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Synthesis and Antibacterial Activity of New Cephalosporins with Lactonyloxyimino Moiety
Suh, Kwee-Hyun,Park, Joo-Woong The Pharmaceutical Society of Korea 1994 Archives of Pharmacal Research Vol.17 No.2
A series of $7-{2-(aminothiazol-4-yl)-2-Z-({\gamma}-lacton-3-yl)oxyiminoactamido}$ cephalosporins with various substituents at the 30position in cephem nucleus in cephem nucleus were synthesized and evaluated microbiologically. The tested compounds showed potent activities but were somewhat less active than cefotaxime or cefixime against a wide variety of Gram-positive and Gram-negative bacteria.
A Novel Synthetic Method for Bepotastine, a Histamine H1 Receptor Antagonist
Tae Hee Ha,Kwee-Hyun Suh,Gwan Sun Lee 대한화학회 2013 Bulletin of the Korean Chemical Society Vol.34 No.2
An efficient and alternative synthesis of enantiomerically pure (+)-(S)-4-(4-((4-chlorophenyl)(pyrid-2- yl)methoxy]piperidin-1-yl)butanoic acid, bepotastine (1) is described. The key resolution of (R/S)-bepotastine l-menthyl ester (3) is achived via diastereomeric salt crystallization using N-benzyloxycarbonyl-L-aspartic acid (NCbzLAA) as the resolving agent to provide (S)-bepotastine l-menthyl ester (S)-3. Hydrolysis of (S)- bepotastine l-menthyl ester (S)-3 afforded the desired bepotastine (1) with good yields and enantiopurity (> 99%). Finally, bepotastine besilate (4) and bepotastine calcium (5) are achived by salt formation of bepotastine (1) with benzene sulfonic acid and calcium salt respectively. The reaction conditions were optimized to make suitable for commercial scale production.
A Novel Synthetic Method for Bepotastine, a Histamine H1 Receptor Antagonist
Ha, Tae Hee,Suh, Kwee-Hyun,Lee, Gwan Sun Korean Chemical Society 2013 Bulletin of the Korean Chemical Society Vol.34 No.2
An efficient and alternative synthesis of enantiomerically pure (+)-(S)-4-(4-((4-chlorophenyl)(pyrid-2-yl)methoxy]piperidin-1-yl)butanoic acid, bepotastine (1) is described. The key resolution of (R/S)-bepotastine l-menthyl ester (3) is achived via diastereomeric salt crystallization using N-benzyloxycarbonyl-L-aspartic acid (NCbzLAA) as the resolving agent to provide (S)-bepotastine l-menthyl ester (S)-3. Hydrolysis of (S)-bepotastine l-menthyl ester (S)-3 afforded the desired bepotastine (1) with good yields and enantiopurity (> 99%). Finally, bepotastine besilate (4) and bepotastine calcium (5) are achived by salt formation of bepotastine (1) with benzene sulfonic acid and calcium salt respectively. The reaction conditions were optimized to make suitable for commercial scale production.
Safety pharmacology of sibutramine mesylate, an anti-obesity drug
Kim, Eun-Joo,Park, Eun-Kyung,Suh, Kwee-Hyun Sage Publications 2005 Human & experimental toxicology Vol.24 No.3
<P>Sibutramine mesylate is a new anti-obesity drug. It is a crystalline salt of sibutramine developed to improve the solubility of sibutramine hydrochloride. Methanesulfonic acid was used as a salt-forming acid instead of hydrochloric acid, resulting in a greatly improved solubility of 1000 mg/mL in water. Sibutramine mesylate was administered orally to ICR mice, Sprague <SUP>/</SUP> respiratory system and the other organ systems. Following administration of sibutramine mesylate, spontaneous locomotor activity was significantly increased from 120 min to 24 hours at 3.45 mg/kg and from 30 min to 24 hours at 11.50 mg/kg. Furthermore, there were a decrease in hexobarbitalinduced sleep time, an increase in respiratory rate at 120 min, increases in intestinal transport capacity and gastric pH at 11.50 mg/kg, and decreases in gastric <SUP>/</SUP> Dawley rats, and beagle dogs at dose levels of 1.15, 3.45, and 11.50 mg/kg to measure its effects on the central nervous system (CNS), general behaviour, cardiovascular volume and total acidity at 3.45 and 11.50 mg/kg. However sibutramine mesylate caused no effects on general behaviour, motor coordination, body temperature, analgesia, convulsion, blood pressure, heart rate, electrocardiogram, cardiac functions of the isolated rat heart, isolated smooth muscles and renal function. Based on the above results, it was concluded that sibutramine mesylate caused effects on the spontaneous locomotor activity, hexobarbital-induced sleep time, respiration, gastrointestinal transport, and gastric secretion at a dose level of 3.45 mg/kg or greater but caused no effects on other general pharmacological reactions.</P>
