SYNTHETIC APPROACHES, CHEMICAL MODIFICATION AND BIOLOGICAL ACTIVITY OF NON-CONDENSED 1,3,4-THIADIAZOLE DERIVATIVES

被引:0
作者
Lelyukh, Maryan [1 ]
Adamchuk, Svitlana [1 ]
Harkov, Stefan [2 ]
Chaban, Ihor [1 ]
Demchuk, Inna [3 ]
Shelepeten, Lesya [1 ]
Chaban, Taras [4 ]
机构
[1] Danylo Halytsky Lviv Natl Med Univ, Dept Pharmaceut Chem FPGE, Pekarska 69, UA-79010 Lvov, Ukraine
[2] Burgas Univ Prof Dr Asen Zlatarov, Dept Pharm, Med Coll, St Stambolov 69 Blvd, Burgas 8000, Bulgaria
[3] Danylo Halytsky Lviv Natl Med Univ, Dept Pharmaceut Organ & Bioorgan Chem, Pekarska 69, UA-79010 Lvov, Ukraine
[4] Danylo Halytsky Lviv Natl Med Univ, Dept Gen Bioinorgan Phys & Colloidal Chem, Pekarska 69, UA-79010 Lvov, Ukraine
关键词
synthesis; 1,3,4-thiadiazoles; chemical modification; biological activity;
D O I
暂无
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The chemical features of 1,3,4-thiadiazoles were described in a numerous reviews focusing on the main approaches to the synthesis and modification. Simultaneously, thiadiazole scaffold was identified as the main structural component of approved drugs and biological agents with antimicrobial, antiviral, antitubercular, anti-inflammatory, anticonvulsant and analgetic activity. The significant biological activity of thiadiazole derivates promotes the scientists to further investigation of this heterocycle as a building block for medicinal chemistry. In this review, we discuss the efforts to identify new promising compounds based on aryl/heteryl substituted non-condensed thiadiazoles highliting the main approaches for the conjugation (hybridization) of heterocycles, derivatization and their pharmacological profile.
引用
收藏
页码:72 / 88
页数:17
相关论文
共 40 条
  • [1] Design, synthesis, and docking studies of new 1,3,4-thiadiazole-2thione derivatives with carbonic anhydrase inhibitory activity
    Abdel-Hamid, Mohammed K.
    Abdel-Hafez, Atef A.
    El-Koussi, Nawal A.
    Mahfouz, Nadia M.
    Innocenti, Alessio
    Supuran, Claudlu T.
    [J]. BIOORGANIC & MEDICINAL CHEMISTRY, 2007, 15 (22) : 6975 - 6984
  • [2] Synthesis and biological activity of new 1,3,4-thiadiazole derivatives
    Aly, AA
    El-Sayed, R
    [J]. CHEMICAL PAPERS, 2006, 60 (01): : 56 - 60
  • [3] New heterocyclic compounds from 1,2,4-triazole and 1,3,4-thiadiazole class bearing diphenylsulfone moieties. Synthesis, characterization and antimicrobial activity evaluation
    Barbuceanu, Stefania-Felicia
    Saramet, Gabriel
    Almajan, Gabriela Laura
    Draghici, Constantin
    Barbuceanu, Florica
    Bancescu, Gabriela
    [J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2012, 49 : 417 - 423
  • [4] 1,3,4-OXADIAZOLE, 1,3,4-THIADIAZOLE, AND 1,2,4-TRIAZOLE ANALOGS OF THE FENAMATES - IN-VITRO INHIBITION OF CYCLOOXYGENASE AND 5-LIPOXYGENASE ACTIVITIES
    BOSCHELLI, DH
    CONNOR, DT
    BORNEMEIER, DA
    DYER, RD
    KENNEDY, JA
    KUIPERS, PJ
    OKONKWO, GC
    SCHRIER, DJ
    WRIGHT, CD
    [J]. JOURNAL OF MEDICINAL CHEMISTRY, 1993, 36 (13) : 1802 - 1810
  • [5] Synthesis, antioxidant properties and radioprotective effects of new benzothiazoles and thiadiazoles
    Cressier, Damien
    Prouillac, Caroline
    Hernandez, Pierre
    Amourette, Christine
    Diserbo, Michel
    Lion, Claude
    Rima, Ghassoub
    [J]. BIOORGANIC & MEDICINAL CHEMISTRY, 2009, 17 (14) : 5275 - 5284
  • [6] New synthetic routes to 1,3,4-thiadiazole derivatives
    Elagamey, A. A.
    El-Taweel, F. M. A.
    Abu El-Enein, R. A. N.
    [J]. PHOSPHORUS SULFUR AND SILICON AND THE RELATED ELEMENTS, 2006, 181 (09) : 2155 - 2176
  • [7] Synthesis and antimycobacterial activity of some alkyl [5-(nitroaryl)-1,3,4-thiadiazol-2-ylthio]propionates
    Foroumadi, A
    Kargar, Z
    Sakhteman, A
    Sharifzadeh, Z
    Feyzmohammadi, R
    Kazemi, M
    Shafiee, A
    [J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2006, 16 (05) : 1164 - 1167
  • [8] Synthesis of 2-aminoaryl-5-substituted-1,3,4-thiadiazoles in a thermal 1,3-dipolar cycloaddition reaction
    Gobis, K
    Foks, H
    Zwolska, Z
    Augustynowicz-Kopec, E
    [J]. PHOSPHORUS SULFUR AND SILICON AND THE RELATED ELEMENTS, 2005, 180 (12) : 2653 - 2666
  • [9] 1,3,4-Thiadiazoles: A potent multi targeted pharmacological scaffold
    Haider, Saqlain
    Alam, Mohammad Samar
    Hamid, Hinna
    [J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2015, 92 : 156 - 177
  • [10] Synthesis, biological evaluation, and molecular modeling studies of new 1,3,4-oxadiazole- and 1,3,4-thiadiazole-substituted 4-oxo-4H-pyrido[1,2-a]pyrimidines as anti-HIV-1 agents
    Hajimahdi, Z.
    Zarghi, A.
    Zabihollahi, R.
    Aghasadeghi, M. R.
    [J]. MEDICINAL CHEMISTRY RESEARCH, 2013, 22 (05) : 2467 - 2475