhopadhyay S, Chaudhary S, Koul S, Singh U, Chugh A, Palle VP, Mookhtiar KA, Vacca J, Chakravarty PK, Nargund RP, Wright SD, Roy S, Graziano MP, Singh SB, Cully D, Cai TQ.

ACS Med Chem Lett. 2011 Oct 7;2(12):919-23. doi: 10.1021/ml2001938. eCollection 2011 Dec 8.

14.

Discovery of a potent and selective small molecule hGPR91 antagonist.

Bhuniya D, Umrani D, Dave B, Salunke D, Kukreja G, Gundu J, Naykodi M, Shaikh NS, Shitole P, Kurhade S, De S, Majumdar S, Reddy SB, Tambe S, Shejul Y, Chugh A, Palle VP, Mookhtiar KA, Cully D, Vacca J, Chakravarty PK, Nargund RP, Wright SD, Graziano MP, Singh SB, Roy S, Cai TQ.

Bioorg Med Chem Lett. 2011 Jun 15;21(12):3596-602. doi: 10.1016/j.bmcl.2011.04.091. Epub 2011 Apr 28.

PMID:
21571530
15.

Synthesis of novel sugar-lactam conjugates using the Aubé reaction.

Kurhade SE, Mengawade T, Bhuniya D, Palle VP, Reddy DS.

Org Biomol Chem. 2011 Feb 7;9(3):744-7. doi: 10.1039/c0ob00719f. Epub 2010 Nov 17.

PMID:
21082141
16.

Synthesis and biological activity of N-substituted aminocarbonyl-1,3-dioxolanes as VLA-4 antagonists.

Rehman A, Soni A, Naik K, Nair S, Palle VP, Dastidar S, Ray A, Alam MS, Salman M, Cliffe IA, Sattigeri V.

Bioorg Med Chem Lett. 2010 Sep 15;20(18):5514-20. doi: 10.1016/j.bmcl.2010.07.069. Epub 2010 Jul 23.

PMID:
20705461
17.

Pharmacology of a novel, orally active PDE4 inhibitor.

Dastidar SG, Ray A, Shirumalla R, Rajagopal D, Chaudhary S, Nanda K, Sharma P, Seth MK, Balachandran S, Gupta N, Palle V.

Pharmacology. 2009;83(5):275-86. doi: 10.1159/000209608. Epub 2009 Mar 25.

PMID:
19321962
18.

Synthesis and optimization of novel and selective muscarinic M(3) receptor antagonists.

Kumar N, Kaur K, Aeron S, Dharmarajan S, Silamkoti AD, Mehta A, Gupta S, Chugh A, Gupta JB, Salman M, Palle VP, Cliffe IA.

Bioorg Med Chem Lett. 2007 Sep 15;17(18):5256-60. Epub 2007 Jun 30.

PMID:
17629699
19.

Novel 1,3-disubstituted 8-(1-benzyl-1H-pyrazol-4-yl) xanthines: high affinity and selective A2B adenosine receptor antagonists.

Kalla RV, Elzein E, Perry T, Li X, Palle V, Varkhedkar V, Gimbel A, Maa T, Zeng D, Zablocki J.

J Med Chem. 2006 Jun 15;49(12):3682-92.

PMID:
16759111
20.

Novel 1,3-dipropyl-8-(1-heteroarylmethyl-1H-pyrazol-4-yl)-xanthine derivatives as high affinity and selective A2B adenosine receptor antagonists.

Elzein E, Kalla R, Li X, Perry T, Parkhill E, Palle V, Varkhedkar V, Gimbel A, Zeng D, Lustig D, Leung K, Zablocki J.

Bioorg Med Chem Lett. 2006 Jan 15;16(2):302-6. Epub 2005 Nov 4.

PMID:
16275090
21.

The discovery of a selective, high affinity A(2B) adenosine receptor antagonist for the potential treatment of asthma.

Zablocki J, Kalla R, Perry T, Palle V, Varkhedkar V, Xiao D, Piscopio A, Maa T, Gimbel A, Hao J, Chu N, Leung K, Zeng D.

Bioorg Med Chem Lett. 2005 Feb 1;15(3):609-12.

PMID:
15664822
22.

2-Pyrazolyl-N(6)-substituted adenosine derivatives as high affinity and selective adenosine A(3) receptor agonists.

Elzein E, Palle V, Wu Y, Maa T, Zeng D, Zablocki J.

J Med Chem. 2004 Sep 9;47(19):4766-73.

PMID:
15341491
23.

Structure-affinity relationships of 5'-aromatic ethers and 5'-aromatic sulfides as partial A1 adenosine agonists, potential supraventricular anti-arrhythmic agents.

Morrison CF, Elzein E, Jiang B, Ibrahim PN, Marquart T, Palle V, Shenk KD, Varkhedkar V, Maa T, Wu L, Wu Y, Zeng D, Fong I, Lustig D, Leung K, Zablocki JA.

Bioorg Med Chem Lett. 2004 Jul 16;14(14):3793-7.

PMID:
15203164
24.

Affinity and intrinsic efficacy (IE) of 5'-carbamoyl adenosine analogues for the A1 adenosine receptor--efforts towards the discovery of a chronic ventricular rate control agent for the treatment of atrial fibrillation (AF).

Palle VP, Varkhedkar V, Ibrahim P, Ahmed H, Li Z, Gao Z, Ozeck M, Wu Y, Zeng D, Wu L, Leung K, Chu N, Zablocki JA.

Bioorg Med Chem Lett. 2004 Jan 19;14(2):535-9.

PMID:
14698198
25.

Structure-affinity relationships of the affinity of 2-pyrazolyl adenosine analogues for the adenosine A2A receptor.

Palle VP, Elzein EO, Gothe SA, Li Z, Gao Z, Meyer S, Blackburn B, Zablocki JA.

Bioorg Med Chem Lett. 2002 Oct 21;12(20):2935-9.

PMID:
12270178
26.

2-substituted pi system derivatives of adenosine that are coronary vasodilators acting via the A2A adenosine receptor.

Zablocki J, Palle V, Blackburn B, Elzein E, Nudelman G, Gothe S, Gao Z, Li Z, Meyer S, Belardinelli L.

Nucleosides Nucleotides Nucleic Acids. 2001 Apr-Jul;20(4-7):343-60.

PMID:
11563047
27.

Novel short-acting A2A adenosine receptor agonists for coronary vasodilation: inverse relationship between affinity and duration of action of A2A agonists.

Gao Z, Li Z, Baker SP, Lasley RD, Meyer S, Elzein E, Palle V, Zablocki JA, Blackburn B, Belardinelli L.

J Pharmacol Exp Ther. 2001 Jul;298(1):209-18.

PMID:
11408544
28.

A partial agonist of the A(1)-adenosine receptor selectively slows AV conduction in guinea pig hearts.

Wu L, Belardinelli L, Zablocki JA, Palle V, Shryock JC.

Am J Physiol Heart Circ Physiol. 2001 Jan;280(1):H334-43.

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