Pharmacological evaluation of HM41322, a novel SGLT1/2 dual inhibitor, in vitro and in vivo
Lee, Kyu Hang,Lee, Sang Don,Kim, Namdu,Suh, Kwee Hyun,Kim, Young Hoon,Sim, Sang Soo The Korean Society of Pharmacology 2019 The Korean Journal of Physiology & Pharmacology Vol.23 No.1
HM41322 is a novel oral sodium-glucose cotransporter (SGLT) 1/2 dual inhibitor. In this study, the in vitro and in vivo pharmacokinetic and pharmacologic profiles of HM41322 were compared to those of dapagliflozin. HM41322 showed a 10-fold selectivity for SGLT2 over SGLT1. HM41322 showed an inhibitory effect on SGLT2 similar to dapagliflozin, but showed a more potent inhibitory effect on SGLT1 than dapagliflozin. The maximum plasma HM41322 level after single oral doses at 0.1, 1, and 3 mg/kg were 142, 439, and 1830 ng/ml, respectively, and the $T_{1/2}$ was 3.1 h. HM41322 was rapidly absorbed and reached the circulation within 15 min. HM41322 maximized urinary glucose excretion by inhibiting both SGLT1 and SGLT2 in the kidney. HM41322 3 mg/kg caused the maximum urinary glucose excretion in normoglycemic mice ($19.32{\pm}1.16mg/g$) at 24 h. In normal and diabetic mice, HM41322 significantly reduced glucose excursion. Four-week administration of HM41322 in db/db mice reduced HbA1c in a dose dependent manner. Taken together, HM41322 showed a favorable preclinical profile of postprandial glucose control through dual inhibitory activities against SGLT1 and SGLT2.
Sibutramine의 신규 염인 Sibutramine Mesilate Hemihydrate의 랫드와 비글견에 대한 단회 경구투여 독성
한수철(Su-Cheol Han),차신우(Shin-Woo Cha),서정은(Jeong-Eun Suh),서귀현(Kwee-Hyun Suh) 한국실험동물학회 2004 Laboratory Animal Research Vol.20 No.4
This study was to investigate single-dose toxicities of sibutramine mesilate hemihydrate (SIBMS), a new salt of sibutramine, in Sprague-Dawley (SD) rats and beagle dogs. The test article was administrated once by gavage to rats at dose levels of 43.1, 86.3, 172.5 and 345.0 ㎎/㎏/day, and to beagle dogs at dose levels of 23.0 and 43.0 ㎎/㎏/day, respectively. For comparison, sibutramine hydrochloride monohydrate (SIBCH) used clinically as anti-obesity agent was administrated to SD rats at dose levels of 37.5, 75.0, 150.0 and 300.0 ㎎/㎏/day and at dose levels of 20.0 and 40.0 ㎎/㎏/day to beagle dogs. In rats, deaths, temporary body weight loss, increased locomotive activity and salivation were observed and the approximate lethal dose of SIBMS was 345.0 ㎎/㎏ for males and 172.5 ㎎/㎏ for females and those of SIBCH was 300.0 ㎎/㎏ for males and 150.0 ㎎/㎏ for females, respectively. In beagle dog, death, temporary body weight loss, vomiting, salivation, hyperemic conjunctiva, anorexia and lacrimation were found. The toxic effect dose of SIBMS were 46.0 ㎎/㎏ and those of SIBCH were 40.0 ㎎/㎏ for both sexes.
Comparative Antihypertensive Activities of Losartan and HM70186 in Rats with Hepatic Dysfunction
Jae-Hong Choi,Sunhee Shin,박동선,Jeong Hee Jeon,Bong Ho Choi,Min-Jung Jang,주성수,오기완,홍진태,김윤배,Kwee-Hyun Suh 대한약학회 2009 Archives of Pharmacal Research Vol.32 No.7
HM70186, a medoxomil ester of EXP3174 which is an active metabolite of angiotensin Ⅱ receptor blocker losartan, was synthesized, and its antihypertensive efficacy was evaluated in rats with hepatic dysfunction. Male Wistar rats were intraperitoneally injected with 0.5 mL/kg of carbon tetrachloride to cause hepatic injury, and implanted with an osmotic minipumpcontaining angiotensin Ⅱ (0.4 mg/kg/day) to induce hypertension. After confirmation of bothhepatic damage and hypertension, the rats were orally administered losartan or HM70186,and then blood pressure and heart rate were monitored for 24 h. In normal animals, angiotensinII-induced hypertension was lowered by losartan, resulting in an ED-30 mmHg of 9.05 mg/kg. HM70186 also immediately decreased the blood pressure in a dose-dependent manner,exhibiting an ED-30 mmHg of 0.89 ng/kg (10,000 times the potency observed with losartan). Moreover, HM70186 (3 ng/kg) exerted a strong antihypertensive effect even in rats withhepatic injury, while losartan (10 μg/kg) was ineffective. These results suggest that HM70186could be a promising candidate for the treatment of hypertension accompanied by hepatic dysfunction.