69999-18-4Relevant academic research and scientific papers
Discovery of indane propanamides as potent and selective TRPV1 antagonists
Ahn, Songyeon,Kim, Yong Soo,Kim, Myeong Seup,Ann, Jihyae,Ha, Heejin,Yoo, Young Dong,Kim, Young Ho,Blumberg, Peter M.,Frank-Foltyn, Robert,Bahrenberg, Gregor,Stockhausen, Hannelore,Christoph, Thomas,Lee, Jeewoo
, (2020/01/03)
A series of indane-type acetamide and propanamide analogues were investigated as TRPV1 antagonists. The analysis of structure–activity relationship indicated that indane A-region analogues exhibited better antagonism than did the corresponding 2,3-dihydrobenzofuran and 1,3-benzodioxole surrogates. Among them, antagonist 36 exhibited potent and selective antagonism toward capsaicin for hTRPV1 and mTRPV1. Further, in vivo studies indicated that antagonist 36 showed excellent analgesic activity in both phases of the formalin mouse pain model and inhibited the pain behavior completely at a dose of 1 mg/kg in the 2nd phase.
Synthesis and anti-inflammatory activity of hydrazones bearing biphenyl moiety and vanillin based hybrids
Kumar Reddy,Kathale, Niren E.
, p. 971 - 978 (2017/05/29)
The intense research work in the field of medicinal chemistry has enhanced the significance of Biphenyl moiety as pharmacologically important compound. Some of the compounds bearing Biphenyl moiety possess important medicinal properties like antihypertensive and calcium channel blocker, anti-inflammatory, diuretic, anti-diabetic activity, antipsychotic and anxiolytic activity. The present article describes the synthesis of novel benzohydrazides and 2-phenylacetohydrazides bearing Biphenyl moiety and vanillin hybrid. The synthesized compounds (31-40) were characterized by 1H NMR, Mass and IR spectroscopic techniques and were evaluated for anti-inflammatory activity by carrageenan paw edema method. The results of the study revealed that compounds 39 and 40 (bearing 2-(4-nitrophenyl)acetohydrazide and 2-(2,3-dihydrobenzofuran-5-yl)acetohydrazide) showed maximum anti-inflammatory activity while the compounds 31, 32, 33, 34 and 38 bearing benzohydrazides displayed moderate anti-inflammatory activity.
Synthesis and anti-inflammatory activity of hydrazide-hydrazones bearing anacardic acid and 1,2,3-triazole ring based hybrids
Kumar Reddy,Kathale, Niren E
, p. 2930 - 2936 (2018/02/20)
A novel series of hydrazide-hydrazone derivatives 39-50, linked with anacardic acid motif and 1,2,3-triazole ring were synthesized by reacting 4-(1-(2-methoxy-6-pentadecylbenzyl)-1H-1, 2, 3-triazol-4-yl)benzaldehyde with 2-phenyl-acetohydrazides and benzohydrazides. The structures of the newly synthesized hydrazide-hydrazone derivatives 39-50 were confirmed by 1H NMR, MS and IR spectroscopic tools. These compounds were also evaluated for their anti-inflammatory activity by carrageenan paw edema method.
SUBSTITUTED PYRROLIDINES
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Page/Page column 31, (2009/01/24)
Disclosed herein are substituted pyrrolidine-based muscarinic receptor modulators of Formula I, process of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.
