Synthesis and investigation of anticancer, antibacterial activities and carbonic anhydrase, acetylcholinesterase inhibition profiles of novel (3aR,4S,7R,7aS)-2-[4-[1-acetyl-5-(aryl/heteroaryl)-4,5-dihydro-1H-pyrazol-3-yl]phenyl]-3a,4,7,7a-tetrahydro-1H-4,7-methanoisoindole-1,3(2H)-diones

Kocyigit, Umit M.; BUDAK, YAKUP; GÜRDERE, MELİHA BURCU; Duru, Nese; Taslimi, Parham; Gulcin, Ilhami; CEYLAN, MUSTAFA

doi:10.1007/s00706-019-2350-z

Synthesis and investigation of anticancer, antibacterial activities and carbonic anhydrase, acetylcholinesterase inhibition profiles of novel (3aR,4S,7R,7aS)-2-[4-[1-acetyl-5-(aryl/heteroaryl)-4,5-dihydro-1H-pyrazol-3-yl]phenyl]-3a,4,7,7a-tetrahydro-1H-4,7-methanoisoindole-1,3(2H)-diones

Yazarlar (7)

Umit M. Kocyigit
Cumhuriyet Üniversitesi, Türkiye

Prof. Dr. Yakup BUDAK Tokat Gaziosmanpaşa Üniversitesi, Türkiye

Prof. Dr. Meliha Burcu GÜRDERE Tokat Gaziosmanpaşa Üniversitesi, Türkiye

Nese Duru
Tokat Gaziosmanpaşa Üniversitesi, Türkiye

Parham Taslimi
Atatürk Üniversitesi, Türkiye

Ilhami Gulcin
Atatürk Üniversitesi, Türkiye

Prof. Dr. Mustafa CEYLAN Tokat Gaziosmanpaşa Üniversitesi, Türkiye

Makale Türü	Özgün Makale
Makale Alt Türü	SSCI, AHCI, SCI, SCI-Exp dergilerinde yayınlanan tam makale
Dergi Adı	Monatshefte Fur Chemie
Dergi ISSN	0026-9247 Wos Dergi Scopus Dergi
Dergi Tarandığı Indeksler	SCI-Expanded
Makale Dili	İngilizce
Basım Tarihi	04-2019
Cilt No	150
Sayı	4
Sayfalar	721 / 731
DOI Numarası	10.1007/s00706-019-2350-z
Makale Linki	http://link.springer.com/10.1007/s00706-019-2350-z

Özet

Abstract: A series of novel 1,3,5-trisubstituted pyrazoline derivatives, (3aR,4S,7R,7aS)-2-[4-[1-acetyl-5-(aryl/heteroaryl)-4,5-dihydro-1H-pyrazol-3-yl]phenyl]-3a,4,7,7a-tetrahydro-1H-4,7-methanoisoindole-1,3(2H)-diones, were synthesized and evaluated for their antimicrobial and anticancer activities. In addition, the compounds were tested against acetylcholinesterase (AChE) enzyme and two physiologically relevant carbonic anhydrase I and II isozymes (hCA I and II). In this study, inhibition of hCA I and hCA II by the novel synthesized 1,3,5-trisubstituted pyrazolines was impressive, with K i values in the range of 3.33–7.90 nM for hCA I and 2.07–8.47 nM for hCA II, while the K i values of these compounds for AChE were recorded in the range of 9.61–48.42 nM, respectively. Two compounds can be investigated as the leader compounds because of their lowest K i values to make further detailed CA inhibition studies. Graphical abstract: [Figure not available: see fulltext.].

Anahtar Kelimeler

BM Sürdürülebilir Kalkınma Amaçları

Atıf Sayıları
WoS	37
SCOPUS	39

Synthesis and investigation of anticancer, antibacterial activities and carbonic anhydrase, acetylcholinesterase inhibition profiles of novel (3aR,4S,7R,7aS)-2-[4-[1-acetyl-5-(aryl/heteroaryl)-4,5-dihydro-1H-pyrazol-3-yl]phenyl]-3a,4,7,7a-tetrahydro-1H-4,7-methanoisoindole-1,3(2H)-diones

Dergi Adı	MONATSHEFTE FUR CHEMIE
Yayıncı	Springer
Açık Erişim	Hayır
ISSN	0026-9247
E-ISSN	1434-4475
CiteScore	3,4
SJR	0,321
SNIP	0,524

Synthesis and investigation of anticancer, antibacterial activities and carbonic anhydrase, acetylcholinesterase inhibition profiles of novel (3aR,4S,7R,7aS)-2-[4-[1-acetyl-5-(aryl/heteroaryl)-4,5-dihydro-1H-pyrazol-3-yl]phenyl]-3a,4,7,7a-tetrahydro-1H-4,7-methanoisoindole-1,3(2H)-diones

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